Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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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
77846754 181960 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 435 5 1 3 6.3 Cc1cc(OC2CCC3(CCCC3)CC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4787458 181960 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 435 5 1 3 6.3 Cc1cc(OC2CCC3(CCCC3)CC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
77846502 180058 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 423 6 2 3 6.1 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNC2CC(C(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4754965 180058 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 423 6 2 3 6.1 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNC2CC(C(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
12573 980 1 None - 1 Human 10.0 pEC50 = 10 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 10.1021/acsmedchemlett.0c00631
77846592 980 1 None - 1 Human 10.0 pEC50 = 10 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 10.1021/acsmedchemlett.0c00631
CHEMBL4748198 980 1 None - 1 Human 10.0 pEC50 = 10 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 10.1021/acsmedchemlett.0c00631
77847762 182841 0 None - 1 Human 10.0 pEC50 = 10 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 397 7 2 3 5.7 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNCCC(=O)O)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4798593 182841 0 None - 1 Human 10.0 pEC50 = 10 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 397 7 2 3 5.7 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNCCC(=O)O)c2ccccc12 10.1021/acsmedchemlett.0c00631
77846503 181728 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 451 6 2 3 6.9 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNC2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4784199 181728 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 451 6 2 3 6.9 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNC2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
11452022 3539 33 None -3 6 Human 9.5 pEC50 = 9.5 Functional
Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligandAgonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/jm050242f
6996 3539 33 None -3 6 Human 9.5 pEC50 = 9.5 Functional
Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligandAgonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/jm050242f
CHEMBL366208 3539 33 None -3 6 Human 9.5 pEC50 = 9.5 Functional
Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligandAgonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/jm050242f
25192001 7976 0 None -2 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay
ChEMBL 413 12 4 4 3.5 CCCCCCCCc1ccc2c(c1)CC[C@@H](C(N)(CO)COP(=O)(O)O)C2 10.1016/j.bmcl.2010.02.006
CHEMBL1091103 7976 0 None -2 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay
ChEMBL 413 12 4 4 3.5 CCCCCCCCc1ccc2c(c1)CC[C@@H](C(N)(CO)COP(=O)(O)O)C2 10.1016/j.bmcl.2010.02.006
11502996 158181 36 None -11 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISAAgonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISA
ChEMBL 435 9 1 4 5.0 CCCc1ccc(COc2ccc3c(c2)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1 10.1021/acs.jmedchem.7b00785
CHEMBL4093489 158181 36 None -11 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISAAgonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISA
ChEMBL 435 9 1 4 5.0 CCCc1ccc(COc2ccc3c(c2)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1 10.1021/acs.jmedchem.7b00785
11452022 3539 33 None -3 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human S1P5RAgonist activity at human S1P5R
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/ml100301k
6996 3539 33 None -3 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human S1P5RAgonist activity at human S1P5R
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/ml100301k
CHEMBL366208 3539 33 None -3 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human S1P5RAgonist activity at human S1P5R
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/ml100301k
11452022 3539 33 None -3 6 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1016/j.bmcl.2010.02.006
6996 3539 33 None -3 6 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1016/j.bmcl.2010.02.006
CHEMBL366208 3539 33 None -3 6 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1016/j.bmcl.2010.02.006
11452022 3539 33 None -3 6 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assayAgonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/acsmedchemlett.0c00631
6996 3539 33 None -3 6 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assayAgonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/acsmedchemlett.0c00631
CHEMBL366208 3539 33 None -3 6 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assayAgonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/acsmedchemlett.0c00631
2924 1610 37 None -4 6 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human S1P5 receptor by GTPgammaS binding assayAgonist activity at human S1P5 receptor by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acsmedchemlett.5b00448
44398069 1610 37 None -4 6 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human S1P5 receptor by GTPgammaS binding assayAgonist activity at human S1P5 receptor by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acsmedchemlett.5b00448
9908268 1610 37 None -4 6 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human S1P5 receptor by GTPgammaS binding assayAgonist activity at human S1P5 receptor by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acsmedchemlett.5b00448
CHEMBL114606 1610 37 None -4 6 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human S1P5 receptor by GTPgammaS binding assayAgonist activity at human S1P5 receptor by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acsmedchemlett.5b00448
11222939 67233 6 None -9 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2010.01.118
44438254 67233 6 None -9 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2010.01.118
CHEMBL190006 67233 6 None -9 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2010.01.118
46881623 6685 0 None 5 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 477 9 2 6 4.1 Cc1cc(CN2CC(C(=O)O)C2)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
CHEMBL1083828 6685 0 None 5 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 477 9 2 6 4.1 Cc1cc(CN2CC(C(=O)O)C2)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
59384310 103912 0 None -2 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
ChEMBL 511 13 3 7 5.2 CCCCCCCCOc1ccc(-c2nnc([C@@](C)(N)COP(=O)(O)O)s2)cc1C(F)(F)F 10.1021/ml400194r
CHEMBL3102904 103912 0 None -2 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
ChEMBL 511 13 3 7 5.2 CCCCCCCCOc1ccc(-c2nnc([C@@](C)(N)COP(=O)(O)O)s2)cc1C(F)(F)F 10.1021/ml400194r
11452022 3539 33 None -3 6 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assayAgonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.8b01695
6996 3539 33 None -3 6 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assayAgonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.8b01695
CHEMBL366208 3539 33 None -3 6 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assayAgonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.8b01695
2924 1610 37 None -4 6 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.0c01109
44398069 1610 37 None -4 6 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.0c01109
9908268 1610 37 None -4 6 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.0c01109
CHEMBL114606 1610 37 None -4 6 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.0c01109
44412994 77917 0 None -7 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 499 7 1 6 5.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C(F)(F)F)C(F)(F)F)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL210942 77917 0 None -7 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 499 7 1 6 5.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C(F)(F)F)C(F)(F)F)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.084
77846505 179436 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 437 6 2 3 6.5 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNC2CCC(C(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4747262 179436 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 437 6 2 3 6.5 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNC2CCC(C(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
10883396 3592 39 None -2 14 Human 9.0 pEC50 = 9.0 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2006.10.014
5283560 3592 39 None -2 14 Human 9.0 pEC50 = 9.0 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2006.10.014
911 3592 39 None -2 14 Human 9.0 pEC50 = 9.0 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2006.10.014
CHEMBL225155 3592 39 None -2 14 Human 9.0 pEC50 = 9.0 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2006.10.014
11568622 157656 0 None -1 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISAAgonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISA
ChEMBL 450 9 1 5 4.7 CCCc1ccc(COc2ccc3c(c2C)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)n1 10.1021/acs.jmedchem.7b00785
CHEMBL4087932 157656 0 None -1 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISAAgonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISA
ChEMBL 450 9 1 5 4.7 CCCc1ccc(COc2ccc3c(c2C)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)n1 10.1021/acs.jmedchem.7b00785
77847765 182817 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 423 5 1 3 6.0 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CN2CCC(C(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4798181 182817 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 423 5 1 3 6.0 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CN2CCC(C(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
44599207 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 10.1016/j.bmcl.2013.09.058
5326 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 10.1016/j.bmcl.2013.09.058
9289 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 10.1016/j.bmcl.2013.09.058
CHEMBL2336071 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 10.1016/j.bmcl.2013.09.058
DB12371 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 10.1016/j.bmcl.2013.09.058
11619303 158404 0 None -3 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISAAgonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISA
ChEMBL 449 9 1 4 5.3 CCCc1ccc(COc2ccc3c(c2C)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1 10.1021/acs.jmedchem.7b00785
CHEMBL4095920 158404 0 None -3 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISAAgonist activity at human S1P5 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISA
ChEMBL 449 9 1 4 5.3 CCCc1ccc(COc2ccc3c(c2C)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1 10.1021/acs.jmedchem.7b00785
77846753 180267 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 449 5 1 3 6.7 Cc1cc(OC2CCC3(CCCCC3)CC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4757160 180267 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 449 5 1 3 6.7 Cc1cc(OC2CCC3(CCCCC3)CC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
90324880 179776 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 343 11 2 3 4.7 CCCCCCOc1cc(C)c2ccccc2c1CNCCC(=O)O 10.1021/acsmedchemlett.0c00631
CHEMBL4751484 179776 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 343 11 2 3 4.7 CCCCCCOc1cc(C)c2ccccc2c1CNCCC(=O)O 10.1021/acsmedchemlett.0c00631
77847763 181226 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 411 8 2 3 6.1 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNCCCC(=O)O)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4778095 181226 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 411 8 2 3 6.1 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNCCCC(=O)O)c2ccccc12 10.1021/acsmedchemlett.0c00631
46884020 8355 0 None -8 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay
ChEMBL 397 11 3 3 4.5 CCCCCCCCc1ccc2c(c1)CC[C@H]([C@@](C)(N)COP(=O)(O)O)C2 10.1016/j.bmcl.2010.02.006
CHEMBL1093686 8355 0 None -8 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay
ChEMBL 397 11 3 3 4.5 CCCCCCCCc1ccc2c(c1)CC[C@H]([C@@](C)(N)COP(=O)(O)O)C2 10.1016/j.bmcl.2010.02.006
10883396 3592 39 None -2 14 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/ml400194r
5283560 3592 39 None -2 14 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/ml400194r
911 3592 39 None -2 14 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/ml400194r
CHEMBL225155 3592 39 None -2 14 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/ml400194r
10904818 300 0 None -1 4 Human 8.7 pEC50 = 8.7 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 10.1016/j.bmcl.2005.09.038
2937 300 0 None -1 4 Human 8.7 pEC50 = 8.7 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 10.1016/j.bmcl.2005.09.038
CHEMBL382739 300 0 None -1 4 Human 8.7 pEC50 = 8.7 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 10.1016/j.bmcl.2005.09.038
44406004 72370 8 None -11 4 Human 8.7 pEC50 = 8.7 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 337 14 4 4 2.9 CCCCCCCCCC/C=C/[C@@H](O)[C@@H](N)COP(=O)(O)O 10.1016/j.bmcl.2005.09.038
CHEMBL199791 72370 8 None -11 4 Human 8.7 pEC50 = 8.7 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 337 14 4 4 2.9 CCCCCCCCCC/C=C/[C@@H](O)[C@@H](N)COP(=O)(O)O 10.1016/j.bmcl.2005.09.038
11678855 133920 0 None -1 3 Human 8.7 pEC50 = 8.7 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 607 21 4 10 5.9 C[C@@](N)(CCc1ccc(OCCCCCCCCCCCNc2ccc([N+](=O)[O-])c3nonc23)cc1)COP(=O)(O)O 10.1016/j.bmcl.2005.09.038
CHEMBL371758 133920 0 None -1 3 Human 8.7 pEC50 = 8.7 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 607 21 4 10 5.9 C[C@@](N)(CCc1ccc(OCCCCCCCCCCCNc2ccc([N+](=O)[O-])c3nonc23)cc1)COP(=O)(O)O 10.1016/j.bmcl.2005.09.038
16215109 146975 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](COP(=O)(O)O)N[C@@H]2CO)cc1 10.1016/j.bmcl.2006.10.014
44438256 146975 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](COP(=O)(O)O)N[C@@H]2CO)cc1 10.1016/j.bmcl.2006.10.014
CHEMBL393055 146975 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](COP(=O)(O)O)N[C@@H]2CO)cc1 10.1016/j.bmcl.2006.10.014
16215109 146975 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](COP(=O)(O)O)N[C@@H]2CO)cc1 10.1016/j.bmcl.2011.09.049
44438256 146975 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](COP(=O)(O)O)N[C@@H]2CO)cc1 10.1016/j.bmcl.2011.09.049
CHEMBL393055 146975 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](COP(=O)(O)O)N[C@@H]2CO)cc1 10.1016/j.bmcl.2011.09.049
78321974 139784 0 None -38 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human S1P5 receptor by GTPgammaS binding assayAgonist activity at human S1P5 receptor by GTPgammaS binding assay
ChEMBL 409 9 3 3 4.8 CCCCCC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acsmedchemlett.5b00448
CHEMBL3806205 139784 0 None -38 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human S1P5 receptor by GTPgammaS binding assayAgonist activity at human S1P5 receptor by GTPgammaS binding assay
ChEMBL 409 9 3 3 4.8 CCCCCC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acsmedchemlett.5b00448
78321974 139784 0 None -38 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assayAgonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
ChEMBL 409 9 3 3 4.8 CCCCCC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.8b01695
CHEMBL3806205 139784 0 None -38 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assayAgonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
ChEMBL 409 9 3 3 4.8 CCCCCC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.8b01695
78321974 139784 0 None -38 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 409 9 3 3 4.8 CCCCCC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.0c01109
CHEMBL3806205 139784 0 None -38 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 409 9 3 3 4.8 CCCCCC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.0c01109
66655386 166967 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCCC2(COc3cc(OCc4c(Cl)cccc4Cl)ccc32)C1 10.1016/j.bmcl.2017.12.018
CHEMBL4218296 166967 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCCC2(COc3cc(OCc4c(Cl)cccc4Cl)ccc32)C1 10.1016/j.bmcl.2017.12.018
CHEMBL4300113 166967 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCCC2(COc3cc(OCc4c(Cl)cccc4Cl)ccc32)C1 10.1016/j.bmcl.2017.12.018
66655175 167014 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 367 6 1 4 3.5 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4213649 167014 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 367 6 1 4 3.5 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4300641 167014 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 367 6 1 4 3.5 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
46881912 6688 0 None -2 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 425 13 2 5 2.8 CCCCCCCOc1ccc(CC[C@](C)(N)CCN2CC(=O)NS2(=O)=O)cc1 10.1016/j.bmcl.2010.01.118
CHEMBL1083841 6688 0 None -2 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 425 13 2 5 2.8 CCCCCCCOc1ccc(CC[C@](C)(N)CCN2CC(=O)NS2(=O)=O)cc1 10.1016/j.bmcl.2010.01.118
44412827 77388 0 None -89 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 432 9 1 4 6.9 Cc1cc(CCCCCC(=O)O)ccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL209008 77388 0 None -89 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 432 9 1 4 6.9 Cc1cc(CCCCCC(=O)O)ccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
44517795 67959 0 None -109 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human S1P5 receptor expressed in HEK293 cells after 2 hrs by beta-arrestin assayAgonist activity at recombinant human S1P5 receptor expressed in HEK293 cells after 2 hrs by beta-arrestin assay
ChEMBL 472 6 1 7 3.9 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)CCN4C(=O)CCC(=O)O)no2)c1 10.1016/j.bmcl.2011.05.110
CHEMBL1916399 67959 0 None -109 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human S1P5 receptor expressed in HEK293 cells after 2 hrs by beta-arrestin assayAgonist activity at recombinant human S1P5 receptor expressed in HEK293 cells after 2 hrs by beta-arrestin assay
ChEMBL 472 6 1 7 3.9 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)CCN4C(=O)CCC(=O)O)no2)c1 10.1016/j.bmcl.2011.05.110
42630194 75425 0 None -7 5 Human 8.0 pEC50 = 8.0 Functional
Agonist activity against human S1P5 by beta arrestin recruitment assayAgonist activity against human S1P5 by beta arrestin recruitment assay
ChEMBL 468 5 2 6 5.2 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4[nH]c5c(c4c3)CCC5CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
CHEMBL2048287 75425 0 None -7 5 Human 8.0 pEC50 = 8.0 Functional
Agonist activity against human S1P5 by beta arrestin recruitment assayAgonist activity against human S1P5 by beta arrestin recruitment assay
ChEMBL 468 5 2 6 5.2 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4[nH]c5c(c4c3)CCC5CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
2924 1610 37 None -4 6 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.5b00928
44398069 1610 37 None -4 6 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.5b00928
9908268 1610 37 None -4 6 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.5b00928
CHEMBL114606 1610 37 None -4 6 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.5b00928
25154344 6462 0 None -38 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 515 11 3 7 3.3 Cc1cc(S(=O)(=O)NCCC(=O)O)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
CHEMBL1082869 6462 0 None -38 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 515 11 3 7 3.3 Cc1cc(S(=O)(=O)NCCC(=O)O)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
66655656 166999 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 431 5 1 3 5.4 O=C(O)CCN1CCC2(CC1)COc1cc(/C=C/c3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4218826 166999 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 431 5 1 3 5.4 O=C(O)CCN1CCC2(CC1)COc1cc(/C=C/c3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4300415 166999 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 431 5 1 3 5.4 O=C(O)CCN1CCC2(CC1)COc1cc(/C=C/c3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
66655211 167174 0 None 316 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 451 6 1 4 5.5 O=C(O)CCN1CCC2(CC1)COc1cc(SCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4205124 167174 0 None 316 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 451 6 1 4 5.5 O=C(O)CCN1CCC2(CC1)COc1cc(SCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4302786 167174 0 None 316 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 451 6 1 4 5.5 O=C(O)CCN1CCC2(CC1)COc1cc(SCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
58344592 154029 0 None -100 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N(C)C)no2)cc1C#N nan
CHEMBL3921214 154029 0 None -100 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N(C)C)no2)cc1C#N nan
CHEMBL3991184 154029 0 None -100 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCC(=O)N(C)C)no2)cc1C#N nan
11654374 77979 0 None -660 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 406 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1ncc(-c2ccc(OC(C)C)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
CHEMBL211046 77979 0 None -660 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 406 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1ncc(-c2ccc(OC(C)C)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
10883396 3592 39 None -2 14 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assayAgonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assay
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm100181s
5283560 3592 39 None -2 14 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assayAgonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assay
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm100181s
911 3592 39 None -2 14 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assayAgonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assay
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm100181s
CHEMBL225155 3592 39 None -2 14 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assayAgonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assay
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm100181s
77846594 180920 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 409 6 1 3 5.8 CC[C@H]1CC[C@@H](Oc2cc(C)c3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
CHEMBL4764896 180920 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 409 6 1 3 5.8 CC[C@H]1CC[C@@H](Oc2cc(C)c3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
66655306 167059 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 469 6 1 4 5.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3C(F)(F)F)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4208787 167059 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 469 6 1 4 5.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3C(F)(F)F)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4301342 167059 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 469 6 1 4 5.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3C(F)(F)F)ccc12 10.1016/j.bmcl.2017.12.018
66655521 167164 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 401 6 1 4 4.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3ccccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4204779 167164 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 401 6 1 4 4.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3ccccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4302677 167164 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 401 6 1 4 4.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3ccccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
11689680 79230 0 None -102 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 391 7 1 6 4.4 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.064
CHEMBL211505 79230 0 None -102 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 391 7 1 6 4.4 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.064
44439851 145114 0 None -37 3 Human 7.9 pEC50 = 7.9 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 403 6 1 6 4.6 Cc1cc([C@@H]2C[C@H]2C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.10.057
CHEMBL391581 145114 0 None -37 3 Human 7.9 pEC50 = 7.9 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 403 6 1 6 4.6 Cc1cc([C@@H]2C[C@H]2C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.10.057
46224767 197618 0 None -18 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 293 2 0 4 3.2 Cc1nn(C(=O)/C=C/c2ccncc2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
CHEMBL590383 197618 0 None -18 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 293 2 0 4 3.2 Cc1nn(C(=O)/C=C/c2ccncc2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
44412865 79493 0 None -616 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 417 7 1 6 5.0 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2cnc(OC(C)C)c(Cl)c2)s1 10.1016/j.bmcl.2006.04.064
CHEMBL212420 79493 0 None -616 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 417 7 1 6 5.0 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2cnc(OC(C)C)c(Cl)c2)s1 10.1016/j.bmcl.2006.04.064
44438257 93393 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](CO)N[C@@H]2COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
44438258 93393 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](CO)N[C@@H]2COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
CHEMBL247698 93393 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@H]2C[C@H](CO)N[C@@H]2COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
25110406 1270 47 None -70 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 409 9 2 7 3.8 OCCNC1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)OCC)OCC nan
2928 1270 47 None -70 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 409 9 2 7 3.8 OCCNC1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)OCC)OCC nan
CHEMBL3922179 1270 47 None -70 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 409 9 2 7 3.8 OCCNC1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)OCC)OCC nan
11603726 76477 0 None -588 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 400 7 1 5 5.2 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL206940 76477 0 None -588 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 400 7 1 5 5.2 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.084
25182899 6046 0 None -11 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 350 7 2 5 3.2 CCCN(CC1CC1)c1cc(C(=O)Nc2ccc3[nH]ncc3c2)ncn1 10.1016/j.bmcl.2010.01.102
CHEMBL1080865 6046 0 None -11 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 350 7 2 5 3.2 CCCN(CC1CC1)c1cc(C(=O)Nc2ccc3[nH]ncc3c2)ncn1 10.1016/j.bmcl.2010.01.102
57390239 67566 0 None 1 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 339 3 0 4 3.7 C/N=C1\S/C(=C\c2cc(C)n(Cc3ccccc3)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910687 67566 0 None 1 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 339 3 0 4 3.7 C/N=C1\S/C(=C\c2cc(C)n(Cc3ccccc3)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
42630194 75425 0 None -7 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity against human S1P5 by beta arrestin recruitment assayAgonist activity against human S1P5 by beta arrestin recruitment assay
ChEMBL 468 5 2 6 5.2 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4[nH]c5c(c4c3)CCC5CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
CHEMBL2048287 75425 0 None -7 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity against human S1P5 by beta arrestin recruitment assayAgonist activity against human S1P5 by beta arrestin recruitment assay
ChEMBL 468 5 2 6 5.2 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4[nH]c5c(c4c3)CCC5CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
44412936 138237 0 None -213 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 405 8 1 6 4.8 CC[C@H](C)Oc1ccc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)cc1C#N 10.1016/j.bmcl.2006.04.084
CHEMBL378054 138237 0 None -213 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 405 8 1 6 4.8 CC[C@H](C)Oc1ccc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)cc1C#N 10.1016/j.bmcl.2006.04.084
58344526 149595 2 None -95 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 404 7 2 7 3.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCCO)no2)cc1C#N nan
CHEMBL3951270 149595 2 None -95 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 404 7 2 7 3.6 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NCCO)no2)cc1C#N nan
58344520 146043 0 None -169 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCC(=O)N(C)C)no2)cc1C#N nan
CHEMBL3922998 146043 0 None -169 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 445 7 1 7 3.7 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCC(=O)N(C)C)no2)cc1C#N nan
66655198 163108 0 None 79 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 449 7 1 4 5.2 O=C(O)CCCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4204437 163108 0 None 79 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 449 7 1 4 5.2 O=C(O)CCCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
66655680 167046 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 429 7 1 4 4.7 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4210234 167046 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 429 7 1 4 4.7 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4301008 167046 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 429 7 1 4 4.7 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
145947403 167107 0 None 125 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 8 1 4 5.1 CCCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4205878 167107 0 None 125 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 8 1 4 5.1 CCCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4301965 167107 0 None 125 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 8 1 4 5.1 CCCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
56601980 167125 0 None 19 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 7 1 4 4.9 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CC(C)C(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4205225 167125 0 None 19 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 7 1 4 4.9 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CC(C)C(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4302166 167125 0 None 19 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 7 1 4 4.9 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CC(C)C(=O)O)CC1 10.1016/j.bmcl.2017.12.018
11603528 139528 0 None -154 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 391 7 1 7 3.3 Cc1cc(CCC(=O)O)ccc1-n1nnc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.064
CHEMBL380040 139528 0 None -154 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 391 7 1 7 3.3 Cc1cc(CCC(=O)O)ccc1-n1nnc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.064
77846593 181927 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 457 6 1 3 6.6 Cc1cc(O[C@H]2CC[C@@H](c3ccccc3)CC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4787014 181927 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 457 6 1 3 6.6 Cc1cc(O[C@H]2CC[C@@H](c3ccccc3)CC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
66655846 167192 0 None 39 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4215002 167192 0 None 39 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4303021 167192 0 None 39 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
49848557 1080 0 None -6 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells by aequorin calcium accumulation assayAgonist activity at human S1P5 receptor expressed in CHO-K1 cells by aequorin calcium accumulation assay
ChEMBL 461 7 1 8 4.0 OC(=O)CCN1CCc2c(C1)c(C)n(n2)c1nnc(s1)c1ccc(c(c1)Cl)OC(C)C 10.1021/acs.jmedchem.5b01512
9492 1080 0 None -6 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells by aequorin calcium accumulation assayAgonist activity at human S1P5 receptor expressed in CHO-K1 cells by aequorin calcium accumulation assay
ChEMBL 461 7 1 8 4.0 OC(=O)CCN1CCc2c(C1)c(C)n(n2)c1nnc(s1)c1ccc(c(c1)Cl)OC(C)C 10.1021/acs.jmedchem.5b01512
CHEMBL3769933 1080 0 None -6 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 cells by aequorin calcium accumulation assayAgonist activity at human S1P5 receptor expressed in CHO-K1 cells by aequorin calcium accumulation assay
ChEMBL 461 7 1 8 4.0 OC(=O)CCN1CCc2c(C1)c(C)n(n2)c1nnc(s1)c1ccc(c(c1)Cl)OC(C)C 10.1021/acs.jmedchem.5b01512
44125170 65624 1 None -16 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazineAgonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine
ChEMBL 446 7 1 7 4.2 Cc1c(-c2noc(-c3ccc(OC(C)C)c(C#N)c3)n2)ccc2c1CCN(CCC(=O)O)C2 10.1021/jm200609t
CHEMBL1836169 65624 1 None -16 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazineAgonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine
ChEMBL 446 7 1 7 4.2 Cc1c(-c2noc(-c3ccc(OC(C)C)c(C#N)c3)n2)ccc2c1CCN(CCC(=O)O)C2 10.1021/jm200609t
77846674 180378 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 549 5 1 3 6.7 CC(C)(C)[C@H]1CC[C@H](Oc2cc(I)c3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
CHEMBL4758438 180378 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 549 5 1 3 6.7 CC(C)(C)[C@H]1CC[C@H](Oc2cc(I)c3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
11977938 70566 24 None -11 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptorAgonist activity at human S1P5 receptor
ChEMBL 461 8 1 7 5.3 CCc1cc(CN2CC(C(=O)O)C2)sc1-c1noc(-c2ccc(Oc3ccccc3)cc2)n1 10.1016/j.ejmech.2012.02.022
CHEMBL1951304 70566 24 None -11 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human S1P5 receptorAgonist activity at human S1P5 receptor
ChEMBL 461 8 1 7 5.3 CCc1cc(CN2CC(C(=O)O)C2)sc1-c1noc(-c2ccc(Oc3ccccc3)cc2)n1 10.1016/j.ejmech.2012.02.022
9969355 58133 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as intracellular calcium levelsAgonist activity at human S1P5 receptor expressed in CHO cells assessed as intracellular calcium levels
ChEMBL 369 14 2 3 4.5 O=C(O)CCNCCCc1ccc(OCCCCCc2ccccc2)cc1 10.1016/j.bmcl.2011.01.029
CHEMBL1683041 58133 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as intracellular calcium levelsAgonist activity at human S1P5 receptor expressed in CHO cells assessed as intracellular calcium levels
ChEMBL 369 14 2 3 4.5 O=C(O)CCNCCCc1ccc(OCCCCCc2ccccc2)cc1 10.1016/j.bmcl.2011.01.029
52938055 147082 0 None -478 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 482 9 1 8 3.6 COCCS(=O)(=O)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3931243 147082 0 None -478 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 482 9 1 8 3.6 COCCS(=O)(=O)N[C@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
11869937 197478 8 None -75 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 292 2 0 3 3.8 Cc1nn(C(=O)/C=C/c2ccccc2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
CHEMBL589402 197478 8 None -75 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 292 2 0 3 3.8 Cc1nn(C(=O)/C=C/c2ccccc2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
44422604 85023 0 None -9 5 Human 7.7 pEC50 = 7.7 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 432 15 4 4 4.4 CCCCCCCCCCc1ccc(NC(=O)[C@H](N)CC(F)OP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
CHEMBL226612 85023 0 None -9 5 Human 7.7 pEC50 = 7.7 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 432 15 4 4 4.4 CCCCCCCCCCc1ccc(NC(=O)[C@H](N)CC(F)OP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
46881875 7249 0 None -1 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 371 13 3 3 4.3 CCCCCCCOc1ccc(CC[C@](C)(N)CCP(=O)(O)O)cc1 10.1016/j.bmcl.2010.01.118
CHEMBL1086170 7249 0 None -1 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 371 13 3 3 4.3 CCCCCCCOc1ccc(CC[C@](C)(N)CCP(=O)(O)O)cc1 10.1016/j.bmcl.2010.01.118
66655362 163067 0 None 79 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 423 8 1 4 4.6 CCc1cccc(CC)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4203755 163067 0 None 79 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 423 8 1 4 4.6 CCc1cccc(CC)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
66654900 167029 0 None 199 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 485 7 1 5 5.0 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3OC(F)(F)F)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4217573 167029 0 None 199 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 485 7 1 5 5.0 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3OC(F)(F)F)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4300821 167029 0 None 199 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 485 7 1 5 5.0 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3OC(F)(F)F)ccc12 10.1016/j.bmcl.2017.12.018
56599785 167099 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 487 7 2 5 4.4 O=P(O)(O)OCCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4205748 167099 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 487 7 2 5 4.4 O=P(O)(O)OCCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4301854 167099 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 487 7 2 5 4.4 O=P(O)(O)OCCN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
53492750 65635 0 None -6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazineAgonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine
ChEMBL 448 7 2 8 3.1 Cc1c(-c2noc(-c3ccc(OC(C)C)c(C#N)c3)n2)ccc2c1CCN(C(CO)CO)C2 10.1021/jm200609t
CHEMBL1836215 65635 0 None -6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazineAgonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine
ChEMBL 448 7 2 8 3.1 Cc1c(-c2noc(-c3ccc(OC(C)C)c(C#N)c3)n2)ccc2c1CCN(C(CO)CO)C2 10.1021/jm200609t
25182769 6188 0 None -7 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 380 6 2 5 4.3 Cc1cc(O)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
CHEMBL1081645 6188 0 None -7 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 380 6 2 5 4.3 Cc1cc(O)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
57390243 67580 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 383 6 0 5 3.7 COCC/N=C1\S/C(=C\c2cc(C)n(Cc3ccccc3)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910802 67580 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 383 6 0 5 3.7 COCC/N=C1\S/C(=C\c2cc(C)n(Cc3ccccc3)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
11222939 67233 6 None -9 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2010.02.006
44438254 67233 6 None -9 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2010.02.006
CHEMBL190006 67233 6 None -9 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2010.02.006
66655583 167015 0 None 7 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cccc(Cl)c3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4210576 167015 0 None 7 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cccc(Cl)c3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4300642 167015 0 None 7 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cccc(Cl)c3Cl)ccc12 10.1016/j.bmcl.2017.12.018
66655587 167075 0 None 5 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cc(Cl)ccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4205714 167075 0 None 5 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cc(Cl)ccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4301563 167075 0 None 5 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 435 6 1 4 4.8 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cc(Cl)ccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
68082485 166959 0 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 395 8 1 4 3.9 O=C(O)CCN1CCC2(CC1)COc1cc(OCCCc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4207162 166959 0 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 395 8 1 4 3.9 O=C(O)CCN1CCC2(CC1)COc1cc(OCCCc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4300006 166959 0 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 395 8 1 4 3.9 O=C(O)CCN1CCC2(CC1)COc1cc(OCCCc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
59384375 103911 0 None -4 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
ChEMBL 510 13 3 6 5.9 CCCCCCCCOc1ccc(-c2cnc([C@@](C)(N)COP(=O)(O)O)s2)cc1C(F)(F)F 10.1021/ml400194r
CHEMBL3102903 103911 0 None -4 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation countingAgonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
ChEMBL 510 13 3 6 5.9 CCCCCCCCOc1ccc(-c2cnc([C@@](C)(N)COP(=O)(O)O)s2)cc1C(F)(F)F 10.1021/ml400194r
46881847 6980 0 None -2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 373 13 3 4 3.8 CCCCCCCOc1ccc(CC[C@](C)(N)COP(=O)(O)O)cc1 10.1016/j.bmcl.2010.01.118
CHEMBL1084929 6980 0 None -2 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 373 13 3 4 3.8 CCCCCCCOc1ccc(CC[C@](C)(N)COP(=O)(O)O)cc1 10.1016/j.bmcl.2010.01.118
77847681 182708 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 409 5 1 3 5.6 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CN2CC(C(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4796939 182708 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 409 5 1 3 5.6 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CN2CC(C(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
66655236 167126 0 None 50 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 445 7 1 4 5.4 CCc1cccc(Cl)c1CSc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4210019 167126 0 None 50 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 445 7 1 4 5.4 CCc1cccc(Cl)c1CSc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4302167 167126 0 None 50 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 445 7 1 4 5.4 CCc1cccc(Cl)c1CSc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
11222939 67233 6 None -9 4 Human 8.5 pEC50 = 8.5 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
44438254 67233 6 None -9 4 Human 8.5 pEC50 = 8.5 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
CHEMBL190006 67233 6 None -9 4 Human 8.5 pEC50 = 8.5 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(CC[C@@](N)(CO)COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
58344778 154000 0 None -117 5 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 360 4 1 6 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N)no2)cc1C#N nan
CHEMBL3902160 154000 0 None -117 5 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 360 4 1 6 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N)no2)cc1C#N nan
CHEMBL3990889 154000 0 None -117 5 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 360 4 1 6 4.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4N)no2)cc1C#N nan
44412661 139013 0 None -14 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 406 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1cnc(-c2ccc(OC(C)C)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
CHEMBL379612 139013 0 None -14 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 406 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1cnc(-c2ccc(OC(C)C)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
46866185 7251 0 None -10 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 321 12 2 3 4.2 CCCCCCCOc1ccc(CC[C@](C)(N)CC(=O)O)cc1 10.1016/j.bmcl.2010.01.118
CHEMBL1086172 7251 0 None -10 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 321 12 2 3 4.2 CCCCCCCOc1ccc(CC[C@](C)(N)CC(=O)O)cc1 10.1016/j.bmcl.2010.01.118
44138103 75431 0 None -131 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against human S1P5 by beta arrestin recruitment assayAgonist activity against human S1P5 by beta arrestin recruitment assay
ChEMBL 468 5 1 7 5.1 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)cc3n4CCC3CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
CHEMBL2048293 75431 0 None -131 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against human S1P5 by beta arrestin recruitment assayAgonist activity against human S1P5 by beta arrestin recruitment assay
ChEMBL 468 5 1 7 5.1 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)cc3n4CCC3CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
11676168 70606 9 None -19 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5RAgonist activity at human S1P5R
ChEMBL 422 11 3 5 3.3 Cc1ccc(CCCC(=O)c2ccc(CC[C@@](C)(N)COP(=O)(O)O)n2C)cc1 10.1021/ml100301k
CHEMBL1951588 70606 9 None -19 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human S1P5RAgonist activity at human S1P5R
ChEMBL 422 11 3 5 3.3 Cc1ccc(CCCC(=O)c2ccc(CC[C@@](C)(N)COP(=O)(O)O)n2C)cc1 10.1021/ml100301k
44438261 93427 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@@H]2C[C@@H](CO)N[C@H]2COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
44438262 93427 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@@H]2C[C@@H](CO)N[C@H]2COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
CHEMBL247901 93427 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@@H]2C[C@@H](CO)N[C@H]2COP(=O)(O)O)cc1 10.1016/j.bmcl.2006.10.014
11646599 77313 0 None -1047 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 380 7 1 5 4.8 Cc1cc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)ccc1OC(C)C 10.1016/j.bmcl.2006.04.084
CHEMBL208898 77313 0 None -1047 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 380 7 1 5 4.8 Cc1cc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)ccc1OC(C)C 10.1016/j.bmcl.2006.04.084
10311 1267 34 None -37 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 405 5 0 5 3.9 COCCN=C1S/C(=C\c2cc(n(c2C)c2ccc(cc2F)F)C)/C(=O)N1C 10.1016/j.bmcl.2011.09.049
49835928 1267 34 None -37 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 405 5 0 5 3.9 COCCN=C1S/C(=C\c2cc(n(c2C)c2ccc(cc2F)F)C)/C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910803 1267 34 None -37 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 405 5 0 5 3.9 COCCN=C1S/C(=C\c2cc(n(c2C)c2ccc(cc2F)F)C)/C(=O)N1C 10.1016/j.bmcl.2011.09.049
57397321 67569 0 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 403 5 0 4 4.7 CC/N=C1\S/C(=C\c2cc(C)n(Cc3c(F)cccc3F)c2C)C(=O)N1CC 10.1016/j.bmcl.2011.09.049
CHEMBL1910690 67569 0 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 403 5 0 4 4.7 CC/N=C1\S/C(=C\c2cc(C)n(Cc3c(F)cccc3F)c2C)C(=O)N1CC 10.1016/j.bmcl.2011.09.049
11632823 137843 0 None -234 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 405 7 1 4 6.1 Cc1cc(CCC(=O)O)ccc1-c1ccc(-c2ccc(OC(C)C)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
CHEMBL377181 137843 0 None -234 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 405 7 1 4 6.1 Cc1cc(CCC(=O)O)ccc1-c1ccc(-c2ccc(OC(C)C)c(C#N)c2)s1 10.1016/j.bmcl.2006.04.064
77846755 181300 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 381 5 1 3 5.2 Cc1cc(OC2CCCCC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4778961 181300 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 381 5 1 3 5.2 Cc1cc(OC2CCCCC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
49835989 67562 1 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 353 4 0 4 4.4 CC/N=C1\S/C(=C\c2cc(C)n(-c3ccccc3)c2C)C(=O)N1CC 10.1016/j.bmcl.2011.09.049
CHEMBL1910681 67562 1 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 353 4 0 4 4.4 CC/N=C1\S/C(=C\c2cc(C)n(-c3ccccc3)c2C)C(=O)N1CC 10.1016/j.bmcl.2011.09.049
11626664 77575 0 None -239 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 455 7 1 6 5.1 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2cnc(OC(C)C(F)(F)F)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL209484 77575 0 None -239 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 455 7 1 6 5.1 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2cnc(OC(C)C(F)(F)F)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.084
11177439 67550 0 None -239 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 413 7 4 3 3.6 N[C@H](CNC(=O)c1cc2c(-c3ccccc3Cc3ccccc3)cccc2[nH]1)C(=O)O 10.1016/j.bmcl.2011.09.049
CHEMBL1910654 67550 0 None -239 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 413 7 4 3 3.6 N[C@H](CNC(=O)c1cc2c(-c3ccccc3Cc3ccccc3)cccc2[nH]1)C(=O)O 10.1016/j.bmcl.2011.09.049
66655406 166988 0 None 50 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 7 1 4 5.2 CC(C)c1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4205333 166988 0 None 50 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 7 1 4 5.2 CC(C)c1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
CHEMBL4300295 166988 0 None 50 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 443 7 1 4 5.2 CC(C)c1cccc(Cl)c1COc1ccc2c(c1)OCC21CCN(CCC(=O)O)CC1 10.1016/j.bmcl.2017.12.018
66655633 167038 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 395 3 1 3 3.9 O=C(O)CCN1CCC2(CC1)COc1cc(C#Cc3ccccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4213894 167038 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 395 3 1 3 3.9 O=C(O)CCN1CCC2(CC1)COc1cc(C#Cc3ccccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4300915 167038 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 395 3 1 3 3.9 O=C(O)CCN1CCC2(CC1)COc1cc(C#Cc3ccccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
25182621 6193 0 None 4 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 326 4 3 5 3.5 Cc1cc(O)ccc1NC(=O)c1cc(NC2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
CHEMBL1081654 6193 0 None 4 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 326 4 3 5 3.5 Cc1cc(O)ccc1NC(=O)c1cc(NC2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
44412867 79332 0 None -660 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 420 7 1 5 5.1 CCOc1ccc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)cc1C(F)(F)F 10.1016/j.bmcl.2006.04.084
CHEMBL211689 79332 0 None -660 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 420 7 1 5 5.1 CCOc1ccc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)cc1C(F)(F)F 10.1016/j.bmcl.2006.04.084
44412868 79354 0 None -812 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 406 6 1 5 4.8 COc1ccc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)cc1C(F)(F)F 10.1016/j.bmcl.2006.04.084
CHEMBL211806 79354 0 None -812 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 406 6 1 5 4.8 COc1ccc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)cc1C(F)(F)F 10.1016/j.bmcl.2006.04.084
44412908 77230 0 None -109 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 318 3 0 3 5.8 Cc1ccccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL208786 77230 0 None -109 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 318 3 0 3 5.8 Cc1ccccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
76955634 182862 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 383 6 2 3 5.3 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNCC(=O)O)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4798888 182862 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 383 6 2 3 5.3 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNCC(=O)O)c2ccccc12 10.1021/acsmedchemlett.0c00631
11682696 79535 0 None -245 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 396 8 1 6 4.5 COc1cc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)ccc1OC(C)C 10.1016/j.bmcl.2006.04.084
CHEMBL212580 79535 0 None -245 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 396 8 1 6 4.5 COc1cc(-c2nc(-c3ccc(CCC(=O)O)cc3C)no2)ccc1OC(C)C 10.1016/j.bmcl.2006.04.084
69263869 104230 0 None -63 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P5 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
ChEMBL 436 6 1 5 6.0 CCc1cc(-c2noc(-c3sc(C)c4c3C[C@@H]3[C@H]4C3(C)C)n2)cc(C)c1CCC(=O)O 10.1021/jm4014373
CHEMBL3105479 104230 0 None -63 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysisAgonist activity at human recombinant S1P5 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 1 hr by topcount scintillation counting analysis
ChEMBL 436 6 1 5 6.0 CCc1cc(-c2noc(-c3sc(C)c4c3C[C@@H]3[C@H]4C3(C)C)n2)cc(C)c1CCC(=O)O 10.1021/jm4014373
24825339 91334 0 None -66 3 Human 7.5 pEC50 = 7.5 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 392 7 1 7 3.8 Cc1nc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.10.057
CHEMBL241052 91334 0 None -66 3 Human 7.5 pEC50 = 7.5 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 392 7 1 7 3.8 Cc1nc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.10.057
46866186 7250 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 307 11 2 3 3.8 CCCCCCCOc1ccc(CC[C@](C)(N)C(=O)O)cc1 10.1016/j.bmcl.2010.01.118
CHEMBL1086171 7250 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 307 11 2 3 3.8 CCCCCCCOc1ccc(CC[C@](C)(N)C(=O)O)cc1 10.1016/j.bmcl.2010.01.118
44138103 75431 0 None -131 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human S1P5 by beta arrestin recruitment assayAgonist activity against human S1P5 by beta arrestin recruitment assay
ChEMBL 468 5 1 7 5.1 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)cc3n4CCC3CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
CHEMBL2048293 75431 0 None -131 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human S1P5 by beta arrestin recruitment assayAgonist activity against human S1P5 by beta arrestin recruitment assay
ChEMBL 468 5 1 7 5.1 N#Cc1cc(OC(F)(F)F)cc(-c2nc(-c3ccc4c(c3)cc3n4CCC3CC(=O)O)no2)c1 10.1016/j.bmcl.2012.04.129
44600476 57102 6 None -14 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5R expressed in CHO cells by Ca(2+) mobilization assayAgonist activity at human S1P5R expressed in CHO cells by Ca(2+) mobilization assay
ChEMBL 459 6 1 5 5.1 O=C(O)C1CN(Cc2ccc(-c3nc4ccc(C5(c6ccccc6)CC5)nc4s3)c(F)c2)C1 10.1021/ml100306h
CHEMBL1651861 57102 6 None -14 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5R expressed in CHO cells by Ca(2+) mobilization assayAgonist activity at human S1P5R expressed in CHO cells by Ca(2+) mobilization assay
ChEMBL 459 6 1 5 5.1 O=C(O)C1CN(Cc2ccc(-c3nc4ccc(C5(c6ccccc6)CC5)nc4s3)c(F)c2)C1 10.1021/ml100306h
44412971 138405 0 None -102 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 445 7 1 6 4.9 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C(F)(F)F)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL378436 138405 0 None -102 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 445 7 1 6 4.9 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C(F)(F)F)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.084
2924 1610 37 None -4 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.5b00928
44398069 1610 37 None -4 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.5b00928
9908268 1610 37 None -4 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.5b00928
CHEMBL114606 1610 37 None -4 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/acs.jmedchem.5b00928
118877433 176766 0 None -14 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assayAgonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
ChEMBL 459 8 3 4 4.5 COc1ccccc1CC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.8b01695
CHEMBL4637401 176766 0 None -14 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assayAgonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay
ChEMBL 459 8 3 4 4.5 COc1ccccc1CC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.8b01695
118877603 179848 0 None -4 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 425 10 3 4 4.1 COCCCCC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.0c01109
CHEMBL4752394 179848 0 None -4 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 425 10 3 4 4.1 COCCCCC[C@@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.0c01109
77846507 179187 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 437 6 1 3 6.4 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CN2CCC(CC(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4744455 179187 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 437 6 1 3 6.4 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CN2CCC(CC(=O)O)C2)c2ccccc12 10.1021/acsmedchemlett.0c00631
11496072 145491 0 None -32 3 Human 8.4 pEC50 = 8.4 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 448 7 1 5 6.1 Cc1cc(C(C)CC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2006.10.057
CHEMBL391869 145491 0 None -32 3 Human 8.4 pEC50 = 8.4 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 448 7 1 5 6.1 Cc1cc(C(C)CC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2006.10.057
44422601 85155 0 None -8 5 Human 7.5 pEC50 = 7.5 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 398 14 4 3 4.2 CCCCCCCCCCc1ccc(NC(=O)[C@H](N)CCP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
CHEMBL228139 85155 0 None -8 5 Human 7.5 pEC50 = 7.5 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 398 14 4 3 4.2 CCCCCCCCCCc1ccc(NC(=O)[C@H](N)CCP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
44422605 85149 0 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 329 11 3 3 3.1 CCCCCCc1ccc(OC[C@@H](N)CCP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
CHEMBL228103 85149 0 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 329 11 3 3 3.1 CCCCCCc1ccc(OC[C@@H](N)CCP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
66655585 166955 0 None 199 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 421 5 1 4 4.4 O=C(O)CN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4209307 166955 0 None 199 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 421 5 1 4 4.4 O=C(O)CN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4299904 166955 0 None 199 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 421 5 1 4 4.4 O=C(O)CN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
66655579 166992 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 429 7 1 4 4.7 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCCN(CCC(=O)O)C1 10.1016/j.bmcl.2017.12.018
CHEMBL4206573 166992 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 429 7 1 4 4.7 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCCN(CCC(=O)O)C1 10.1016/j.bmcl.2017.12.018
CHEMBL4300331 166992 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 429 7 1 4 4.7 CCc1cccc(Cl)c1COc1ccc2c(c1)OCC21CCCN(CCC(=O)O)C1 10.1016/j.bmcl.2017.12.018
145947321 167105 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 436 6 1 5 4.2 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cc(Cl)nc(Cl)c3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4218094 167105 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 436 6 1 5 4.2 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cc(Cl)nc(Cl)c3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4301951 167105 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 436 6 1 5 4.2 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cc(Cl)nc(Cl)c3)ccc12 10.1016/j.bmcl.2017.12.018
66655208 167122 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 401 6 1 4 4.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cccc(Cl)c3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4210080 167122 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 401 6 1 4 4.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cccc(Cl)c3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4302153 167122 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 401 6 1 4 4.1 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3cccc(Cl)c3)ccc12 10.1016/j.bmcl.2017.12.018
107970 1609 76 None -77 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2017.12.018
2407 1609 76 None -77 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2017.12.018
4167 1609 76 None -77 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2017.12.018
CHEMBL314854 1609 76 None -77 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2017.12.018
DB08868 1609 76 None -77 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2017.12.018
67194420 142480 0 None -645 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 468 8 2 8 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCO)no2)cc1C#N nan
CHEMBL3894716 142480 0 None -645 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 468 8 2 8 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NS(=O)(=O)CCO)no2)cc1C#N nan
25192001 7976 0 None -2 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay
ChEMBL 413 12 4 4 3.5 CCCCCCCCc1ccc2c(c1)CC[C@@H](C(N)(CO)COP(=O)(O)O)C2 10.1016/j.bmcl.2010.02.006
CHEMBL1091103 7976 0 None -2 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assayAgonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay
ChEMBL 413 12 4 4 3.5 CCCCCCCCc1ccc2c(c1)CC[C@@H](C(N)(CO)COP(=O)(O)O)C2 10.1016/j.bmcl.2010.02.006
44412604 137878 0 None -10 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 405 7 1 4 6.1 Cc1cc(CCC(=O)O)ccc1-c1cc(-c2ccc(OC(C)C)c(C#N)c2)cs1 10.1016/j.bmcl.2006.04.064
CHEMBL377339 137878 0 None -10 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 405 7 1 4 6.1 Cc1cc(CCC(=O)O)ccc1-c1cc(-c2ccc(OC(C)C)c(C#N)c2)cs1 10.1016/j.bmcl.2006.04.064
44412605 139024 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 405 7 1 4 6.1 Cc1cc(CCC(=O)O)ccc1-c1csc(-c2ccc(OC(C)C)c(C#N)c2)c1 10.1016/j.bmcl.2006.04.064
CHEMBL379660 139024 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 405 7 1 4 6.1 Cc1cc(CCC(=O)O)ccc1-c1csc(-c2ccc(OC(C)C)c(C#N)c2)c1 10.1016/j.bmcl.2006.04.064
46224714 197577 0 None -12 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 360 2 0 3 4.9 Cc1nn(C(=O)/C=C/c2cccc(C(F)(F)F)c2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
CHEMBL590134 197577 0 None -12 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 360 2 0 3 4.9 Cc1nn(C(=O)/C=C/c2cccc(C(F)(F)F)c2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
11545181 3952 4 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 370 12 4 3 3.4 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](CCP(=O)(O)O)N 10.1016/j.bmc.2006.10.060
2930 3952 4 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 370 12 4 3 3.4 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](CCP(=O)(O)O)N 10.1016/j.bmc.2006.10.060
CHEMBL389033 3952 4 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 370 12 4 3 3.4 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](CCP(=O)(O)O)N 10.1016/j.bmc.2006.10.060
90660718 59669 0 None -3 3 Human 6.5 pEC50 = 6.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 5 (S1P5) counterscreen assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1509, AID1523, AID1563, AID1686, AID1701, AID1801, AID463107, AID463225, AID504400]PUBCHEM_BIOASSAY: Late-stage fluorescence-based dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 5 (S1P5) counterscreen assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1509, AID1523, AID1563, AID1686, AID1701, AID1801, AID463107, AID463225, AID504400]
ChEMBL 391 4 0 5 3.9 C/N=C1\S/C(=C/c2cc(C)n(Cc3c(F)cccc3F)c2C)C(=O)N1OC nan
CHEMBL1734070 59669 0 None -3 3 Human 6.5 pEC50 = 6.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 5 (S1P5) counterscreen assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1509, AID1523, AID1563, AID1686, AID1701, AID1801, AID463107, AID463225, AID504400]PUBCHEM_BIOASSAY: Late-stage fluorescence-based dose-response cell-based assay to identify agonists of the Sphingosine 1-Phosphate Receptor 4 (S1P4): Sphingosine 1-Phosphate Receptor 5 (S1P5) counterscreen assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1509, AID1523, AID1563, AID1686, AID1701, AID1801, AID463107, AID463225, AID504400]
ChEMBL 391 4 0 5 3.9 C/N=C1\S/C(=C/c2cc(C)n(Cc3c(F)cccc3F)c2C)C(=O)N1OC nan
57400714 67568 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 375 3 0 4 4.0 C/N=C1\S/C(=C\c2cc(C)n(Cc3c(F)cccc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910689 67568 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 375 3 0 4 4.0 C/N=C1\S/C(=C\c2cc(C)n(Cc3c(F)cccc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
57390238 67561 0 None -7 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 377 2 0 4 4.4 C/N=C1\S/C(=C\c2cc(C)n(-c3ccc(Cl)cc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910680 67561 0 None -7 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 377 2 0 4 4.4 C/N=C1\S/C(=C\c2cc(C)n(-c3ccc(Cl)cc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
46224768 197619 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 293 2 0 4 3.2 Cc1nn(C(=O)/C=C/c2cccnc2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
CHEMBL590384 197619 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 293 2 0 4 3.2 Cc1nn(C(=O)/C=C/c2cccnc2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
77846675 178835 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 457 5 1 3 6.8 CC(C)(C)[C@H]1CC[C@H](Oc2cc(Cl)c3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
CHEMBL4740175 178835 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 457 5 1 3 6.8 CC(C)(C)[C@H]1CC[C@H](Oc2cc(Cl)c3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
46881877 7026 0 None -5 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 359 13 2 5 3.8 CCCCCCCOc1ccc(CC[C@](C)(N)CCc2nnn[nH]2)cc1 10.1016/j.bmcl.2010.01.118
CHEMBL1085191 7026 0 None -5 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS bindingAgonist activity at human S1P5 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding
ChEMBL 359 13 2 5 3.8 CCCCCCCOc1ccc(CC[C@](C)(N)CCc2nnn[nH]2)cc1 10.1016/j.bmcl.2010.01.118
57398998 67570 0 None 3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 375 3 0 4 4.0 C/N=C1\S/C(=C\c2cc(C)n(Cc3ccc(F)cc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910691 67570 0 None 3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 375 3 0 4 4.0 C/N=C1\S/C(=C\c2cc(C)n(Cc3ccc(F)cc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
44439852 93413 0 None -47 2 Human 7.4 pEC50 = 7.4 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 403 6 1 6 4.6 Cc1cc([C@H]2C[C@H]2C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.10.057
CHEMBL247766 93413 0 None -47 2 Human 7.4 pEC50 = 7.4 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 403 6 1 6 4.6 Cc1cc([C@H]2C[C@H]2C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.10.057
77847766 180931 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 451 5 1 3 6.8 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CN2CCC(C)(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4765011 180931 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 451 5 1 3 6.8 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CN2CCC(C)(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
58344502 142313 0 None -398 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 459 5 2 7 3.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CC(O)C3)no2)cc1C#N nan
CHEMBL3893172 142313 0 None -398 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 459 5 2 7 3.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NC(=O)N3CC(O)C3)no2)cc1C#N nan
66655999 167093 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 361 3 1 3 3.3 O=C(O)CCN1CCC2(CC1)COc1cc(C#Cc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4208055 167093 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 361 3 1 3 3.3 O=C(O)CCN1CCC2(CC1)COc1cc(C#Cc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4301752 167093 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 361 3 1 3 3.3 O=C(O)CCN1CCC2(CC1)COc1cc(C#Cc3ccccc3)ccc12 10.1016/j.bmcl.2017.12.018
2924 1610 37 None -4 6 Human 8.4 pEC50 = 8.4 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1016/j.bmc.2006.10.060
44398069 1610 37 None -4 6 Human 8.4 pEC50 = 8.4 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1016/j.bmc.2006.10.060
9908268 1610 37 None -4 6 Human 8.4 pEC50 = 8.4 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1016/j.bmc.2006.10.060
CHEMBL114606 1610 37 None -4 6 Human 8.4 pEC50 = 8.4 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1016/j.bmc.2006.10.060
46872626 213 18 None 72 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
9496 213 18 None 72 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
CHEMBL3741589 213 18 None 72 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
52938427 2936 47 None -33 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting methodAgonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting method
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.1016/j.bmcl.2019.06.042
5383 2936 47 None -33 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting methodAgonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting method
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.1016/j.bmcl.2019.06.042
8709 2936 47 None -33 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting methodAgonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting method
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.1016/j.bmcl.2019.06.042
CHEMBL3707247 2936 47 None -33 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting methodAgonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting method
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.1016/j.bmcl.2019.06.042
DB12612 2936 47 None -33 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting methodAgonist activity at S1P5 (unknown origin) assessed as stimulation of [35S]GTPgammaS binding incubated for 120 mins in presence of GDP by TopCount scintillation counting method
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 10.1016/j.bmcl.2019.06.042
2924 1610 37 None -4 6 Human 8.3 pEC50 = 8.3 Functional
Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligandAgonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/jm050242f
44398069 1610 37 None -4 6 Human 8.3 pEC50 = 8.3 Functional
Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligandAgonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/jm050242f
9908268 1610 37 None -4 6 Human 8.3 pEC50 = 8.3 Functional
Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligandAgonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/jm050242f
CHEMBL114606 1610 37 None -4 6 Human 8.3 pEC50 = 8.3 Functional
Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligandAgonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/jm050242f
118877584 181871 0 None -7 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 411 9 3 4 3.7 CCOCCC[C@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.0c01109
CHEMBL4786296 181871 0 None -7 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting methodAgonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method
ChEMBL 411 9 3 4 3.7 CCOCCC[C@H]1CCc2cc([C@H]3CC[C@](N)(COP(=O)(O)O)C3)ccc2C1 10.1021/acs.jmedchem.0c01109
24825338 77357 0 None -467 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 434 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL208924 77357 0 None -467 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 434 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2006.04.084
24825338 77357 0 None -467 3 Human 7.4 pEC50 = 7.4 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 434 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2006.10.057
CHEMBL208924 77357 0 None -467 3 Human 7.4 pEC50 = 7.4 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 434 7 1 5 5.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2006.10.057
44412854 165378 0 None -4 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 376 5 1 4 5.4 Cc1cc(CC(=O)O)ccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL425058 165378 0 None -4 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 376 5 1 4 5.4 Cc1cc(CC(=O)O)ccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
90318298 179001 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 371 13 2 3 5.5 CCCCCCCCOc1cc(C)c2ccccc2c1CNCCC(=O)O 10.1021/acsmedchemlett.0c00631
CHEMBL4742052 179001 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 371 13 2 3 5.5 CCCCCCCCOc1cc(C)c2ccccc2c1CNCCC(=O)O 10.1021/acsmedchemlett.0c00631
44422579 85154 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 356 13 4 3 3.9 CCCCCCCCc1cccc(NC[C@H](N)CCP(=O)(O)O)c1 10.1016/j.bmc.2006.10.060
CHEMBL228138 85154 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 356 13 4 3 3.9 CCCCCCCCc1cccc(NC[C@H](N)CCP(=O)(O)O)c1 10.1016/j.bmc.2006.10.060
44412578 77778 0 None -26 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 391 7 1 7 3.3 Cc1cc(CCC(=O)O)ccc1-c1nnn(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.064
CHEMBL210345 77778 0 None -26 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 391 7 1 7 3.3 Cc1cc(CCC(=O)O)ccc1-c1nnn(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.064
11575913 77768 0 None 5 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 444 7 1 5 5.3 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(Br)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL210316 77768 0 None 5 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 444 7 1 5 5.3 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(Br)c2)n1 10.1016/j.bmcl.2006.04.084
54764919 69558 36 None -123 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human S1P5 expressed in CHO-K1 cells coexpressing Gq/i5 assessed as calcium mobilization-induced bioluminescence change measured for 90 secs by fluorimetryAgonist activity at human S1P5 expressed in CHO-K1 cells coexpressing Gq/i5 assessed as calcium mobilization-induced bioluminescence change measured for 90 secs by fluorimetry
ChEMBL 415 4 2 4 4.7 COc1ccncc1C(=O)NC(=O)Nc1ccc(-c2ccccc2)c(C(F)(F)F)c1 10.1021/ml2001399
CHEMBL1938952 69558 36 None -123 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human S1P5 expressed in CHO-K1 cells coexpressing Gq/i5 assessed as calcium mobilization-induced bioluminescence change measured for 90 secs by fluorimetryAgonist activity at human S1P5 expressed in CHO-K1 cells coexpressing Gq/i5 assessed as calcium mobilization-induced bioluminescence change measured for 90 secs by fluorimetry
ChEMBL 415 4 2 4 4.7 COc1ccncc1C(=O)NC(=O)Nc1ccc(-c2ccccc2)c(C(F)(F)F)c1 10.1021/ml2001399
16038017 138888 0 None -398 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 431 7 1 6 4.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OCC(F)(F)F)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL379380 138888 0 None -398 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 431 7 1 6 4.5 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OCC(F)(F)F)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.084
52938426 3324 8 None -70 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 360 4 1 6 4.0 N#Cc1cc(ccc1OC(C)C)c1onc(n1)c1cccc2c1CC[C@@H]2N nan
9889 3324 8 None -70 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 360 4 1 6 4.0 N#Cc1cc(ccc1OC(C)C)c1onc(n1)c1cccc2c1CC[C@@H]2N nan
CHEMBL3899384 3324 8 None -70 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 360 4 1 6 4.0 N#Cc1cc(ccc1OC(C)C)c1onc(n1)c1cccc2c1CC[C@@H]2N nan
44412621 77992 0 None -416 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 391 7 1 6 4.4 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(OC(C)C)c(C#N)c2)o1 10.1016/j.bmcl.2006.04.064
CHEMBL211081 77992 0 None -416 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 391 7 1 6 4.4 Cc1cc(CCC(=O)O)ccc1-c1nnc(-c2ccc(OC(C)C)c(C#N)c2)o1 10.1016/j.bmcl.2006.04.064
44422606 85147 0 None 2 5 Human 7.3 pEC50 = 7.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 329 11 3 3 3.1 CCCCCCc1ccc(OC[C@H](N)CCP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
CHEMBL228049 85147 0 None 2 5 Human 7.3 pEC50 = 7.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 329 11 3 3 3.1 CCCCCCc1ccc(OC[C@H](N)CCP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
44342175 85095 0 None -2 4 Human 6.3 pEC50 = 6.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
CHEMBL227371 85095 0 None -2 4 Human 6.3 pEC50 = 6.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
CHEMBL422074 85095 0 None -2 4 Human 6.3 pEC50 = 6.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
67196597 147430 0 None -562 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 482 9 1 8 3.6 COCCS(=O)(=O)N[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
CHEMBL3933952 147430 0 None -562 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 482 9 1 8 3.6 COCCS(=O)(=O)N[C@@H]1CCc2c(-c3noc(-c4ccc(OC(C)C)c(C#N)c4)n3)cccc21 nan
44439850 145494 0 None -24 3 Human 8.3 pEC50 = 8.3 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 446 6 1 5 5.7 Cc1cc([C@@H]2C[C@H]2C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2006.10.057
CHEMBL391870 145494 0 None -24 3 Human 8.3 pEC50 = 8.3 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 446 6 1 5 5.7 Cc1cc([C@@H]2C[C@H]2C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2006.10.057
44439851 145114 0 None -37 3 Human 8.3 pEC50 = 8.3 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 403 6 1 6 4.6 Cc1cc([C@@H]2C[C@H]2C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.10.057
CHEMBL391581 145114 0 None -37 3 Human 8.3 pEC50 = 8.3 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 403 6 1 6 4.6 Cc1cc([C@@H]2C[C@H]2C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.10.057
46872626 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
9496 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
CHEMBL3741589 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assayAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
44438259 93394 0 None 2 2 Human 8.2 pEC50 = 8.2 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@@H]2C[C@@H](COP(=O)(O)O)N[C@H]2CO)cc1 10.1016/j.bmcl.2006.10.014
44438260 93394 0 None 2 2 Human 8.2 pEC50 = 8.2 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@@H]2C[C@@H](COP(=O)(O)O)N[C@H]2CO)cc1 10.1016/j.bmcl.2006.10.014
CHEMBL247699 93394 0 None 2 2 Human 8.2 pEC50 = 8.2 Functional
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assayActivity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
ChEMBL 399 12 4 4 3.5 CCCCCCCCc1ccc([C@@H]2C[C@@H](COP(=O)(O)O)N[C@H]2CO)cc1 10.1016/j.bmcl.2006.10.014
44406009 72364 0 None -10 4 Human 7.3 pEC50 = 7.3 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 515 18 5 10 3.4 N[C@@H](COP(=O)(O)O)[C@H](O)/C=C/CCCCCCCCCCNc1ccc([N+](=O)[O-])c2nonc12 10.1016/j.bmcl.2005.09.038
CHEMBL199754 72364 0 None -10 4 Human 7.3 pEC50 = 7.3 Functional
Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assayBinding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 515 18 5 10 3.4 N[C@@H](COP(=O)(O)O)[C@H](O)/C=C/CCCCCCCCCCNc1ccc([N+](=O)[O-])c2nonc12 10.1016/j.bmcl.2005.09.038
46224769 199158 0 None -251 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 331 2 1 3 4.3 Cc1nn(C(=O)/C=C/c2cccc3[nH]ccc23)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
CHEMBL601062 199158 0 None -251 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 331 2 1 3 4.3 Cc1nn(C(=O)/C=C/c2cccc3[nH]ccc23)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
57397320 67567 0 None 1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 357 3 0 4 3.8 C/N=C1\S/C(=C\c2cc(C)n(Cc3ccccc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910688 67567 0 None 1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 357 3 0 4 3.8 C/N=C1\S/C(=C\c2cc(C)n(Cc3ccccc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
11588811 3949 39 None 1 4 Human 7.3 pEC50 = 7.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](COP(=O)(O)O)N 10.1016/j.bmc.2006.10.060
136212600 3949 39 None 1 4 Human 7.3 pEC50 = 7.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](COP(=O)(O)O)N 10.1016/j.bmc.2006.10.060
3324 3949 39 None 1 4 Human 7.3 pEC50 = 7.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](COP(=O)(O)O)N 10.1016/j.bmc.2006.10.060
CHEMBL228102 3949 39 None 1 4 Human 7.3 pEC50 = 7.3 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](COP(=O)(O)O)N 10.1016/j.bmc.2006.10.060
11501873 139617 0 None -275 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 384 7 1 5 4.7 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(F)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL380253 139617 0 None -275 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 384 7 1 5 4.7 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(F)c2)n1 10.1016/j.bmcl.2006.04.084
52938427 2936 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C nan
5383 2936 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C nan
8709 2936 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C nan
CHEMBL3707247 2936 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C nan
DB12612 2936 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C nan
25110382 145576 0 None -354 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 366 6 1 6 4.2 CCOc1ccc(-c2nc(-c3cccc4c3CCC4O)no2)cc1OCC nan
CHEMBL3919445 145576 0 None -354 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 366 6 1 6 4.2 CCOc1ccc(-c2nc(-c3cccc4c3CCC4O)no2)cc1OCC nan
58344715 142541 0 None -575 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 468 8 2 8 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CCO)no2)cc1C#N nan
CHEMBL3895230 142541 0 None -575 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 468 8 2 8 3.0 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NS(=O)(=O)CCO)no2)cc1C#N nan
11224984 8629 18 None -13 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assayAgonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assay
ChEMBL 460 8 2 6 4.3 CCC/N=C1\S/C(=C\c2ccc(OC[C@@H](O)CO)c(Cl)c2)C(=O)N1c1ccccc1C 10.1021/jm100181s
CHEMBL1095833 8629 18 None -13 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assayAgonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assay
ChEMBL 460 8 2 6 4.3 CCC/N=C1\S/C(=C\c2ccc(OC[C@@H](O)CO)c(Cl)c2)C(=O)N1c1ccccc1C 10.1021/jm100181s
44412882 76935 0 None -1174 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 390 6 1 4 5.8 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL208168 76935 0 None -1174 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 390 6 1 4 5.8 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
25182926 7859 0 None 3 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 451 11 3 6 3.8 O=C(O)CCNCc1ccc(NC(=O)c2cc(N(CC3CC3)C3CCCCC3)ncn2)cc1 10.1016/j.bmcl.2010.01.102
CHEMBL1090423 7859 0 None 3 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 451 11 3 6 3.8 O=C(O)CCNCc1ccc(NC(=O)c2cc(N(CC3CC3)C3CCCCC3)ncn2)cc1 10.1016/j.bmcl.2010.01.102
66655775 167124 0 None 158 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 453 6 1 4 4.9 O=C(O)CCN1CCC2(CC1)COc1c2ccc(OCc2c(Cl)cccc2Cl)c1F 10.1016/j.bmcl.2017.12.018
CHEMBL4208771 167124 0 None 158 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 453 6 1 4 4.9 O=C(O)CCN1CCC2(CC1)COc1c2ccc(OCc2c(Cl)cccc2Cl)c1F 10.1016/j.bmcl.2017.12.018
CHEMBL4302165 167124 0 None 158 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 453 6 1 4 4.9 O=C(O)CCN1CCC2(CC1)COc1c2ccc(OCc2c(Cl)cccc2Cl)c1F 10.1016/j.bmcl.2017.12.018
11689680 79230 0 None -102 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 391 7 1 6 4.4 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL211505 79230 0 None -102 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 391 7 1 6 4.4 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.04.084
11689680 79230 0 None -102 3 Human 8.2 pEC50 = 8.2 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 391 7 1 6 4.4 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.10.057
CHEMBL211505 79230 0 None -102 3 Human 8.2 pEC50 = 8.2 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 391 7 1 6 4.4 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.10.057
90318624 180753 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 423 5 1 3 6.1 CC(C)(C)[C@H]1CC[C@H](Oc2ccc3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
CHEMBL4762836 180753 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 423 5 1 3 6.1 CC(C)(C)[C@H]1CC[C@H](Oc2ccc3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
57395471 67578 0 None -58 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 389 4 0 4 4.7 CC/N=C1\S/C(=C\c2cc(C)n(-c3ccc(F)cc3F)c2C)C(=O)N1CC 10.1016/j.bmcl.2011.09.049
CHEMBL1910800 67578 0 None -58 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 389 4 0 4 4.7 CC/N=C1\S/C(=C\c2cc(C)n(-c3ccc(F)cc3F)c2C)C(=O)N1CC 10.1016/j.bmcl.2011.09.049
45377662 83702 0 None -204 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 468 9 1 6 4.3 CCCCN(C(=O)c1ccccc1F)c1nnc(-c2ccc(CN3CC(C(=O)O)C3)cc2)s1 10.1016/j.bmcl.2012.09.110
CHEMBL2207778 83702 0 None -204 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 468 9 1 6 4.3 CCCCN(C(=O)c1ccccc1F)c1nnc(-c2ccc(CN3CC(C(=O)O)C3)cc2)s1 10.1016/j.bmcl.2012.09.110
56601979 167108 0 None 19 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 449 6 1 4 5.0 CC(CN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12)C(=O)O 10.1016/j.bmcl.2017.12.018
CHEMBL4217349 167108 0 None 19 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 449 6 1 4 5.0 CC(CN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12)C(=O)O 10.1016/j.bmcl.2017.12.018
CHEMBL4301966 167108 0 None 19 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 449 6 1 4 5.0 CC(CN1CCC2(CC1)COc1cc(OCc3c(Cl)cccc3Cl)ccc12)C(=O)O 10.1016/j.bmcl.2017.12.018
66655050 167140 0 None 100 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 419 6 1 4 4.3 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(F)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4207361 167140 0 None 100 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 419 6 1 4 4.3 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(F)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4302356 167140 0 None 100 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 419 6 1 4 4.3 O=C(O)CCN1CCC2(CC1)COc1cc(OCc3c(F)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
11452022 3539 33 None -3 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazineAgonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/jm200609t
6996 3539 33 None -3 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazineAgonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/jm200609t
CHEMBL366208 3539 33 None -3 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazineAgonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CC[C@@](COP(=O)(O)O)(CO)N 10.1021/jm200609t
57398996 67558 1 None -1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 343 2 0 4 3.8 C/N=C1\S/C(=C\c2cc(C)n(-c3ccc(F)cc3)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910674 67558 1 None -1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 343 2 0 4 3.8 C/N=C1\S/C(=C\c2cc(C)n(-c3ccc(F)cc3)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
77846591 181303 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 451 7 1 3 6.8 CCC(C)(C)[C@H]1CC[C@H](Oc2cc(C)c3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
CHEMBL4779029 181303 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assayAntagonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as EC80 S1P-induced calcium flux measured for 180 secs by FLIPR assay
ChEMBL 451 7 1 3 6.8 CCC(C)(C)[C@H]1CC[C@H](Oc2cc(C)c3ccccc3c2CN2CCC(C(=O)O)CC2)CC1 10.1021/acsmedchemlett.0c00631
66655836 166998 0 None 39 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 449 6 1 4 5.1 Cc1cc(Cl)c(COc2ccc3c(c2)OCC32CCN(CCC(=O)O)CC2)c(Cl)c1 10.1016/j.bmcl.2017.12.018
CHEMBL4213167 166998 0 None 39 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 449 6 1 4 5.1 Cc1cc(Cl)c(COc2ccc3c(c2)OCC32CCN(CCC(=O)O)CC2)c(Cl)c1 10.1016/j.bmcl.2017.12.018
CHEMBL4300404 166998 0 None 39 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 449 6 1 4 5.1 Cc1cc(Cl)c(COc2ccc3c(c2)OCC32CCN(CCC(=O)O)CC2)c(Cl)c1 10.1016/j.bmcl.2017.12.018
1776080 67551 7 None -3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 343 2 0 4 3.8 C/N=C1\S/C(=C\c2cc(C)n(-c3ccccc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
CHEMBL1910655 67551 7 None -3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 343 2 0 4 3.8 C/N=C1\S/C(=C\c2cc(C)n(-c3ccccc3F)c2C)C(=O)N1C 10.1016/j.bmcl.2011.09.049
11603726 76477 0 None -588 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 400 7 1 5 5.2 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.064
CHEMBL206940 76477 0 None -588 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 400 7 1 5 5.2 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.064
44422573 85131 0 None -2 4 Human 7.1 pEC50 = 7.1 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 370 12 4 3 3.4 CCCCCCCCc1ccc(NC(=O)[C@H](N)CCP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
CHEMBL227851 85131 0 None -2 4 Human 7.1 pEC50 = 7.1 Functional
Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assayActivity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay
ChEMBL 370 12 4 3 3.4 CCCCCCCCc1ccc(NC(=O)[C@H](N)CCP(=O)(O)O)cc1 10.1016/j.bmc.2006.10.060
58344692 144389 0 None -758 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 459 5 2 7 3.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CC(O)C3)no2)cc1C#N nan
CHEMBL3910269 144389 0 None -758 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrsAgonist activity at human S1P5 expressed in bla TANGO U2OS cells assessed as inhibition of cAMP formation preincubated for 4 hrs followed by FRET-based beta-lactamase fluorescent substrate addition measured after 2 hrs
ChEMBL 459 5 2 7 3.4 CC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@H]4NC(=O)N3CC(O)C3)no2)cc1C#N nan
145948099 167157 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 469 5 1 5 3.8 O=C(O)CN1CCC2(CC1)COc1cc(S(=O)(=O)Cc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4209494 167157 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 469 5 1 5 3.8 O=C(O)CN1CCC2(CC1)COc1cc(S(=O)(=O)Cc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
CHEMBL4302573 167157 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assayAgonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
ChEMBL 469 5 1 5 3.8 O=C(O)CN1CCC2(CC1)COc1cc(S(=O)(=O)Cc3c(Cl)cccc3Cl)ccc12 10.1016/j.bmcl.2017.12.018
136212602 11648 7 None 2 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 369 11 4 4 3.6 CCCCCCCCc1ccc2nc([C@@H](N)COP(=O)(O)O)[nH]c2c1 10.1016/j.bmcl.2011.09.049
44394498 11648 7 None 2 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 369 11 4 4 3.6 CCCCCCCCc1ccc2nc([C@@H](N)COP(=O)(O)O)[nH]c2c1 10.1016/j.bmcl.2011.09.049
CHEMBL1181619 11648 7 None 2 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 369 11 4 4 3.6 CCCCCCCCc1ccc2nc([C@@H](N)COP(=O)(O)O)[nH]c2c1 10.1016/j.bmcl.2011.09.049
CHEMBL1910653 11648 7 None 2 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at S1P5 receptorAgonist activity at S1P5 receptor
ChEMBL 369 11 4 4 3.6 CCCCCCCCc1ccc2nc([C@@H](N)COP(=O)(O)O)[nH]c2c1 10.1016/j.bmcl.2011.09.049
46224715 197578 0 None -7 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 371 3 1 5 2.5 Cc1nn(C(=O)/C=C/c2cccc(S(N)(=O)=O)c2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
CHEMBL590135 197578 0 None -7 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 371 3 1 5 2.5 Cc1nn(C(=O)/C=C/c2cccc(S(N)(=O)=O)c2)c2c1[C@H]1[C@@H](C2)C1(C)C 10.1016/j.bmcl.2009.11.045
11611053 77589 0 None -912 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 401 7 1 5 4.9 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(C(F)(F)C(C)C)cn2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL209567 77589 0 None -912 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 401 7 1 5 4.9 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2ccc(C(F)(F)C(C)C)cn2)n1 10.1016/j.bmcl.2006.04.084
44412883 76944 0 None -58 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 404 7 1 4 6.2 Cc1cc(CCCC(=O)O)ccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL208224 76944 0 None -58 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 404 7 1 4 6.2 Cc1cc(CCCC(=O)O)ccc1-c1noc(-c2ccc(C3CCCCC3)cc2)n1 10.1016/j.bmcl.2006.04.084
44547414 68001 0 None -67 6 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human S1P5 receptor expressed in HEK293 cells after 2 hrs by beta-arrestin assayAgonist activity at recombinant human S1P5 receptor expressed in HEK293 cells after 2 hrs by beta-arrestin assay
ChEMBL 499 5 1 5 5.2 O=C(O)CCC(=O)N1CCc2cc(-c3noc(-c4cc(C(F)(F)F)cc(C(F)(F)F)c4)n3)ccc21 10.1016/j.bmcl.2011.05.110
CHEMBL1916559 68001 0 None -67 6 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human S1P5 receptor expressed in HEK293 cells after 2 hrs by beta-arrestin assayAgonist activity at recombinant human S1P5 receptor expressed in HEK293 cells after 2 hrs by beta-arrestin assay
ChEMBL 499 5 1 5 5.2 O=C(O)CCC(=O)N1CCc2cc(-c3noc(-c4cc(C(F)(F)F)cc(C(F)(F)F)c4)n3)ccc21 10.1016/j.bmcl.2011.05.110
44439851 145114 0 None -37 3 Human 7.1 pEC50 = 7.1 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 403 6 1 6 4.6 Cc1cc([C@@H]2C[C@H]2C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.10.057
CHEMBL391581 145114 0 None -37 3 Human 7.1 pEC50 = 7.1 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 403 6 1 6 4.6 Cc1cc([C@@H]2C[C@H]2C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C#N)c2)n1 10.1016/j.bmcl.2006.10.057
11662328 91333 0 None -33 3 Human 8.0 pEC50 = 8 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 448 7 1 5 5.8 Cc1cc(CC(C)C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2006.10.057
CHEMBL241050 91333 0 None -33 3 Human 8.0 pEC50 = 8 Functional
Displacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cellsDisplacement of [35S]GTP-gamma-S from human S1P5 receptor expressed in CHO cells
ChEMBL 448 7 1 5 5.8 Cc1cc(CC(C)C(=O)O)ccc1-c1noc(-c2ccc(OC(C)C)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2006.10.057
46224712 199118 0 None -35 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 352 4 0 5 3.9 COc1ccc(/C=C/C(=O)n2nc(C)c3c2C[C@@H]2[C@H]3C2(C)C)cc1OC 10.1016/j.bmcl.2009.11.045
CHEMBL600762 199118 0 None -35 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human SIP5 receptor by [35S]GTPgammaS binding assayAgonist activity at human SIP5 receptor by [35S]GTPgammaS binding assay
ChEMBL 352 4 0 5 3.9 COc1ccc(/C=C/C(=O)n2nc(C)c3c2C[C@@H]2[C@H]3C2(C)C)cc1OC 10.1016/j.bmcl.2009.11.045
11697013 77872 0 None -1318 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 401 7 1 6 4.6 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2cnc(OC(C)C)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.064
CHEMBL210695 77872 0 None -1318 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S bindingAgonist activity at S1P5 receptor assessed as induction of [35S]GTP-gamma-S binding
ChEMBL 401 7 1 6 4.6 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2cnc(OC(C)C)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.064
11697013 77872 0 None -1318 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 401 7 1 6 4.6 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2cnc(OC(C)C)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.084
CHEMBL210695 77872 0 None -1318 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptakeAgonist activity at S1P5 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake
ChEMBL 401 7 1 6 4.6 Cc1cc(CCC(=O)O)ccc1-c1noc(-c2cnc(OC(C)C)c(Cl)c2)n1 10.1016/j.bmcl.2006.04.084
25182773 7545 0 None -53 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 443 7 2 6 3.2 Cc1cc(S(N)(=O)=O)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
CHEMBL1088177 7545 0 None -53 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assayAgonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 443 7 2 6 3.2 Cc1cc(S(N)(=O)=O)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1 10.1016/j.bmcl.2010.01.102
44607575 52267 0 None -69 5 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 375 4 1 3 5.8 COc1cccc(C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 nan
CHEMBL1592119 52267 0 None -69 5 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 375 4 1 3 5.8 COc1cccc(C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 nan
44607577 43645 0 None -120 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 415 5 1 2 7.8 CC(C)c1cccc(C(C)C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 nan
CHEMBL1511839 43645 0 None -120 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 415 5 1 2 7.8 CC(C)c1cccc(C(C)C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 nan
2328694 53446 2 None -8 5 Human 5.9 pIC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 408 6 2 3 5.2 O=C(Nc1ccccc1)Nc1cc(OCC(F)(F)F)cc(OCC(F)(F)F)c1 nan
CHEMBL1603615 53446 2 None -8 5 Human 5.9 pIC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 408 6 2 3 5.2 O=C(Nc1ccccc1)Nc1cc(OCC(F)(F)F)cc(OCC(F)(F)F)c1 nan
46872388 136248 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 303 8 1 3 3.4 CCCCCC(=O)c1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3741172 136248 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 303 8 1 3 3.4 CCCCCC(=O)c1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
4492589 30692 7 None -181 4 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at S1P5 receptorAntagonist activity at S1P5 receptor
ChEMBL 359 3 1 2 6.1 Cc1cccc(C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 10.1016/j.bmcl.2011.06.132
CHEMBL1397874 30692 7 None -181 4 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at S1P5 receptorAntagonist activity at S1P5 receptor
ChEMBL 359 3 1 2 6.1 Cc1cccc(C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 10.1016/j.bmcl.2011.06.132
44607578 52068 0 None -45 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 379 7 1 4 5.5 CCOc1ccc(OC)cc1-c1ccc(C(=O)Nc2c(C)cccc2CC)o1 nan
CHEMBL1589684 52068 0 None -45 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 379 7 1 4 5.5 CCOc1ccc(OC)cc1-c1ccc(C(=O)Nc2c(C)cccc2CC)o1 nan
59451874 136123 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 289 8 1 3 3.0 CCCCCC(=O)c1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740009 136123 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 289 8 1 3 3.0 CCCCCC(=O)c1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
46872386 136073 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 323 6 1 3 3.0 O=C(Cc1ccccc1)c1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3739593 136073 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 323 6 1 3 3.0 O=C(Cc1ccccc1)c1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
59451795 136183 1 None - 1 Human 7.5 pIC50 = 7.5 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 309 6 1 3 2.6 O=C(Cc1ccccc1)c1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740604 136183 1 None - 1 Human 7.5 pIC50 = 7.5 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 309 6 1 3 2.6 O=C(Cc1ccccc1)c1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
6217704 32367 3 None 7 6 Human 7.5 pIC50 = 7.5 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 490 7 0 8 5.2 CCOC(=O)/C(=C\c1ccc(OC(F)F)cc1)C1=Nn2c(nnc2-c2ccc(Cl)cc2)SC1 nan
CHEMBL1412583 32367 3 None 7 6 Human 7.5 pIC50 = 7.5 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 490 7 0 8 5.2 CCOC(=O)/C(=C\c1ccc(OC(F)F)cc1)C1=Nn2c(nnc2-c2ccc(Cl)cc2)SC1 nan
59451808 136223 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 317 9 1 3 3.7 CCCCCCC(=O)c1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740964 136223 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 317 9 1 3 3.7 CCCCCCC(=O)c1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
46872389 136106 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 303 9 1 3 3.4 CCCCCCC(=O)c1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3739887 136106 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 303 9 1 3 3.4 CCCCCCC(=O)c1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
59451857 136142 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 391 6 1 3 4.3 O=C(Cc1ccc(Cl)c(Cl)c1)c1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740180 136142 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 391 6 1 3 4.3 O=C(Cc1ccc(Cl)c(Cl)c1)c1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
59451852 136339 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 377 6 1 3 3.9 O=C(Cc1ccc(Cl)c(Cl)c1)c1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3741988 136339 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB methodAgonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
ChEMBL 377 6 1 3 3.9 O=C(Cc1ccc(Cl)c(Cl)c1)c1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
1363299 32724 10 None -37 5 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 359 3 1 2 6.1 Cc1cccc(C)c1NC(=O)c1ccc(-c2ccc(Cl)cc2Cl)o1 nan
CHEMBL1415555 32724 10 None -37 5 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluorescence dose response cell-based screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 5 (S1P5). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1510, AID1524, AID1692, AID1853, AID2332, AID489009, AID489017]
ChEMBL 359 3 1 2 6.1 Cc1cccc(C)c1NC(=O)c1ccc(-c2ccc(Cl)cc2Cl)o1 nan
71450073 82177 0 None -288 4 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human S1P5R receptor expressed in CHO cell membranes by [35S]GTPgamma binding assayAntagonist activity at human S1P5R receptor expressed in CHO cell membranes by [35S]GTPgamma binding assay
ChEMBL 585 10 2 5 5.5 Cc1cc(S(=O)(=O)Nc2cccc(-c3cc(C)c(C(=O)N(C)[C@@H](CCN(C)C)C(=O)O)c(C)c3)c2)c(C)cc1Cl 10.1021/jm3009508
CHEMBL2178814 82177 0 None -288 4 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human S1P5R receptor expressed in CHO cell membranes by [35S]GTPgamma binding assayAntagonist activity at human S1P5R receptor expressed in CHO cell membranes by [35S]GTPgamma binding assay
ChEMBL 585 10 2 5 5.5 Cc1cc(S(=O)(=O)Nc2cccc(-c3cc(C)c(C(=O)N(C)[C@@H](CCN(C)C)C(=O)O)c(C)c3)c2)c(C)cc1Cl 10.1021/jm3009508
11363176 3100 42 None -3 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 460 8 2 6 4.3 CCCN=C1S/C(=C\c2ccc(c(c2)Cl)OC[C@@H](CO)O)/C(=O)N1c1ccccc1C None
5446 3100 42 None -3 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 460 8 2 6 4.3 CCCN=C1S/C(=C\c2ccc(c(c2)Cl)OC[C@@H](CO)O)/C(=O)N1c1ccccc1C None
9320 3100 42 None -3 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 460 8 2 6 4.3 CCCN=C1S/C(=C\c2ccc(c(c2)Cl)OC[C@@H](CO)O)/C(=O)N1c1ccccc1C None
CHEMBL1096146 3100 42 None -3 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 460 8 2 6 4.3 CCCN=C1S/C(=C\c2ccc(c(c2)Cl)OC[C@@H](CO)O)/C(=O)N1c1ccccc1C None
52938427 2936 47 None -33 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
5383 2936 47 None -33 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
8709 2936 47 None -33 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
CHEMBL3707247 2936 47 None -33 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
DB12612 2936 47 None -33 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
44599207 3552 40 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Possible mechanism of actionPossible mechanism of action
Drug Central 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C None
5326 3552 40 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Possible mechanism of actionPossible mechanism of action
Drug Central 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C None
9289 3552 40 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Possible mechanism of actionPossible mechanism of action
Drug Central 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C None
CHEMBL2336071 3552 40 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Possible mechanism of actionPossible mechanism of action
Drug Central 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C None
DB12371 3552 40 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Possible mechanism of actionPossible mechanism of action
Drug Central 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C None
107970 1609 76 None -77 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
Drug Central 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N None
2407 1609 76 None -77 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
Drug Central 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N None
4167 1609 76 None -77 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
Drug Central 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N None
CHEMBL314854 1609 76 None -77 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
Drug Central 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N None
DB08868 1609 76 None -77 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
Drug Central 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N None
52938426 3324 8 None -70 5 Human 8.2 pEC50 = 8.2 Functional
As measured in a GTPγS assay.As measured in a GTPγS assay.
Guide to Pharmacology 360 4 1 6 4.0 N#Cc1cc(ccc1OC(C)C)c1onc(n1)c1cccc2c1CC[C@@H]2N 29608575
9889 3324 8 None -70 5 Human 8.2 pEC50 = 8.2 Functional
As measured in a GTPγS assay.As measured in a GTPγS assay.
Guide to Pharmacology 360 4 1 6 4.0 N#Cc1cc(ccc1OC(C)C)c1onc(n1)c1cccc2c1CC[C@@H]2N 29608575
CHEMBL3899384 3324 8 None -70 5 Human 8.2 pEC50 = 8.2 Functional
As measured in a GTPγS assay.As measured in a GTPγS assay.
Guide to Pharmacology 360 4 1 6 4.0 N#Cc1cc(ccc1OC(C)C)c1onc(n1)c1cccc2c1CC[C@@H]2N 29608575
44623998 1566 33 None -75 8 Human 7.6 pEC50 = 7.6 Functional
In a β-arrestin recruitment assay.In a β-arrestin recruitment assay.
Guide to Pharmacology 457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1 25516790
9331 1566 33 None -75 8 Human 7.6 pEC50 = 7.6 Functional
In a β-arrestin recruitment assay.In a β-arrestin recruitment assay.
Guide to Pharmacology 457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1 25516790
CHEMBL3358920 1566 33 None -75 8 Human 7.6 pEC50 = 7.6 Functional
In a β-arrestin recruitment assay.In a β-arrestin recruitment assay.
Guide to Pharmacology 457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1 25516790
DB14766 1566 33 None -75 8 Human 7.6 pEC50 = 7.6 Functional
In a β-arrestin recruitment assay.In a β-arrestin recruitment assay.
Guide to Pharmacology 457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1 25516790
46872626 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 26509640
46872626 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 29688337
9496 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 26509640
9496 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 29688337
CHEMBL3741589 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 26509640
CHEMBL3741589 213 18 None 72 2 Human 8.2 pEC50 = 8.2 Functional
In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.In a GTP&gamma;S assay using membranes from S1P<sub>5</sub>-transfected HEK293 cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 29688337
52938427 2936 47 None -33 5 Human 8.0 pEC50 = 8.0 Functional
In a GTP&gamma;S assay.In a GTP&gamma;S assay.
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 26990079
5383 2936 47 None -33 5 Human 8.0 pEC50 = 8.0 Functional
In a GTP&gamma;S assay.In a GTP&gamma;S assay.
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 26990079
8709 2936 47 None -33 5 Human 8.0 pEC50 = 8.0 Functional
In a GTP&gamma;S assay.In a GTP&gamma;S assay.
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 26990079
CHEMBL3707247 2936 47 None -33 5 Human 8.0 pEC50 = 8.0 Functional
In a GTP&gamma;S assay.In a GTP&gamma;S assay.
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 26990079
DB12612 2936 47 None -33 5 Human 8.0 pEC50 = 8.0 Functional
In a GTP&gamma;S assay.In a GTP&gamma;S assay.
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C 26990079
44599207 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 22646698
44599207 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 24125884
44599207 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 9735753
5326 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 22646698
5326 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 24125884
5326 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 9735753
9289 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 22646698
9289 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 24125884
9289 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 9735753
CHEMBL2336071 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 22646698
CHEMBL2336071 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 24125884
CHEMBL2336071 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 9735753
DB12371 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 22646698
DB12371 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 24125884
DB12371 3552 40 None -3 5 Human 9.0 pEC50 = 9.0 Functional
In a GTP&gamma;S binding assayIn a GTP&gamma;S binding assay
Guide to Pharmacology 516 9 1 4 6.8 CCc1cc(ccc1CN1CC(C1)C(=O)O)/C(=N/OCc1ccc(c(c1)C(F)(F)F)C1CCCCC1)/C 9735753
16755143 499 0 None -1 4 Human 8.1 pEC50 = 8.1 Functional
In a GTP&gamma;S binding assay.In a GTP&gamma;S binding assay.
Guide to Pharmacology 442 4 1 5 5.6 C[C@@H](C(F)(F)F)Oc1ccc(cc1C(F)(F)F)c1onc(n1)c1ccc2c(c1)nc[nH]2 25347187
9569 499 0 None -1 4 Human 8.1 pEC50 = 8.1 Functional
In a GTP&gamma;S binding assay.In a GTP&gamma;S binding assay.
Guide to Pharmacology 442 4 1 5 5.6 C[C@@H](C(F)(F)F)Oc1ccc(cc1C(F)(F)F)c1onc(n1)c1ccc2c(c1)nc[nH]2 25347187
CHEMBL4297350 499 0 None -1 4 Human 8.1 pEC50 = 8.1 Functional
In a GTP&gamma;S binding assay.In a GTP&gamma;S binding assay.
Guide to Pharmacology 442 4 1 5 5.6 C[C@@H](C(F)(F)F)Oc1ccc(cc1C(F)(F)F)c1onc(n1)c1ccc2c(c1)nc[nH]2 25347187
DB11819 499 0 None -1 4 Human 8.1 pEC50 = 8.1 Functional
In a GTP&gamma;S binding assay.In a GTP&gamma;S binding assay.
Guide to Pharmacology 442 4 1 5 5.6 C[C@@H](C(F)(F)F)Oc1ccc(cc1C(F)(F)F)c1onc(n1)c1ccc2c(c1)nc[nH]2 25347187
46872626 213 18 None 72 2 Human 8.4 pEC50 = 8.4 Functional
In a forskolin-induced cAMP inhibition assay in S1P<sub>5</sub>-transfected CHO cells.In a forskolin-induced cAMP inhibition assay in S1P<sub>5</sub>-transfected CHO cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 26509640
9496 213 18 None 72 2 Human 8.4 pEC50 = 8.4 Functional
In a forskolin-induced cAMP inhibition assay in S1P<sub>5</sub>-transfected CHO cells.In a forskolin-induced cAMP inhibition assay in S1P<sub>5</sub>-transfected CHO cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 26509640
CHEMBL3741589 213 18 None 72 2 Human 8.4 pEC50 = 8.4 Functional
In a forskolin-induced cAMP inhibition assay in S1P<sub>5</sub>-transfected CHO cells.In a forskolin-induced cAMP inhibition assay in S1P<sub>5</sub>-transfected CHO cells.
Guide to Pharmacology 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 26509640
49848557 1080 0 None -6 5 Human 7.8 pEC50 = 7.8 Functional
In an aequorin calcium accumulation assay.In an aequorin calcium accumulation assay.
Guide to Pharmacology 461 7 1 8 4.0 OC(=O)CCN1CCc2c(C1)c(C)n(n2)c1nnc(s1)c1ccc(c(c1)Cl)OC(C)C 26751273
9492 1080 0 None -6 5 Human 7.8 pEC50 = 7.8 Functional
In an aequorin calcium accumulation assay.In an aequorin calcium accumulation assay.
Guide to Pharmacology 461 7 1 8 4.0 OC(=O)CCN1CCc2c(C1)c(C)n(n2)c1nnc(s1)c1ccc(c(c1)Cl)OC(C)C 26751273
CHEMBL3769933 1080 0 None -6 5 Human 7.8 pEC50 = 7.8 Functional
In an aequorin calcium accumulation assay.In an aequorin calcium accumulation assay.
Guide to Pharmacology 461 7 1 8 4.0 OC(=O)CCN1CCc2c(C1)c(C)n(n2)c1nnc(s1)c1ccc(c(c1)Cl)OC(C)C 26751273
11259583 520 12 None -380 6 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 455 7 2 3 6.8 OC(=O)CCNCc1ccc2c(c1)cc(s2)c1ccc(c(c1)C(F)(F)F)c1ccccc1 17114004
2925 520 12 None -380 6 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 455 7 2 3 6.8 OC(=O)CCNCc1ccc2c(c1)cc(s2)c1ccc(c(c1)C(F)(F)F)c1ccccc1 17114004
CHEMBL4579553 520 12 None -380 6 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 455 7 2 3 6.8 OC(=O)CCNCc1ccc2c(c1)cc(s2)c1ccc(c(c1)C(F)(F)F)c1ccccc1 17114004
11311 1847 0 None -3 2 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 440 8 1 7 5.1 OC(=O)CCCn1ccc2c1cccc2c1noc(n1)c1cnc(c(c1)Cl)OC(C)C 27128606
24988201 1847 0 None -3 2 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 440 8 1 7 5.1 OC(=O)CCCn1ccc2c1cccc2c1noc(n1)c1cnc(c(c1)Cl)OC(C)C 27128606
CHEMBL4297542 1847 0 None -3 2 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 440 8 1 7 5.1 OC(=O)CCCn1ccc2c1cccc2c1noc(n1)c1cnc(c(c1)Cl)OC(C)C 27128606
DB11987 1847 0 None -3 2 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 440 8 1 7 5.1 OC(=O)CCCn1ccc2c1cccc2c1noc(n1)c1cnc(c(c1)Cl)OC(C)C 27128606
52938427 2936 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
5383 2936 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
8709 2936 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
CHEMBL3707247 2936 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
DB12612 2936 47 None -33 5 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 404 7 2 7 3.6 OCCN[C@H]1CCc2c1cccc2c1noc(n1)c1ccc(c(c1)C#N)OC(C)C None
10883396 3592 39 None -12 14 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11705398
10883396 3592 39 None -12 14 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 14732717
5283560 3592 39 None -12 14 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11705398
5283560 3592 39 None -12 14 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 14732717
911 3592 39 None -12 14 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11705398
911 3592 39 None -12 14 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 14732717
CHEMBL225155 3592 39 None -12 14 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11705398
CHEMBL225155 3592 39 None -12 14 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 14732717
10883396 3592 39 None -2 14 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11705398
10883396 3592 39 None -2 14 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11967257
10883396 3592 39 None -2 14 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 14732717
10883396 3592 39 None -2 14 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 17114004
5283560 3592 39 None -2 14 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11705398
5283560 3592 39 None -2 14 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11967257
5283560 3592 39 None -2 14 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 14732717
5283560 3592 39 None -2 14 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 17114004
911 3592 39 None -2 14 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11705398
911 3592 39 None -2 14 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11967257
911 3592 39 None -2 14 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 14732717
911 3592 39 None -2 14 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 17114004
CHEMBL225155 3592 39 None -2 14 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11705398
CHEMBL225155 3592 39 None -2 14 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 11967257
CHEMBL225155 3592 39 None -2 14 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 14732717
CHEMBL225155 3592 39 None -2 14 Human 8.2 pEC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 17114004
6992 3946 0 None 7 2 Human 8.6 pEC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 369 11 3 3 4.3 CCCCCCCCc1cccc(c1)C1CC(C1)(N)COP(=O)(O)O 21632869
73755254 3946 0 None 7 2 Human 8.6 pEC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 369 11 3 3 4.3 CCCCCCCCc1cccc(c1)C1CC(C1)(N)COP(=O)(O)O 21632869
10904818 300 0 None -1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 11967257
10904818 300 0 None -1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 14732717
2937 300 0 None -1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 11967257
2937 300 0 None -1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 14732717
CHEMBL382739 300 0 None -1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 11967257
CHEMBL382739 300 0 None -1 4 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 373 13 3 4 3.8 CCCCCCCOc1ccc(cc1)CC[C@](COP(=O)(O)O)(N)C 14732717
2924 1610 37 None -4 6 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 11967257
2924 1610 37 None -4 6 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 14747617
2924 1610 37 None -4 6 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 17114004
44398069 1610 37 None -4 6 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 11967257
44398069 1610 37 None -4 6 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 14747617
44398069 1610 37 None -4 6 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 17114004
9908268 1610 37 None -4 6 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 11967257
9908268 1610 37 None -4 6 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 14747617
9908268 1610 37 None -4 6 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 17114004
CHEMBL114606 1610 37 None -4 6 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 11967257
CHEMBL114606 1610 37 None -4 6 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 14747617
CHEMBL114606 1610 37 None -4 6 Human 8.9 pEC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 17114004
11259583 520 12 None -354 6 Mouse 6.5 pEC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 455 7 2 3 6.8 OC(=O)CCNCc1ccc2c(c1)cc(s2)c1ccc(c(c1)C(F)(F)F)c1ccccc1 17114004
2925 520 12 None -354 6 Mouse 6.5 pEC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 455 7 2 3 6.8 OC(=O)CCNCc1ccc2c(c1)cc(s2)c1ccc(c(c1)C(F)(F)F)c1ccccc1 17114004
CHEMBL4579553 520 12 None -354 6 Mouse 6.5 pEC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 455 7 2 3 6.8 OC(=O)CCNCc1ccc2c(c1)cc(s2)c1ccc(c(c1)C(F)(F)F)c1ccccc1 17114004
11545181 3952 4 None -1 3 Human 7.5 pEC50 None 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 12 4 3 3.4 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](CCP(=O)(O)O)N 17113298
2930 3952 4 None -1 3 Human 7.5 pEC50 None 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 12 4 3 3.4 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](CCP(=O)(O)O)N 17113298
CHEMBL389033 3952 4 None -1 3 Human 7.5 pEC50 None 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 12 4 3 3.4 CCCCCCCCc1cccc(c1)NC(=O)[C@@H](CCP(=O)(O)O)N 17113298
12573 980 1 None - 1 Human 10.0 pIC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 33738061
77846592 980 1 None - 1 Human 10.0 pIC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 33738061
CHEMBL4748198 980 1 None - 1 Human 10.0 pIC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 33738061
107970 1609 76 None -77 4 Human 5.7 pIC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 15615513
2407 1609 76 None -77 4 Human 5.7 pIC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 15615513
4167 1609 76 None -77 4 Human 5.7 pIC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 15615513
CHEMBL314854 1609 76 None -77 4 Human 5.7 pIC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 15615513
DB08868 1609 76 None -77 4 Human 5.7 pIC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 15615513
2924 1610 37 None -4 6 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 14747617
44398069 1610 37 None -4 6 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 14747617
9908268 1610 37 None -4 6 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 14747617
CHEMBL114606 1610 37 None -4 6 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 14747617
10430549 1032 33 None -1 4 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 16190743
2929 1032 33 None -1 4 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 16190743
CHEMBL194419 1032 33 None -1 4 Human 9.0 pIC50 None 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 16190743


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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
10883396 3592 39 None - 4 Human 9.7 pEC50 = 9.7 Binding
Displacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation countingDisplacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm100181s
5283560 3592 39 None - 4 Human 9.7 pEC50 = 9.7 Binding
Displacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation countingDisplacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm100181s
911 3592 39 None - 4 Human 9.7 pEC50 = 9.7 Binding
Displacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation countingDisplacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm100181s
CHEMBL225155 3592 39 None - 4 Human 9.7 pEC50 = 9.7 Binding
Displacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation countingDisplacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm100181s
107970 1609 76 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2013.09.058
2407 1609 76 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2013.09.058
4167 1609 76 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2013.09.058
CHEMBL314854 1609 76 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2013.09.058
DB08868 1609 76 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at S1P5 receptor (unknown origin)Agonist activity at S1P5 receptor (unknown origin)
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1016/j.bmcl.2013.09.058
49868651 170582 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at S1P5 receptor (unknown origin) measured after 45 mins by [35S]GTP-gammaS binding assayAgonist activity at S1P5 receptor (unknown origin) measured after 45 mins by [35S]GTP-gammaS binding assay
ChEMBL 542 8 2 8 5.3 O=C(O)C[C@H]1CCCN(C[C@@H](O)c2ccc(-c3noc(-c4onc(-c5ccccc5)c4C(F)(F)F)n3)cc2)C1 10.1021/acs.jmedchem.6b00373
CHEMBL4458575 170582 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at S1P5 receptor (unknown origin) measured after 45 mins by [35S]GTP-gammaS binding assayAgonist activity at S1P5 receptor (unknown origin) measured after 45 mins by [35S]GTP-gammaS binding assay
ChEMBL 542 8 2 8 5.3 O=C(O)C[C@H]1CCCN(C[C@@H](O)c2ccc(-c3noc(-c4onc(-c5ccccc5)c4C(F)(F)F)n3)cc2)C1 10.1021/acs.jmedchem.6b00373
50925337 169884 6 None - 0 Human 9.0 pEC50 = 9.0 Binding
Agonist activity at S1P5 receptor (unknown origin) measured after 45 mins by [35S]GTP-gammaS binding assayAgonist activity at S1P5 receptor (unknown origin) measured after 45 mins by [35S]GTP-gammaS binding assay
ChEMBL 528 7 2 8 4.9 O=C(O)[C@H]1CCCN(C[C@@H](O)c2ccc(-c3noc(-c4onc(-c5ccccc5)c4C(F)(F)F)n3)cc2)C1 10.1021/acs.jmedchem.6b00373
CHEMBL4448752 169884 6 None - 0 Human 9.0 pEC50 = 9.0 Binding
Agonist activity at S1P5 receptor (unknown origin) measured after 45 mins by [35S]GTP-gammaS binding assayAgonist activity at S1P5 receptor (unknown origin) measured after 45 mins by [35S]GTP-gammaS binding assay
ChEMBL 528 7 2 8 4.9 O=C(O)[C@H]1CCCN(C[C@@H](O)c2ccc(-c3noc(-c4onc(-c5ccccc5)c4C(F)(F)F)n3)cc2)C1 10.1021/acs.jmedchem.6b00373
10883396 3592 39 None - 4 Human 8.8 pEC50 = 8.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2004.07.030
5283560 3592 39 None - 4 Human 8.8 pEC50 = 8.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2004.07.030
911 3592 39 None - 4 Human 8.8 pEC50 = 8.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2004.07.030
CHEMBL225155 3592 39 None - 4 Human 8.8 pEC50 = 8.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2004.07.030
134130131 141755 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 339 7 2 3 4.8 Cc1cccc(-c2cccc3cc(CNCCCC(=O)O)sc23)c1 10.1016/j.bmcl.2016.11.050
CHEMBL3885151 141755 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 339 7 2 3 4.8 Cc1cccc(-c2cccc3cc(CNCCCC(=O)O)sc23)c1 10.1016/j.bmcl.2016.11.050
46174905 115788 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 457 6 1 3 6.9 O=C(O)CC1CCn2c1cc1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12 10.1021/ml500422m
CHEMBL3358955 115788 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 457 6 1 3 6.9 O=C(O)CC1CCn2c1cc1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12 10.1021/ml500422m
134129958 141748 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 376 6 3 4 4.2 NC(CNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
CHEMBL3885074 141748 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 376 6 3 4 4.2 NC(CNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
44342468 12012 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL1184089 12012 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL332050 12012 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
11682677 11677 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 395 12 4 4 4.1 CCCCCCCCc1ccc(-c2c[nH]c([C@@H](N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1181748 11677 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 395 12 4 4 4.1 CCCCCCCCc1ccc(-c2c[nH]c([C@@H](N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL190865 11677 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 395 12 4 4 4.1 CCCCCCCCc1ccc(-c2c[nH]c([C@@H](N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
44342231 11994 3 None - 0 Human 5.9 pEC50 = 5.9 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 408 19 4 4 4.0 CCCCCCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
CHEMBL1183950 11994 3 None - 0 Human 5.9 pEC50 = 5.9 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 408 19 4 4 4.0 CCCCCCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
CHEMBL325408 11994 3 None - 0 Human 5.9 pEC50 = 5.9 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 408 19 4 4 4.0 CCCCCCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
134131071 141589 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 O=C(O)CCCNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883377 141589 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 O=C(O)CCCNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1 10.1016/j.bmcl.2016.11.050
134130884 141618 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 389 8 2 3 6.1 O=C(O)CCCCNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883572 141618 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 389 8 2 3 6.1 O=C(O)CCCCNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1 10.1016/j.bmcl.2016.11.050
134131188 141766 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 354 7 3 4 3.6 CCc1ccccc1-c1cccc2cc(CNCC(N)C(=O)O)sc12 10.1016/j.bmcl.2016.11.050
CHEMBL3885229 141766 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 354 7 3 4 3.6 CCc1ccccc1-c1cccc2cc(CNCC(N)C(=O)O)sc12 10.1016/j.bmcl.2016.11.050
44398049 13067 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 441 13 5 5 3.4 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1190950 13067 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 441 13 5 5 3.4 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL541890 13067 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 441 13 5 5 3.4 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
44342331 11311 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 428 16 4 4 4.5 CCCCCCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL116953 11311 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 428 16 4 4 4.5 CCCCCCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL1180214 11311 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 428 16 4 4 4.5 CCCCCCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
44342244 64545 3 None - 0 Human 5.8 pEC50 = 5.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 380 17 4 4 3.2 CCCCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
CHEMBL182164 64545 3 None - 0 Human 5.8 pEC50 = 5.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 380 17 4 4 3.2 CCCCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
CHEMBL423691 64545 3 None - 0 Human 5.8 pEC50 = 5.8 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 380 17 4 4 3.2 CCCCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
134130571 141685 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 7.0 O=C(O)Cc1cccc(NCc2cc3cccc(-c4ccc5ccccc5c4)c3s2)c1 10.1016/j.bmcl.2016.11.050
CHEMBL3884292 141685 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 7.0 O=C(O)Cc1cccc(NCc2cc3cccc(-c4ccc5ccccc5c4)c3s2)c1 10.1016/j.bmcl.2016.11.050
44398076 12791 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 425 13 5 5 3.2 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1188968 12791 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 425 13 5 5 3.2 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL537849 12791 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 425 13 5 5 3.2 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
134131598 141738 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 373 4 1 3 5.2 O=C(O)C1CN(Cc2cc3c(-c4ccc5ccccc5c4)cccc3s2)C1 10.1016/j.bmcl.2016.11.050
CHEMBL3884966 141738 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 373 4 1 3 5.2 O=C(O)C1CN(Cc2cc3c(-c4ccc5ccccc5c4)cccc3s2)C1 10.1016/j.bmcl.2016.11.050
53362086 115855 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F 10.1021/ml500422m
CHEMBL3359523 115855 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 481 7 1 4 6.6 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C(F)(F)F 10.1021/ml500422m
134131470 141763 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 7 2 3 6.4 CCc1ccccc1-c1cccc2cc(CNc3ccc(CC(=O)O)cc3)sc12 10.1016/j.bmcl.2016.11.050
CHEMBL3885195 141763 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 7 2 3 6.4 CCc1ccccc1-c1cccc2cc(CNc3ccc(CC(=O)O)cc3)sc12 10.1016/j.bmcl.2016.11.050
134130538 141629 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 351 5 1 3 4.6 CCc1ccccc1-c1cccc2sc(CN3CC(C(=O)O)C3)cc12 10.1016/j.bmcl.2016.11.050
CHEMBL3883646 141629 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 351 5 1 3 4.6 CCc1ccccc1-c1cccc2sc(CN3CC(C(=O)O)C3)cc12 10.1016/j.bmcl.2016.11.050
134131301 141630 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 7.0 O=C(O)Cc1cccc(NCc2cc3c(-c4ccc5ccccc5c4)cccc3s2)c1 10.1016/j.bmcl.2016.11.050
CHEMBL3883658 141630 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 7.0 O=C(O)Cc1cccc(NCc2cc3c(-c4ccc5ccccc5c4)cccc3s2)c1 10.1016/j.bmcl.2016.11.050
124171453 136802 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
ChEMBL 473 6 0 7 4.5 Cc1nc(CC(C)C)cc(-c2nc(-c3cc(F)c(O[C@@H]4CCC(=O)N(C)C4)cc3Cl)no2)n1 10.1016/j.bmcl.2015.11.090
CHEMBL3752660 136802 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
ChEMBL 473 6 0 7 4.5 Cc1nc(CC(C)C)cc(-c2nc(-c3cc(F)c(O[C@@H]4CCC(=O)N(C)C4)cc3Cl)no2)n1 10.1016/j.bmcl.2015.11.090
134130169 141621 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 373 4 1 3 5.2 O=C(O)C1CN(Cc2cc3cc(-c4ccc5ccccc5c4)ccc3s2)C1 10.1016/j.bmcl.2016.11.050
CHEMBL3883597 141621 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 373 4 1 3 5.2 O=C(O)C1CN(Cc2cc3cc(-c4ccc5ccccc5c4)ccc3s2)C1 10.1016/j.bmcl.2016.11.050
134130662 141742 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 6 2 3 5.5 CC(CNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
CHEMBL3884995 141742 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 6 2 3 5.5 CC(CNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
134130114 141739 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 O=C(O)CCCNCc1cc2cccc(-c3cccc4ccccc34)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3884986 141739 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 O=C(O)CCCNCc1cc2cccc(-c3cccc4ccccc34)c2s1 10.1016/j.bmcl.2016.11.050
44623998 1566 33 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1 10.1021/ml500389m
9331 1566 33 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1 10.1021/ml500389m
CHEMBL3358920 1566 33 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1 10.1021/ml500389m
DB14766 1566 33 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1 10.1021/ml500389m
44394564 12152 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 289 9 3 3 3.5 CCCCCCCCc1ccc2[nH]c([C@@H](N)CO)nc2c1 10.1016/j.bmcl.2004.07.030
CHEMBL1184660 12152 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 289 9 3 3 3.5 CCCCCCCCc1ccc2[nH]c([C@@H](N)CO)nc2c1 10.1016/j.bmcl.2004.07.030
CHEMBL363076 12152 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 289 9 3 3 3.5 CCCCCCCCc1ccc2[nH]c([C@@H](N)CO)nc2c1 10.1016/j.bmcl.2004.07.030
134130188 141660 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 367 9 2 3 5.5 CCc1ccccc1-c1cccc2cc(CNCCCCC(=O)O)sc12 10.1016/j.bmcl.2016.11.050
CHEMBL3884048 141660 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 367 9 2 3 5.5 CCc1ccccc1-c1cccc2cc(CNCCCCC(=O)O)sc12 10.1016/j.bmcl.2016.11.050
134130519 141649 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 361 6 2 3 5.3 O=C(O)CCNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883972 141649 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 361 6 2 3 5.3 O=C(O)CCNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1 10.1016/j.bmcl.2016.11.050
134130022 141678 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 339 7 2 3 4.7 CCc1ccccc1-c1cccc2cc(CNCCC(=O)O)sc12 10.1016/j.bmcl.2016.11.050
CHEMBL3884172 141678 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 339 7 2 3 4.7 CCc1ccccc1-c1cccc2cc(CNCCC(=O)O)sc12 10.1016/j.bmcl.2016.11.050
11675907 11671 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 409 12 4 4 4.3 CCCCCCCCc1ccc(-c2c[nH]c(C(C)(N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1181694 11671 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 409 12 4 4 4.3 CCCCCCCCc1ccc(-c2c[nH]c(C(C)(N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL188881 11671 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 409 12 4 4 4.3 CCCCCCCCc1ccc(-c2c[nH]c(C(C)(N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
134130111 141771 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 347 5 2 3 4.9 O=C(O)CNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3885275 141771 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 347 5 2 3 4.9 O=C(O)CNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1 10.1016/j.bmcl.2016.11.050
134131081 141606 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 361 6 2 3 5.3 O=C(O)CCNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883456 141606 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 361 6 2 3 5.3 O=C(O)CCNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1 10.1016/j.bmcl.2016.11.050
134130375 141670 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 339 7 2 3 4.8 Cc1ccc(-c2cccc3cc(CNCCCC(=O)O)sc23)cc1 10.1016/j.bmcl.2016.11.050
CHEMBL3884099 141670 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 339 7 2 3 4.8 Cc1ccc(-c2cccc3cc(CNCCCC(=O)O)sc23)cc1 10.1016/j.bmcl.2016.11.050
44398170 11667 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 411 12 4 4 4.2 CCCCCCCCc1ccc(-c2c[nH]c([C@@H](N)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1181688 11667 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 411 12 4 4 4.2 CCCCCCCCc1ccc(-c2c[nH]c([C@@H](N)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL188826 11667 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 411 12 4 4 4.2 CCCCCCCCc1ccc(-c2c[nH]c([C@@H](N)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
134130732 141662 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 393 7 2 3 5.5 O=C(O)CCCNCc1cc2cccc(-c3cccc(C(F)(F)F)c3)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3884056 141662 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 393 7 2 3 5.5 O=C(O)CCCNCc1cc2cccc(-c3cccc(C(F)(F)F)c3)c2s1 10.1016/j.bmcl.2016.11.050
134130546 141637 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 361 6 2 3 5.3 O=C(O)CCNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883812 141637 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 361 6 2 3 5.3 O=C(O)CCNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1 10.1016/j.bmcl.2016.11.050
134131256 141645 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 369 7 2 5 4.3 O=C(O)CCCNCc1cc2cccc(-c3ccc4c(c3)OCO4)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883947 141645 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 369 7 2 5 4.3 O=C(O)CCCNCc1cc2cccc(-c3ccc4c(c3)OCO4)c2s1 10.1016/j.bmcl.2016.11.050
134130150 141607 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 376 6 3 4 4.2 NC(CNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
CHEMBL3883471 141607 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 376 6 3 4 4.2 NC(CNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
124171444 136885 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
ChEMBL 435 7 1 7 4.0 Cc1cc(-c2nc(-c3cc(C)c(OC[C@@H]4CCC(=O)N4)c(C)n3)no2)cc(CC(C)C)n1 10.1016/j.bmcl.2015.11.090
CHEMBL3753300 136885 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
ChEMBL 435 7 1 7 4.0 Cc1cc(-c2nc(-c3cc(C)c(OC[C@@H]4CCC(=O)N4)c(C)n3)no2)cc(CC(C)C)n1 10.1016/j.bmcl.2015.11.090
124171442 136924 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
ChEMBL 422 6 2 8 3.3 Cc1cc(-c2nc(-c3ccc(O[C@H]4CCC(=O)NC4)c(C)n3)no2)cc(NC(C)C)n1 10.1016/j.bmcl.2015.11.090
CHEMBL3753609 136924 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
ChEMBL 422 6 2 8 3.3 Cc1cc(-c2nc(-c3ccc(O[C@H]4CCC(=O)NC4)c(C)n3)no2)cc(NC(C)C)n1 10.1016/j.bmcl.2015.11.090
134130316 141790 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 347 5 2 3 4.9 O=C(O)CNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3885468 141790 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 347 5 2 3 4.9 O=C(O)CNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1 10.1016/j.bmcl.2016.11.050
134131399 141783 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 339 7 2 3 4.8 Cc1ccccc1-c1cccc2cc(CNCCCC(=O)O)sc12 10.1016/j.bmcl.2016.11.050
CHEMBL3885401 141783 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 339 7 2 3 4.8 Cc1ccccc1-c1cccc2cc(CNCCCC(=O)O)sc12 10.1016/j.bmcl.2016.11.050
134130548 141657 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 6.7 O=C(O)c1ccc(CNCc2cc3c(-c4ccc5ccccc5c4)cccc3s2)cc1 10.1016/j.bmcl.2016.11.050
CHEMBL3884011 141657 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 6.7 O=C(O)c1ccc(CNCc2cc3c(-c4ccc5ccccc5c4)cccc3s2)cc1 10.1016/j.bmcl.2016.11.050
124171447 136906 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
ChEMBL 425 6 1 7 3.5 Cc1nc(CC(C)C)cc(-c2nc(-c3ccc(O[C@@H]4CCC(=O)NC4)c(F)c3)no2)n1 10.1016/j.bmcl.2015.11.090
CHEMBL3753479 136906 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor expressed in EDG8-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
ChEMBL 425 6 1 7 3.5 Cc1nc(CC(C)C)cc(-c2nc(-c3ccc(O[C@@H]4CCC(=O)NC4)c(F)c3)no2)n1 10.1016/j.bmcl.2015.11.090
44398058 11661 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 395 12 4 4 4.1 CCCCCCCCc1ccc(-c2c[nH]c([C@H](N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1181660 11661 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 395 12 4 4 4.1 CCCCCCCCc1ccc(-c2c[nH]c([C@H](N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL187712 11661 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 395 12 4 4 4.1 CCCCCCCCc1ccc(-c2c[nH]c([C@H](N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2005.05.097
124221654 1103 1 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 OC(=O)CCCNCc1cc2c(s1)c(ccc2)c1ccc2c(c1)cccc2 10.1016/j.bmcl.2016.11.050
9495 1103 1 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 OC(=O)CCCNCc1cc2c(s1)c(ccc2)c1ccc2c(c1)cccc2 10.1016/j.bmcl.2016.11.050
CHEMBL3884038 1103 1 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 OC(=O)CCCNCc1cc2c(s1)c(ccc2)c1ccc2c(c1)cccc2 10.1016/j.bmcl.2016.11.050
44394289 12303 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 383 11 4 4 3.7 CCCCCCCCc1ccc2[nH]c(C(C)(N)COP(=O)(O)O)nc2c1 10.1016/j.bmcl.2004.07.030
CHEMBL1185803 12303 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 383 11 4 4 3.7 CCCCCCCCc1ccc2[nH]c(C(C)(N)COP(=O)(O)O)nc2c1 10.1016/j.bmcl.2004.07.030
CHEMBL433593 12303 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 383 11 4 4 3.7 CCCCCCCCc1ccc2[nH]c(C(C)(N)COP(=O)(O)O)nc2c1 10.1016/j.bmcl.2004.07.030
44394521 11656 1 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 289 9 3 3 3.5 CCCCCCCCc1ccc2[nH]c([C@H](N)CO)nc2c1 10.1016/j.bmcl.2004.07.030
CHEMBL1181640 11656 1 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 289 9 3 3 3.5 CCCCCCCCc1ccc2[nH]c([C@H](N)CO)nc2c1 10.1016/j.bmcl.2004.07.030
CHEMBL186815 11656 1 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 289 9 3 3 3.5 CCCCCCCCc1ccc2[nH]c([C@H](N)CO)nc2c1 10.1016/j.bmcl.2004.07.030
134131209 141786 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 7 2 3 6.4 CCc1ccccc1-c1cccc2cc(CNc3cccc(CC(=O)O)c3)sc12 10.1016/j.bmcl.2016.11.050
CHEMBL3885415 141786 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 7 2 3 6.4 CCc1ccccc1-c1cccc2cc(CNc3cccc(CC(=O)O)c3)sc12 10.1016/j.bmcl.2016.11.050
2924 1610 37 None - 0 Human 7.4 pEC50 = 7.4 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1016/j.bmcl.2005.05.097
44398069 1610 37 None - 0 Human 7.4 pEC50 = 7.4 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1016/j.bmcl.2005.05.097
9908268 1610 37 None - 0 Human 7.4 pEC50 = 7.4 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1016/j.bmcl.2005.05.097
CHEMBL114606 1610 37 None - 0 Human 7.4 pEC50 = 7.4 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1016/j.bmcl.2005.05.097
134131067 141653 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 7.0 O=C(O)Cc1ccc(NCc2cc3cccc(-c4ccc5ccccc5c4)c3s2)cc1 10.1016/j.bmcl.2016.11.050
CHEMBL3883991 141653 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 7.0 O=C(O)Cc1ccc(NCc2cc3cccc(-c4ccc5ccccc5c4)c3s2)cc1 10.1016/j.bmcl.2016.11.050
10023913 12027 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 400 14 4 4 3.7 CCCCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL1184130 12027 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 400 14 4 4 3.7 CCCCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL334038 12027 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 400 14 4 4 3.7 CCCCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
67249162 115852 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 404 7 1 5 4.8 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C#N 10.1021/ml500422m
CHEMBL3359520 115852 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 404 7 1 5 4.8 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C#N 10.1021/ml500422m
134129983 141616 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 389 8 2 3 6.1 O=C(O)CCCCNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883555 141616 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 389 8 2 3 6.1 O=C(O)CCCCNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1 10.1016/j.bmcl.2016.11.050
134130146 141593 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 353 7 2 3 4.9 CCc1ccccc1-c1cccc2cc(CNCC(C)C(=O)O)sc12 10.1016/j.bmcl.2016.11.050
CHEMBL3883401 141593 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 353 7 2 3 4.9 CCc1ccccc1-c1cccc2cc(CNCC(C)C(=O)O)sc12 10.1016/j.bmcl.2016.11.050
44342219 11306 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 344 10 4 4 2.2 CCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL115344 11306 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 344 10 4 4 2.2 CCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL1180152 11306 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 344 10 4 4 2.2 CCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
10883396 3592 39 None - 4 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/s0960-894x(03)00812-6
5283560 3592 39 None - 4 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/s0960-894x(03)00812-6
911 3592 39 None - 4 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/s0960-894x(03)00812-6
CHEMBL225155 3592 39 None - 4 Human 7.4 pEC50 = 7.4 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/s0960-894x(03)00812-6
134130183 141636 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 6.7 O=C(O)c1ccc(CNCc2cc3cccc(-c4ccc5ccccc5c4)c3s2)cc1 10.1016/j.bmcl.2016.11.050
CHEMBL3883805 141636 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 6.7 O=C(O)c1ccc(CNCc2cc3cccc(-c4ccc5ccccc5c4)c3s2)cc1 10.1016/j.bmcl.2016.11.050
134131169 141731 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 381 7 2 3 5.8 CC(C)(C)c1ccc(-c2cccc3cc(CNCCCC(=O)O)sc23)cc1 10.1016/j.bmcl.2016.11.050
CHEMBL3884888 141731 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 381 7 2 3 5.8 CC(C)(C)c1ccc(-c2cccc3cc(CNCCCC(=O)O)sc23)cc1 10.1016/j.bmcl.2016.11.050
67250226 115854 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N 10.1021/ml500422m
CHEMBL3359522 115854 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 438 7 1 5 5.5 CC(C)Oc1ccc(COc2ccc3c(c2)c(Cl)c2n3CC[C@@H]2CC(=O)O)cc1C#N 10.1021/ml500422m
134131475 141655 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 7 2 3 6.4 CCc1ccccc1-c1cccc2sc(CNc3ccc(CC(=O)O)cc3)cc12 10.1016/j.bmcl.2016.11.050
CHEMBL3883998 141655 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 7 2 3 6.4 CCc1ccccc1-c1cccc2sc(CNc3ccc(CC(=O)O)cc3)cc12 10.1016/j.bmcl.2016.11.050
134130066 141721 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 8 2 3 6.2 O=C(O)CCCNCc1cc2cccc(-c3cccc(-c4ccccc4)c3)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3884809 141721 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 8 2 3 6.2 O=C(O)CCCNCc1cc2cccc(-c3cccc(-c4ccccc4)c3)c2s1 10.1016/j.bmcl.2016.11.050
49839234 117448 1 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21 10.1016/j.bmcl.2014.11.089
CHEMBL3403619 117448 1 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 472 6 3 3 6.1 O=C(O)CC1NCCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)cc21 10.1016/j.bmcl.2014.11.089
134131291 141619 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 373 4 1 3 5.2 O=C(O)C1CN(Cc2cc3cccc(-c4ccc5ccccc5c4)c3s2)C1 10.1016/j.bmcl.2016.11.050
CHEMBL3883579 141619 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 373 4 1 3 5.2 O=C(O)C1CN(Cc2cc3cccc(-c4ccc5ccccc5c4)c3s2)C1 10.1016/j.bmcl.2016.11.050
134130695 141604 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 347 5 2 3 4.9 O=C(O)CNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883447 141604 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 347 5 2 3 4.9 O=C(O)CNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1 10.1016/j.bmcl.2016.11.050
44398012 12158 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 425 12 4 4 4.4 CCCCCCCCc1ccc(-c2c[nH]c(C(C)(N)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1184707 12158 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 425 12 4 4 4.4 CCCCCCCCc1ccc(-c2c[nH]c(C(C)(N)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL364950 12158 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 425 12 4 4 4.4 CCCCCCCCc1ccc(-c2c[nH]c(C(C)(N)COP(O)(O)=S)n2)cc1 10.1016/j.bmcl.2005.05.097
44342175 85095 0 None - 2 Human 7.3 pEC50 = 7.3 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL227371 85095 0 None - 2 Human 7.3 pEC50 = 7.3 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL422074 85095 0 None - 2 Human 7.3 pEC50 = 7.3 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 372 12 4 4 3.0 CCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
44342339 11301 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 344 10 4 4 2.2 CCCCCCc1ccc(NC(=O)[C@@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL114031 11301 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 344 10 4 4 2.2 CCCCCCc1ccc(NC(=O)[C@@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
CHEMBL1180115 11301 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligandIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand
ChEMBL 344 10 4 4 2.2 CCCCCCc1ccc(NC(=O)[C@@H](N)COP(=O)(O)O)cc1 10.1016/s0960-894x(03)00812-6
134131363 141718 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 393 7 2 3 5.5 O=C(O)CCCNCc1cc2cccc(-c3ccc(C(F)(F)F)cc3)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3884795 141718 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 393 7 2 3 5.5 O=C(O)CCCNCc1cc2cccc(-c3ccc(C(F)(F)F)cc3)c2s1 10.1016/j.bmcl.2016.11.050
44394497 66361 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 497 11 4 6 4.3 CCCCCCCCc1ccc2[nH]c([C@@H](N)COP(=O)(O)O)nc2c1.COC(=O)C(F)(F)F 10.1016/j.bmcl.2004.07.030
CHEMBL185491 66361 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 497 11 4 6 4.3 CCCCCCCCc1ccc2[nH]c([C@@H](N)COP(=O)(O)O)nc2c1.COC(=O)C(F)(F)F 10.1016/j.bmcl.2004.07.030
134131381 141777 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 O=C(O)CCCNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3885331 141777 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 7 2 3 5.7 O=C(O)CCCNCc1cc2c(-c3ccc4ccccc4c3)cccc2s1 10.1016/j.bmcl.2016.11.050
44342221 11987 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand; Not determinedIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand; Not determined
ChEMBL 352 15 4 4 2.5 CCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
CHEMBL1183918 11987 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand; Not determinedIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand; Not determined
ChEMBL 352 15 4 4 2.5 CCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
CHEMBL324358 11987 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand; Not determinedIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand; Not determined
ChEMBL 352 15 4 4 2.5 CCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O 10.1016/s0960-894x(03)00812-6
134130947 141697 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 8 2 3 6.2 O=C(O)CCCNCc1cc2cccc(-c3ccc(-c4ccccc4)cc3)c2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3884580 141697 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 8 2 3 6.2 O=C(O)CCCNCc1cc2cccc(-c3ccc(-c4ccccc4)cc3)c2s1 10.1016/j.bmcl.2016.11.050
134131043 141746 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 7 2 3 6.1 CCc1ccccc1-c1cccc2sc(CNCc3ccc(C(=O)O)cc3)cc12 10.1016/j.bmcl.2016.11.050
CHEMBL3885068 141746 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 401 7 2 3 6.1 CCc1ccccc1-c1cccc2sc(CNCc3ccc(C(=O)O)cc3)cc12 10.1016/j.bmcl.2016.11.050
44398074 12777 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 345 11 4 4 3.1 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)CO)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1188885 12777 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 345 11 4 4 3.1 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)CO)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL537632 12777 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 345 11 4 4 3.1 CCCCCCCCc1ccc(-c2c[nH]c(C(N)(CO)CO)n2)cc1 10.1016/j.bmcl.2005.05.097
134131297 141625 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 389 8 2 3 6.1 O=C(O)CCCCNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1 10.1016/j.bmcl.2016.11.050
CHEMBL3883621 141625 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 389 8 2 3 6.1 O=C(O)CCCCNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1 10.1016/j.bmcl.2016.11.050
134130023 141679 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 376 6 3 4 4.2 NC(CNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
CHEMBL3884173 141679 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 376 6 3 4 4.2 NC(CNCc1cc2cc(-c3ccc4ccccc4c3)ccc2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
66829311 139279 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at S1PR5 (unknown origin)Agonist activity at S1PR5 (unknown origin)
ChEMBL 530 13 3 9 3.6 CCc1cc(-c2noc(-c3cc(C)c(CN(C)CC(C)C)s3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1016/j.ejmech.2016.03.048
CHEMBL3798837 139279 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at S1PR5 (unknown origin)Agonist activity at S1PR5 (unknown origin)
ChEMBL 530 13 3 9 3.6 CCc1cc(-c2noc(-c3cc(C)c(CN(C)CC(C)C)s3)n2)cc(C)c1OC[C@@H](O)CNC(=O)CO 10.1016/j.ejmech.2016.03.048
134131316 141667 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 7.0 O=C(O)Cc1cccc(NCc2cc3cc(-c4ccc5ccccc5c4)ccc3s2)c1 10.1016/j.bmcl.2016.11.050
CHEMBL3884077 141667 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 423 6 2 3 7.0 O=C(O)Cc1cccc(NCc2cc3cc(-c4ccc5ccccc5c4)ccc3s2)c1 10.1016/j.bmcl.2016.11.050
44394327 11647 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 383 11 4 4 4.0 CCCCCCCCc1ccc2[nH]c([C@@H](N)[C@@H](C)OP(=O)(O)O)nc2c1 10.1016/j.bmcl.2004.07.030
CHEMBL1181601 11647 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 383 11 4 4 4.0 CCCCCCCCc1ccc2[nH]c([C@@H](N)[C@@H](C)OP(=O)(O)O)nc2c1 10.1016/j.bmcl.2004.07.030
CHEMBL183894 11647 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 383 11 4 4 4.0 CCCCCCCCc1ccc2[nH]c([C@@H](N)[C@@H](C)OP(=O)(O)O)nc2c1 10.1016/j.bmcl.2004.07.030
44394459 123120 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 497 11 4 6 4.3 CCCCCCCCc1ccc2[nH]c([C@H](N)COP(=O)(O)O)nc2c1.COC(=O)C(F)(F)F 10.1016/j.bmcl.2004.07.030
CHEMBL361915 123120 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonistIn vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist
ChEMBL 497 11 4 6 4.3 CCCCCCCCc1ccc2[nH]c([C@H](N)COP(=O)(O)O)nc2c1.COC(=O)C(F)(F)F 10.1016/j.bmcl.2004.07.030
46174905 115788 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 457 6 1 3 6.9 O=C(O)CC1CCn2c1cc1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12 10.1021/ml500422m
CHEMBL3358955 115788 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 457 6 1 3 6.9 O=C(O)CC1CCn2c1cc1cc(OCc3ccc(C4CCCC4)c(C(F)(F)F)c3)ccc12 10.1021/ml500422m
44398172 11674 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 315 10 3 3 4.0 CCCCCCCCc1ccc(-c2c[nH]c([C@H](N)CO)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL1181739 11674 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 315 10 3 3 4.0 CCCCCCCCc1ccc(-c2c[nH]c([C@H](N)CO)n2)cc1 10.1016/j.bmcl.2005.05.097
CHEMBL190529 11674 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 315 10 3 3 4.0 CCCCCCCCc1ccc(-c2c[nH]c([C@H](N)CO)n2)cc1 10.1016/j.bmcl.2005.05.097
134130192 141672 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 6 2 3 5.5 CC(CNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
CHEMBL3884134 141672 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting methodAgonist activity at recombinant human S1PR5 expressed in CHO cell membranes assessed as [35S]GTP-gammaS binding measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 375 6 2 3 5.5 CC(CNCc1cc2cccc(-c3ccc4ccccc4c3)c2s1)C(=O)O 10.1016/j.bmcl.2016.11.050
10883396 3592 39 None - 4 Human 8.0 pEC50 = 8.0 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2005.05.097
5283560 3592 39 None - 4 Human 8.0 pEC50 = 8.0 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2005.05.097
911 3592 39 None - 4 Human 8.0 pEC50 = 8.0 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2005.05.097
CHEMBL225155 3592 39 None - 4 Human 8.0 pEC50 = 8.0 Binding
Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assayEffective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2005.05.097
10883396 3592 39 None - 4 Human 8.0 pEC50 = 8.0 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/s0960-894x(03)00812-6
5283560 3592 39 None - 4 Human 8.0 pEC50 = 8.0 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/s0960-894x(03)00812-6
911 3592 39 None - 4 Human 8.0 pEC50 = 8.0 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/s0960-894x(03)00812-6
CHEMBL225155 3592 39 None - 4 Human 8.0 pEC50 = 8.0 Binding
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/s0960-894x(03)00812-6
67249162 115852 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 404 7 1 5 4.8 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C#N 10.1021/ml500422m
CHEMBL3359520 115852 0 None - 0 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human S1P5 receptor by beta-arrestin recruitment assayAgonist activity at human S1P5 receptor by beta-arrestin recruitment assay
ChEMBL 404 7 1 5 4.8 CC(C)Oc1ccc(COc2ccc3c(c2)cc2n3CCC2CC(=O)O)cc1C#N 10.1021/ml500422m
11743459 140260 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 431 7 1 5 4.4 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(CCC(F)(F)F)cc4)n3)cc2)C1 10.1021/jm0503244
CHEMBL381872 140260 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 431 7 1 5 4.4 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(CCC(F)(F)F)cc4)n3)cc2)C1 10.1021/jm0503244
11575787 70288 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 439 6 1 5 4.8 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)C1 10.1021/jm0503244
CHEMBL195014 70288 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 439 6 1 5 4.8 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)C1 10.1021/jm0503244
11604577 71981 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 439 6 1 5 4.8 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc([C@H]5CCC(F)(F)C5)cc4)n3)cc2)C1 10.1021/jm0503244
CHEMBL198415 71981 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 439 6 1 5 4.8 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc([C@H]5CCC(F)(F)C5)cc4)n3)cc2)C1 10.1021/jm0503244
10408874 72145 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 403 6 1 5 4.6 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(C5CCCC5)cc4)n3)cc2)C1 10.1021/jm0503244
CHEMBL198976 72145 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 403 6 1 5 4.6 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(C5CCCC5)cc4)n3)cc2)C1 10.1021/jm0503244
10883396 3592 39 None - 4 Human 9.3 pIC50 = 9.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm0492507
5283560 3592 39 None - 4 Human 9.3 pIC50 = 9.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm0492507
911 3592 39 None - 4 Human 9.3 pIC50 = 9.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm0492507
CHEMBL225155 3592 39 None - 4 Human 9.3 pIC50 = 9.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1021/jm0492507
44394191 65977 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 381 12 3 2 5.3 CCCCCCCCCc1ccc(C2CCC(CCP(=O)(O)O)N2)cc1 10.1016/j.bmcl.2004.07.049
CHEMBL184879 65977 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 381 12 3 2 5.3 CCCCCCCCCc1ccc(C2CCC(CCP(=O)(O)O)N2)cc1 10.1016/j.bmcl.2004.07.049
44394191 65977 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 381 12 3 2 5.3 CCCCCCCCCc1ccc(C2CCC(CCP(=O)(O)O)N2)cc1 10.1016/j.bmcl.2004.07.049
CHEMBL184879 65977 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 381 12 3 2 5.3 CCCCCCCCCc1ccc(C2CCC(CCP(=O)(O)O)N2)cc1 10.1016/j.bmcl.2004.07.049
2924 1610 37 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/jm0492507
44398069 1610 37 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/jm0492507
9908268 1610 37 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/jm0492507
CHEMBL114606 1610 37 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 387 14 4 4 3.3 CCCCCCCCc1ccc(cc1)CCC(COP(=O)(O)O)(CO)N 10.1021/jm0492507
46905530 10195 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 389 14 5 6 2.6 CCCCCCCCc1ccc(CCC(N)(CO)CO[PH](O)(O)O)cc1 10.1016/j.bmcl.2004.07.049
CHEMBL1161691 10195 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 389 14 5 6 2.6 CCCCCCCCc1ccc(CCC(N)(CO)CO[PH](O)(O)O)cc1 10.1016/j.bmcl.2004.07.049
9979368 71362 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 417 6 1 5 5.0 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(C5CCCCC5)cc4)n3)cc2)C1 10.1021/jm0503244
CHEMBL196534 71362 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 417 6 1 5 5.0 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(C5CCCCC5)cc4)n3)cc2)C1 10.1021/jm0503244
10430549 1032 33 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 10.1021/jm0503244
2929 1032 33 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 10.1021/jm0503244
CHEMBL194419 1032 33 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 10.1021/jm0503244
10045980 69497 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 8 1 5 4.3 CCCCc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
CHEMBL193789 69497 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 8 1 5 4.3 CCCCc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
49830722 71410 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 379 6 1 3 4.1 Cc1cc(OCc2cccc(C(F)(F)F)c2)ccc1CN1CC(C(=O)O)C1 10.1021/acs.jmedchem.5b00928
CHEMBL1966501 71410 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 379 6 1 3 4.1 Cc1cc(OCc2cccc(C(F)(F)F)c2)ccc1CN1CC(C(=O)O)C1 10.1021/acs.jmedchem.5b00928
49830919 71647 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 363 6 1 2 4.0 O=C(O)C1CN(Cc2ccc(CCc3cccc(C(F)(F)F)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL1973936 71647 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 363 6 1 2 4.0 O=C(O)C1CN(Cc2ccc(CCc3cccc(C(F)(F)F)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
46872619 72157 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 379 6 1 3 4.4 Cc1cc(OCc2ccc(Cl)c(Cl)c2)ccc1CN1CC(C(=O)O)C1 10.1021/acs.jmedchem.5b00928
CHEMBL1990223 72157 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 379 6 1 3 4.4 Cc1cc(OCc2ccc(Cl)c(Cl)c2)ccc1CN1CC(C(=O)O)C1 10.1021/acs.jmedchem.5b00928
127037695 136052 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 333 12 1 3 4.3 CCCCCCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3739440 136052 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 333 12 1 3 4.3 CCCCCCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
59451793 136239 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 399 6 1 3 4.5 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)c(Cl)c2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3741092 136239 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 399 6 1 3 4.5 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)c(Cl)c2)C1 10.1021/acs.jmedchem.5b00928
10430549 1032 33 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 10.1016/j.bmcl.2006.03.090
2929 1032 33 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 10.1016/j.bmcl.2006.03.090
CHEMBL194419 1032 33 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 391 7 1 5 4.1 CC(Cc1ccc(cc1)c1onc(n1)c1ccc(cc1)CN1CC(C1)C(=O)O)C 10.1016/j.bmcl.2006.03.090
10883396 3592 39 None - 4 Human 9.0 pIC50 = 9.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2008.11.072
5283560 3592 39 None - 4 Human 9.0 pIC50 = 9.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2008.11.072
911 3592 39 None - 4 Human 9.0 pIC50 = 9.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2008.11.072
CHEMBL225155 3592 39 None - 4 Human 9.0 pIC50 = 9.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2008.11.072
44591266 178720 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 443 13 4 5 4.2 CCCCCCCCOc1ccc(-c2c[nH]c([C@@](C)(N)COP(=O)(O)O)n2)cc1F 10.1016/j.bmcl.2008.11.072
CHEMBL473269 178720 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 443 13 4 5 4.2 CCCCCCCCOc1ccc(-c2c[nH]c([C@@](C)(N)COP(=O)(O)O)n2)cc1F 10.1016/j.bmcl.2008.11.072
44394273 64247 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 395 12 3 2 5.6 CCCCCCCCCc1ccc(CN[C@H]2CCC[C@H](P(=O)(O)O)C2)cc1 10.1016/j.bmcl.2004.07.049
CHEMBL181597 64247 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 395 12 3 2 5.6 CCCCCCCCCc1ccc(CN[C@H]2CCC[C@H](P(=O)(O)O)C2)cc1 10.1016/j.bmcl.2004.07.049
44591265 179401 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 425 13 4 5 4.1 CCCCCCCCOc1ccc(-c2c[nH]c([C@@](C)(N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2008.11.072
CHEMBL474689 179401 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 425 13 4 5 4.1 CCCCCCCCOc1ccc(-c2c[nH]c([C@@](C)(N)COP(=O)(O)O)n2)cc1 10.1016/j.bmcl.2008.11.072
10317453 70075 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 377 7 1 5 3.9 CCCc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
CHEMBL194578 70075 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 377 7 1 5 3.9 CCCc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
10363915 134670 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 405 7 1 5 4.6 CCC(C)(C)c1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
CHEMBL372066 134670 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 405 7 1 5 4.6 CCC(C)(C)c1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
59451812 136366 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 331 6 1 3 3.4 O=C(O)C1CN(Cc2ccc(OCc3cccc(Cl)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3742245 136366 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 331 6 1 3 3.4 O=C(O)C1CN(Cc2ccc(OCc3cccc(Cl)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
59451770 136376 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 277 8 1 3 2.8 CCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3742304 136376 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 277 8 1 3 2.8 CCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
10127776 10950 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 465 15 3 4 4.9 CCCCCCCCOc1c(Br)cc(CNCCCP(=O)(O)O)cc1OC 10.1021/jm0492507
CHEMBL117723 10950 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 465 15 3 4 4.9 CCCCCCCCOc1c(Br)cc(CNCCCP(=O)(O)O)cc1OC 10.1021/jm0492507
11271470 137059 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 475 8 1 4 6.1 CCc1cc(CN2CC(C(=O)O)C2)ccc1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1 10.1021/jm0492507
CHEMBL375488 137059 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 475 8 1 4 6.1 CCc1cc(CN2CC(C(=O)O)C2)ccc1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1 10.1021/jm0492507
44412282 77893 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 405 7 2 5 4.9 CC(C)Cc1ccc(-c2nc(-c3ccc([C@@H]4CC[C@@H](CC(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
CHEMBL210785 77893 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 405 7 2 5 4.9 CC(C)Cc1ccc(-c2nc(-c3ccc([C@@H]4CC[C@@H](CC(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
11502026 71110 0 None - 0 Human 6.0 pIC50 = 6 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 5 1 5 4.2 CC(C)(C)c1ccc(-c2nnc(-c3ccc(CN4CC(C(=O)O)C4)cc3)o2)cc1 10.1021/jm0503244
CHEMBL196149 71110 0 None - 0 Human 6.0 pIC50 = 6 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 5 1 5 4.2 CC(C)(C)c1ccc(-c2nnc(-c3ccc(CN4CC(C(=O)O)C4)cc3)o2)cc1 10.1021/jm0503244
11683935 178761 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 456 9 4 5 3.7 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
CHEMBL473563 178761 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 456 9 4 5 3.7 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
59451878 136172 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 311 6 1 3 3.3 C[C@@H](Oc1ccc(CN2CC(C(=O)O)C2)cc1)c1ccccc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740494 136172 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 311 6 1 3 3.3 C[C@@H](Oc1ccc(CN2CC(C(=O)O)C2)cc1)c1ccccc1 10.1021/acs.jmedchem.5b00928
10251062 70293 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 411 6 1 5 4.6 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(-c5ccccc5)cc4)n3)cc2)C1 10.1021/jm0503244
CHEMBL195025 70293 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 411 6 1 5 4.6 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(-c5ccccc5)cc4)n3)cc2)C1 10.1021/jm0503244
44413349 77286 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 453 6 2 5 5.4 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL208838 77286 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 453 6 2 5 5.4 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
10149721 84673 4 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 317 11 1 2 4.5 CCCCCCCCCc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/jm0492507
CHEMBL224623 84673 4 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 317 11 1 2 4.5 CCCCCCCCCc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/jm0492507
44394220 66668 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 15 3 2 5.8 CCCCCCCCCCCCCCNC1CCCC(P(=O)(O)O)C1 10.1016/j.bmcl.2004.07.049
CHEMBL186921 66668 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 15 3 2 5.8 CCCCCCCCCCCCCCNC1CCCC(P(=O)(O)O)C1 10.1016/j.bmcl.2004.07.049
59451743 136254 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 361 7 1 4 3.4 COc1cc(CN2CC(C(=O)O)C2)ccc1OCc1ccccc1Cl 10.1021/acs.jmedchem.5b00928
CHEMBL3741222 136254 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 361 7 1 4 3.4 COc1cc(CN2CC(C(=O)O)C2)ccc1OCc1ccccc1Cl 10.1021/acs.jmedchem.5b00928
10249979 71302 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 393 7 1 6 3.7 CC(C)Oc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
CHEMBL196357 71302 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 393 7 1 6 3.7 CC(C)Oc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
11603220 134658 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 375 6 1 5 3.8 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(C5CC5)cc4)n3)cc2)C1 10.1021/jm0503244
CHEMBL371985 134658 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 375 6 1 5 3.8 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(C5CC5)cc4)n3)cc2)C1 10.1021/jm0503244
11408903 84702 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 475 7 1 4 6.1 Cc1cc(CN2CC(C(=O)O)C2)cc(C)c1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1 10.1021/jm0492507
CHEMBL224853 84702 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 475 7 1 4 6.1 Cc1cc(CN2CC(C(=O)O)C2)cc(C)c1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1 10.1021/jm0492507
44565738 189161 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 445 11 4 5 3.8 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCCCCc3ccccc3)cc2)c[nH]1 10.1016/j.bmcl.2009.02.073
CHEMBL515917 189161 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 445 11 4 5 3.8 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCCCCc3ccccc3)cc2)c[nH]1 10.1016/j.bmcl.2009.02.073
10195325 84696 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.9 O=C(O)C1CCN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1021/jm0492507
CHEMBL224799 84696 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.9 O=C(O)C1CCN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1021/jm0492507
46872748 136352 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 319 9 1 3 3.9 CCCCCCOc1ccc(CN2CCC[C@H](C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3742107 136352 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 319 9 1 3 3.9 CCCCCCOc1ccc(CN2CCC[C@H](C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
11540052 179985 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 470 10 4 5 3.7 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
CHEMBL475405 179985 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 470 10 4 5 3.7 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
59451751 136198 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 319 9 1 3 3.9 CCCCCCOc1ccc(CN2CCC[C@@H](C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740739 136198 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 319 9 1 3 3.9 CCCCCCOc1ccc(CN2CCC[C@@H](C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
44412221 76757 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 391 6 2 5 4.5 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4CC[C@@H](C(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
CHEMBL207580 76757 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 391 6 2 5 4.5 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4CC[C@@H](C(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
44412165 77408 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 453 6 2 5 5.6 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
CHEMBL209076 77408 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 453 6 2 5 5.6 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
10288527 84605 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.8 Cc1cc(CN2CC(C(=O)O)C2)ccc1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1 10.1021/jm0492507
CHEMBL224005 84605 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.8 Cc1cc(CN2CC(C(=O)O)C2)ccc1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1 10.1021/jm0492507
44344193 114414 5 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 335 17 3 2 4.8 CCCCCCCCCCCCCCNCCCP(=O)(O)O 10.1021/jm0492507
CHEMBL334213 114414 5 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 335 17 3 2 4.8 CCCCCCCCCCCCCCNCCCP(=O)(O)O 10.1021/jm0492507
44344193 114414 5 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 335 17 3 2 4.8 CCCCCCCCCCCCCCNCCCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
CHEMBL334213 114414 5 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 335 17 3 2 4.8 CCCCCCCCCCCCCCNCCCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
44413274 138182 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 447 6 2 4 5.7 O=C(O)C1CNC(c2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL377968 138182 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 447 6 2 4 5.7 O=C(O)C1CNC(c2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1016/j.bmcl.2006.03.090
44394220 66668 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 15 3 2 5.8 CCCCCCCCCCCCCCNC1CCCC(P(=O)(O)O)C1 10.1016/j.bmcl.2004.07.049
CHEMBL186921 66668 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 15 3 2 5.8 CCCCCCCCCCCCCCNC1CCCC(P(=O)(O)O)C1 10.1016/j.bmcl.2004.07.049
11503967 7939 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 482 10 4 5 3.9 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(C(=O)CCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2010.02.098
CHEMBL1090796 7939 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 482 10 4 5 3.9 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(C(=O)CCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2010.02.098
44413430 138240 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 405 7 2 5 4.7 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4C[C@@H](CC(=O)O)CN4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.090
CHEMBL378061 138240 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 405 7 2 5 4.7 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4C[C@@H](CC(=O)O)CN4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.090
4492589 30692 7 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of S1P5 receptorInhibition of S1P5 receptor
ChEMBL 359 3 1 2 6.1 Cc1cccc(C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 10.1016/j.bmcl.2011.04.097
CHEMBL1397874 30692 7 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of S1P5 receptorInhibition of S1P5 receptor
ChEMBL 359 3 1 2 6.1 Cc1cccc(C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 10.1016/j.bmcl.2011.04.097
11224984 8629 18 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation countingDisplacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation counting
ChEMBL 460 8 2 6 4.3 CCC/N=C1\S/C(=C\c2ccc(OC[C@@H](O)CO)c(Cl)c2)C(=O)N1c1ccccc1C 10.1021/jm100181s
CHEMBL1095833 8629 18 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation countingDisplacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation counting
ChEMBL 460 8 2 6 4.3 CCC/N=C1\S/C(=C\c2ccc(OC[C@@H](O)CO)c(Cl)c2)C(=O)N1c1ccccc1C 10.1021/jm100181s
59451867 136266 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 335 4 1 2 4.2 O=C(O)C1CN(Cc2ccc(-c3cc(Cl)cc(Cl)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3741338 136266 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 335 4 1 2 4.2 O=C(O)C1CN(Cc2ccc(-c3cc(Cl)cc(Cl)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
44412165 77408 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 453 6 2 5 5.6 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
CHEMBL209076 77408 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 453 6 2 5 5.6 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
44394212 66834 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 373 15 2 2 6.5 CCCCCCCCCCCCCC1CCCC(CCP(C)(=O)O)N1 10.1016/j.bmcl.2004.07.049
CHEMBL187692 66834 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 373 15 2 2 6.5 CCCCCCCCCCCCCC1CCCC(CCP(C)(=O)O)N1 10.1016/j.bmcl.2004.07.049
44412364 77749 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 453 6 2 5 5.6 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc([C@H]5CCC(F)(F)C5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
CHEMBL210257 77749 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 453 6 2 5 5.6 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc([C@H]5CCC(F)(F)C5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
46872874 136092 2 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 319 9 1 3 3.9 CCCCCCOc1ccc(CN2CCC(C(=O)O)CC2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3739759 136092 2 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 319 9 1 3 3.9 CCCCCCOc1ccc(CN2CCC(C(=O)O)CC2)cc1 10.1021/acs.jmedchem.5b00928
59451883 136312 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 295 6 1 2 3.0 O=C(O)C1CN(Cc2ccc(CCc3ccccc3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3741743 136312 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 295 6 1 2 3.0 O=C(O)C1CN(Cc2ccc(CCc3ccccc3)cc2)C1 10.1021/acs.jmedchem.5b00928
10174255 84793 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 485 6 1 6 5.7 O=C(O)C1CN(Cc2ccc(-c3noc(-c4cc(-c5ccccc5)c(C(F)(F)F)s4)n3)cc2)C1 10.1021/jm0492507
CHEMBL225575 84793 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 485 6 1 6 5.7 O=C(O)C1CN(Cc2ccc(-c3noc(-c4cc(-c5ccccc5)c(C(F)(F)F)s4)n3)cc2)C1 10.1021/jm0492507
44394279 66814 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 16 3 2 5.8 CCCCCCCCCCCCCC[C@H]1CC[C@H](CCP(=O)(O)O)N1 10.1016/j.bmcl.2004.07.049
CHEMBL187588 66814 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 16 3 2 5.8 CCCCCCCCCCCCCC[C@H]1CC[C@H](CCP(=O)(O)O)N1 10.1016/j.bmcl.2004.07.049
10217498 84662 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 481 7 1 4 6.2 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(Cl)c2)C1 10.1021/jm0492507
CHEMBL224571 84662 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 481 7 1 4 6.2 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(Cl)c2)C1 10.1021/jm0492507
44412232 165767 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 391 6 2 5 4.5 CC(C)Cc1ccc(-c2nc(-c3ccc([C@@H]4CC[C@@H](C(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
CHEMBL427221 165767 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 391 6 2 5 4.5 CC(C)Cc1ccc(-c2nc(-c3ccc([C@@H]4CC[C@@H](C(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
46885798 7949 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 561 10 4 5 5.7 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCCc3ccc(-c4ccccc4)cc3)c(C(F)(F)F)c2)c[nH]1 10.1016/j.bmcl.2010.02.098
CHEMBL1090829 7949 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 561 10 4 5 5.7 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCCc3ccc(-c4ccccc4)cc3)c(C(F)(F)F)c2)c[nH]1 10.1016/j.bmcl.2010.02.098
44412165 77408 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 453 6 2 5 5.6 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
CHEMBL209076 77408 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 453 6 2 5 5.6 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
49830724 72040 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 399 6 1 3 4.5 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)cc2Cl)C1 10.1021/acs.jmedchem.5b00928
CHEMBL1986265 72040 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 399 6 1 3 4.5 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)cc2Cl)C1 10.1021/acs.jmedchem.5b00928
49830723 72387 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 383 6 1 3 3.9 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)cc2F)C1 10.1021/acs.jmedchem.5b00928
CHEMBL1998478 72387 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 383 6 1 3 3.9 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)cc2F)C1 10.1021/acs.jmedchem.5b00928
59451819 136293 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 383 6 1 3 3.9 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)c(F)c2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3741572 136293 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 383 6 1 3 3.9 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)c(F)c2)C1 10.1021/acs.jmedchem.5b00928
10883396 3592 39 None - 4 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2010.02.098
5283560 3592 39 None - 4 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2010.02.098
911 3592 39 None - 4 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2010.02.098
CHEMBL225155 3592 39 None - 4 Human 8.7 pIC50 = 8.7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2010.02.098
10287034 65852 3 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 367 11 2 2 4.7 CCCCCCCCCc1ccc(CN2CCC(P(=O)(O)O)C2)cc1 10.1016/j.bmcl.2004.07.049
CHEMBL184349 65852 3 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 367 11 2 2 4.7 CCCCCCCCCc1ccc(CN2CCC(P(=O)(O)O)C2)cc1 10.1016/j.bmcl.2004.07.049
44565597 178707 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 436 12 4 5 3.2 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCCCc2ccccc2)cc1 10.1016/j.bmcl.2009.02.073
CHEMBL473156 178707 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 436 12 4 5 3.2 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCCCc2ccccc2)cc1 10.1016/j.bmcl.2009.02.073
11696807 125436 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 5 1 5 4.2 CC(C)(C)c1ccc(-c2noc(-c3ccc(CN4CC(C(=O)O)C4)cc3)n2)cc1 10.1021/jm0503244
CHEMBL364899 125436 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 5 1 5 4.2 CC(C)(C)c1ccc(-c2noc(-c3ccc(CN4CC(C(=O)O)C4)cc3)n2)cc1 10.1021/jm0503244
44412416 77827 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 431 6 2 5 5.7 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc(C5CCCCC5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
CHEMBL210520 77827 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 431 6 2 5 5.7 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc(C5CCCCC5)cc4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
44412233 77783 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 405 7 2 5 4.9 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4CC[C@@H](CC(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
CHEMBL210352 77783 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 405 7 2 5 4.9 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4CC[C@@H](CC(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
44565716 179163 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 493 10 4 5 4.6 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCCc3ccc(-c4ccccc4)cc3)cc2)c[nH]1 10.1016/j.bmcl.2009.02.073
CHEMBL474418 179163 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 493 10 4 5 4.6 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCCc3ccc(-c4ccccc4)cc3)cc2)c[nH]1 10.1016/j.bmcl.2009.02.073
44413365 77029 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 467 6 2 5 5.8 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc(C5CCC(F)(F)CC5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL208648 77029 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 467 6 2 5 5.8 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc(C5CCC(F)(F)CC5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
11168252 84660 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 515 7 1 4 6.5 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(C(F)(F)F)c2)C1 10.1021/jm0492507
CHEMBL224549 84660 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 515 7 1 4 6.5 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(C(F)(F)F)c2)C1 10.1021/jm0492507
107970 1609 76 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1021/jm0492507
2407 1609 76 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1021/jm0492507
4167 1609 76 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1021/jm0492507
CHEMBL314854 1609 76 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1021/jm0492507
DB08868 1609 76 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 307 12 3 3 3.2 CCCCCCCCc1ccc(cc1)CCC(CO)(CO)N 10.1021/jm0492507
59451797 136379 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 335 4 1 2 4.2 O=C(O)C1CN(Cc2ccc(-c3ccc(Cl)c(Cl)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3742345 136379 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 335 4 1 2 4.2 O=C(O)C1CN(Cc2ccc(-c3ccc(Cl)c(Cl)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
10127475 165476 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 447 7 1 4 5.5 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL425563 165476 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 447 7 1 4 5.5 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1016/j.bmcl.2006.03.090
10127475 165476 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 447 7 1 4 5.5 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1021/jm0492507
CHEMBL425563 165476 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 447 7 1 4 5.5 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1021/jm0492507
44394161 66690 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 389 16 2 2 6.1 CCCCCCCCCCCCCC1CCCCN1CCCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
CHEMBL187061 66690 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 389 16 2 2 6.1 CCCCCCCCCCCCCC1CCCCN1CCCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
44394116 66018 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 349 17 2 2 5.2 CCCCCCCCCCCCCCN(C)CCCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
CHEMBL185100 66018 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 349 17 2 2 5.2 CCCCCCCCCCCCCCN(C)CCCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
46872507 136144 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 311 6 1 3 3.3 CC(Oc1ccc(CN2CC(C(=O)O)C2)cc1)c1ccccc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740188 136144 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 311 6 1 3 3.3 CC(Oc1ccc(CN2CC(C(=O)O)C2)cc1)c1ccccc1 10.1021/acs.jmedchem.5b00928
59451779 136062 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 305 9 1 3 3.6 CCCCCCOc1ccc(CN2CC[C@@H](C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3739509 136062 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 305 9 1 3 3.6 CCCCCCOc1ccc(CN2CC[C@@H](C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
44565622 178760 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 428 11 4 5 3.6 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCCC2CCCCC2)cc1 10.1016/j.bmcl.2009.02.073
CHEMBL473562 178760 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 428 11 4 5 3.6 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCCC2CCCCC2)cc1 10.1016/j.bmcl.2009.02.073
44394211 66827 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 14 2 3 5.4 CCCCCCCCCCCCCCN1CCC(O)(P(C)(=O)O)CC1 10.1016/j.bmcl.2004.07.049
CHEMBL187645 66827 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 14 2 3 5.4 CCCCCCCCCCCCCCN1CCC(O)(P(C)(=O)O)CC1 10.1016/j.bmcl.2004.07.049
46872872 136119 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 333 9 1 3 4.2 CCCCCCOc1ccc(CN2CCC(C(=O)O)C(C)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3739964 136119 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 333 9 1 3 4.2 CCCCCCOc1ccc(CN2CCC(C(=O)O)C(C)C2)cc1 10.1021/acs.jmedchem.5b00928
10215259 84683 5 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 331 11 1 2 4.9 CCCCCCCCCc1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/jm0492507
CHEMBL224703 84683 5 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 331 11 1 2 4.9 CCCCCCCCCc1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/jm0492507
59451870 136136 2 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 277 7 1 3 2.6 CC(C)CCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740090 136136 2 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 277 7 1 3 2.6 CC(C)CCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
59451813 136164 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 295 5 1 2 3.4 CCc1ccc(-c2ccc(CN3CC(C(=O)O)C3)cc2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740359 136164 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 295 5 1 2 3.4 CCc1ccc(-c2ccc(CN3CC(C(=O)O)C3)cc2)cc1 10.1021/acs.jmedchem.5b00928
10883396 3592 39 None - 4 Human 8.5 pIC50 = 8.5 Binding
Displacement of [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counterDisplacement of [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counter
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1039/d1md00357g
5283560 3592 39 None - 4 Human 8.5 pIC50 = 8.5 Binding
Displacement of [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counterDisplacement of [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counter
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1039/d1md00357g
911 3592 39 None - 4 Human 8.5 pIC50 = 8.5 Binding
Displacement of [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counterDisplacement of [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counter
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1039/d1md00357g
CHEMBL225155 3592 39 None - 4 Human 8.5 pIC50 = 8.5 Binding
Displacement of [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counterDisplacement of [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counter
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1039/d1md00357g
10883396 3592 39 None - 4 Human 8.5 pIC50 = 8.5 Binding
Displacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting methodDisplacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2017.12.010
5283560 3592 39 None - 4 Human 8.5 pIC50 = 8.5 Binding
Displacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting methodDisplacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2017.12.010
911 3592 39 None - 4 Human 8.5 pIC50 = 8.5 Binding
Displacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting methodDisplacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2017.12.010
CHEMBL225155 3592 39 None - 4 Human 8.5 pIC50 = 8.5 Binding
Displacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting methodDisplacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method
ChEMBL 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10.1016/j.bmcl.2017.12.010
44591264 179399 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 420 13 4 5 3.3 CCCCCCCCOc1ccc(NC(=O)[C@@](C)(N)COP(=O)(O)O)c(F)c1 10.1016/j.bmcl.2008.11.072
CHEMBL474688 179399 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 420 13 4 5 3.3 CCCCCCCCOc1ccc(NC(=O)[C@@](C)(N)COP(=O)(O)O)c(F)c1 10.1016/j.bmcl.2008.11.072
44565739 178382 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 459 12 4 5 4.2 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCCCCCc3ccccc3)cc2)c[nH]1 10.1016/j.bmcl.2009.02.073
CHEMBL470511 178382 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 459 12 4 5 4.2 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCCCCCc3ccccc3)cc2)c[nH]1 10.1016/j.bmcl.2009.02.073
44412294 138120 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 419 8 2 5 5.3 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4CC[C@@H](CCC(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
CHEMBL377637 138120 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 419 8 2 5 5.3 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4CC[C@@H](CCC(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
44412353 165675 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 435 6 2 5 5.5 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc(C5CCCC5)c(F)c4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
CHEMBL426688 165675 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 435 6 2 5 5.5 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc(C5CCCC5)c(F)c4)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
11495139 138375 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 405 7 2 5 4.7 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4C[C@H](CC(=O)O)CN4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.090
CHEMBL378300 138375 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 405 7 2 5 4.7 CC(C)Cc1ccc(-c2nc(-c3ccc([C@H]4C[C@H](CC(=O)O)CN4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.090
54582607 62130 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of S1P5 receptorInhibition of S1P5 receptor
ChEMBL 375 3 2 3 5.8 Cc1cc(O)cc(C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 10.1016/j.bmcl.2011.04.097
CHEMBL1779895 62130 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of S1P5 receptorInhibition of S1P5 receptor
ChEMBL 375 3 2 3 5.8 Cc1cc(O)cc(C)c1NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1 10.1016/j.bmcl.2011.04.097
11752659 165591 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 515 7 1 4 6.8 O=C(O)C1CN(Cc2cc(Cl)c(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(Cl)c2)C1 10.1021/jm0492507
CHEMBL426191 165591 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 515 7 1 4 6.8 O=C(O)C1CN(Cc2cc(Cl)c(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(Cl)c2)C1 10.1021/jm0492507
44394153 65825 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 363 14 3 3 4.3 CCCCCCCCCCCCCCN1CCC(O)(P(=O)(O)O)C1 10.1016/j.bmcl.2004.07.049
CHEMBL184237 65825 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 363 14 3 3 4.3 CCCCCCCCCCCCCCN1CCC(O)(P(=O)(O)O)C1 10.1016/j.bmcl.2004.07.049
59451739 136202 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 311 6 1 3 3.1 Cc1ccccc1COc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740768 136202 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 311 6 1 3 3.1 Cc1ccccc1COc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
44413415 138161 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 461 7 2 4 6.1 O=C(O)CC1CNC(c2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL377855 138161 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 461 7 2 4 6.1 O=C(O)CC1CNC(c2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)cc2)C1 10.1016/j.bmcl.2006.03.090
11653967 70230 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 389 6 1 5 4.2 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(C5CCC5)cc4)n3)cc2)C1 10.1021/jm0503244
CHEMBL194898 70230 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 389 6 1 5 4.2 O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(C5CCC5)cc4)n3)cc2)C1 10.1021/jm0503244
49830828 71471 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 365 6 1 3 4.1 O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)cc3Cl)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL1968499 71471 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 365 6 1 3 4.1 O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)cc3Cl)cc2)C1 10.1021/acs.jmedchem.5b00928
49830725 71547 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 365 6 1 3 3.8 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL1971132 71547 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 365 6 1 3 3.8 O=C(O)C1CN(Cc2ccc(OCc3cccc(C(F)(F)F)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
44394149 123509 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 377 15 3 3 4.5 CCCCCCCCCCCCCCN1CCC(C(O)P(=O)(O)O)C1 10.1016/j.bmcl.2004.07.049
CHEMBL363008 123509 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 377 15 3 3 4.5 CCCCCCCCCCCCCCN1CCC(C(O)P(=O)(O)O)C1 10.1016/j.bmcl.2004.07.049
59451824 136350 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 335 4 1 2 3.9 O=C(O)C1CN(Cc2ccc(-c3cccc(C(F)(F)F)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3742100 136350 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 335 4 1 2 3.9 O=C(O)C1CN(Cc2ccc(-c3cccc(C(F)(F)F)c3)cc2)C1 10.1021/acs.jmedchem.5b00928
59451859 136315 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 315 6 1 3 2.9 O=C(O)C1CN(Cc2ccc(OCc3ccccc3)c(F)c2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3741775 136315 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 315 6 1 3 2.9 O=C(O)C1CN(Cc2ccc(OCc3ccccc3)c(F)c2)C1 10.1021/acs.jmedchem.5b00928
11248292 142974 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 465 7 1 4 5.7 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(F)c2)C1 10.1021/jm0492507
CHEMBL389880 142974 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 465 7 1 4 5.7 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(F)c2)C1 10.1021/jm0492507
44565596 188955 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 422 11 4 5 2.9 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCCc2ccccc2)cc1 10.1016/j.bmcl.2009.02.073
CHEMBL514302 188955 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 422 11 4 5 2.9 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCCc2ccccc2)cc1 10.1016/j.bmcl.2009.02.073
11540052 179985 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 470 10 4 5 3.7 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2010.02.098
CHEMBL475405 179985 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 470 10 4 5 3.7 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2010.02.098
11690779 189123 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 442 8 4 5 3.9 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(Oc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
CHEMBL515603 189123 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 442 8 4 5 3.9 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(Oc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
2926 3538 72 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 440 3 0 4 7.2 FC(c1sc(cc1c1ccccc1)c1onc(n1)c1cccc(c1)C(F)(F)F)(F)F 10.1021/jm0492507
4077460 3538 72 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 440 3 0 4 7.2 FC(c1sc(cc1c1ccccc1)c1onc(n1)c1cccc(c1)C(F)(F)F)(F)F 10.1021/jm0492507
CHEMBL224720 3538 72 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 440 3 0 4 7.2 FC(c1sc(cc1c1ccccc1)c1onc(n1)c1cccc(c1)C(F)(F)F)(F)F 10.1021/jm0492507
11501764 133876 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 379 7 1 6 3.3 CCOc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
CHEMBL371743 133876 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 379 7 1 6 3.3 CCOc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
127041987 136105 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 319 11 1 3 3.9 CCCCCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3739878 136105 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 319 11 1 3 3.9 CCCCCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
46872620 136137 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 383 6 1 3 4.2 O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)c(F)c2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3740093 136137 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 383 6 1 3 4.2 O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)c(F)c2)C1 10.1021/acs.jmedchem.5b00928
59451845 136232 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 410 7 1 5 4.0 O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)c([N+](=O)[O-])c2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3741022 136232 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 410 7 1 5 4.0 O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)c([N+](=O)[O-])c2)C1 10.1021/acs.jmedchem.5b00928
59451849 136262 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 383 6 1 3 4.2 O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)cc2F)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3741298 136262 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 383 6 1 3 4.2 O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)cc2F)C1 10.1021/acs.jmedchem.5b00928
44413349 77286 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 453 6 2 5 5.4 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL208838 77286 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 453 6 2 5 5.4 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc([C@@H]5CCC(F)(F)C5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
10249887 70584 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 5 1 5 4.2 CC(C)(C)c1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
CHEMBL195141 70584 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 391 5 1 5 4.2 CC(C)(C)c1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
44413482 165485 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 445 7 2 5 5.0 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc(CCC(F)(F)F)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL425602 165485 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 445 7 2 5 5.0 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc(CCC(F)(F)F)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
11466640 84666 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 525 7 1 4 6.3 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(Br)c2)C1 10.1021/jm0492507
CHEMBL224599 84666 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 525 7 1 4 6.3 O=C(O)C1CN(Cc2ccc(OCc3cc(-c4ccccc4)c(C(F)(F)F)s3)c(Br)c2)C1 10.1021/jm0492507
10312 1268 16 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of S1P5 receptorInhibition of S1P5 receptor
ChEMBL 388 4 2 3 5.6 NCc1cc(C)c(c(c1)C)NC(=O)c1ccc(o1)c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2011.04.097
53358422 1268 16 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of S1P5 receptorInhibition of S1P5 receptor
ChEMBL 388 4 2 3 5.6 NCc1cc(C)c(c(c1)C)NC(=O)c1ccc(o1)c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2011.04.097
CHEMBL1779732 1268 16 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of S1P5 receptorInhibition of S1P5 receptor
ChEMBL 388 4 2 3 5.6 NCc1cc(C)c(c(c1)C)NC(=O)c1ccc(o1)c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2011.04.097
44413447 138154 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 431 6 2 5 5.6 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc(C5CCCCC5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL377828 138154 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 431 6 2 5 5.6 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc(C5CCCCC5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
46872626 213 18 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
9496 213 18 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
CHEMBL3741589 213 18 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 365 6 1 3 4.1 OC(=O)C1CN(C1)Cc1ccc(cc1)OCc1ccc(c(c1)Cl)Cl 10.1021/acs.jmedchem.5b00928
46872622 72092 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 331 6 1 3 3.4 O=C(O)C1CN(Cc2ccc(OCc3ccccc3)cc2Cl)C1 10.1021/acs.jmedchem.5b00928
CHEMBL1987998 72092 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 331 6 1 3 3.4 O=C(O)C1CN(Cc2ccc(OCc3ccccc3)cc2Cl)C1 10.1021/acs.jmedchem.5b00928
10287034 65852 3 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 367 11 2 2 4.7 CCCCCCCCCc1ccc(CN2CCC(P(=O)(O)O)C2)cc1 10.1021/jm0492507
CHEMBL184349 65852 3 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 367 11 2 2 4.7 CCCCCCCCCc1ccc(CN2CCC(P(=O)(O)O)C2)cc1 10.1021/jm0492507
10409838 133661 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 419 10 1 5 5.0 CCCCCCc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
CHEMBL371670 133661 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 419 10 1 5 5.0 CCCCCCc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
10476387 126993 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 405 6 1 5 4.5 CC(C)(C)Cc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
CHEMBL366181 126993 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cellsConcentration required for displacement of [33P]-labeled S1P from human sphingosine 1-phosphate receptor 5 expressed in CHO cells
ChEMBL 405 6 1 5 4.5 CC(C)(C)Cc1ccc(-c2nc(-c3ccc(CN4CC(C(=O)O)C4)cc3)no2)cc1 10.1021/jm0503244
44591250 189162 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 420 13 4 5 3.3 CCCCCCCCOc1ccc(NC(=O)[C@@](C)(N)COP(=O)(O)O)cc1F 10.1016/j.bmcl.2008.11.072
CHEMBL515921 189162 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 420 13 4 5 3.3 CCCCCCCCOc1ccc(NC(=O)[C@@](C)(N)COP(=O)(O)O)cc1F 10.1016/j.bmcl.2008.11.072
44412428 77892 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 435 6 2 5 5.5 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc(C5CCCC5)cc4F)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
CHEMBL210782 77892 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 435 6 2 5 5.5 O=C(O)C[C@@H]1CC[C@H](c2ccc(-c3noc(-c4ccc(C5CCCC5)cc4F)n3)cc2)N1 10.1016/j.bmcl.2006.03.038
44394212 66834 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 373 15 2 2 6.5 CCCCCCCCCCCCCC1CCCC(CCP(C)(=O)O)N1 10.1016/j.bmcl.2004.07.049
CHEMBL187692 66834 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 373 15 2 2 6.5 CCCCCCCCCCCCCC1CCCC(CCP(C)(=O)O)N1 10.1016/j.bmcl.2004.07.049
44394169 66350 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 16 2 2 5.7 CCCCCCCCCCCCCCN1CCCC1CCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
CHEMBL185447 66350 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 375 16 2 2 5.7 CCCCCCCCCCCCCCN1CCCC1CCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
44413446 77947 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 417 6 2 5 5.2 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc(C5CCCC5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
CHEMBL211006 77947 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [33P]S1P from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]S1P from human S1P5 receptor expressed in CHO cells
ChEMBL 417 6 2 5 5.2 O=C(O)C[C@@H]1CN[C@@H](c2ccc(-c3noc(-c4ccc(C5CCCC5)cc4)n3)cc2)C1 10.1016/j.bmcl.2006.03.090
44394117 66009 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 389 17 2 2 6.1 CCCCCCCCCCCCCCC1CCCN1CCCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
CHEMBL185066 66009 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 389 17 2 2 6.1 CCCCCCCCCCCCCCC1CCCN1CCCP(=O)(O)O 10.1016/j.bmcl.2004.07.049
59451753 136384 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 281 4 1 2 3.2 Cc1ccc(-c2ccc(CN3CC(C(=O)O)C3)cc2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3742384 136384 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 281 4 1 2 3.2 Cc1ccc(-c2ccc(CN3CC(C(=O)O)C3)cc2)cc1 10.1021/acs.jmedchem.5b00928
44565714 178717 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 484 11 4 5 4.1 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
CHEMBL473238 178717 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 484 11 4 5 4.1 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
59451780 136279 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 305 9 1 3 3.6 CCCCCCOc1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3741459 136279 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 305 9 1 3 3.6 CCCCCCOc1ccc(CN2CCC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
59451832 136120 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 297 6 1 3 2.8 O=C(O)C1CN(Cc2ccc(OCc3ccccc3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3739977 136120 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 297 6 1 3 2.8 O=C(O)C1CN(Cc2ccc(OCc3ccccc3)cc2)C1 10.1021/acs.jmedchem.5b00928
10310952 84697 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 477 8 1 5 5.5 COc1cc(CN2CC(C(=O)O)C2)ccc1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1 10.1021/jm0492507
CHEMBL224800 84697 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cellsDisplacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
ChEMBL 477 8 1 5 5.5 COc1cc(CN2CC(C(=O)O)C2)ccc1OCc1cc(-c2ccccc2)c(C(F)(F)F)s1 10.1021/jm0492507
46872625 136147 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 317 5 1 3 3.6 O=C(O)C1CN(Cc2ccc(Oc3ccc(Cl)cc3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3740219 136147 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 317 5 1 3 3.6 O=C(O)C1CN(Cc2ccc(Oc3ccc(Cl)cc3)cc2)C1 10.1021/acs.jmedchem.5b00928
59451750 136341 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 311 6 1 3 3.1 Cc1cc(OCc2ccccc2)ccc1CN1CC(C(=O)O)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3742033 136341 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 311 6 1 3 3.1 Cc1cc(OCc2ccccc2)ccc1CN1CC(C(=O)O)C1 10.1021/acs.jmedchem.5b00928
11725751 12738 5 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 355 14 3 2 4.6 CCCCCCCCCc1ccc(CNCCCP(=O)(O)O)cc1 10.1016/j.bmcl.2004.07.049
CHEMBL118860 12738 5 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranesInhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
ChEMBL 355 14 3 2 4.6 CCCCCCCCCc1ccc(CNCCCP(=O)(O)O)cc1 10.1016/j.bmcl.2004.07.049
44591249 180054 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 402 13 4 5 3.2 CCCCCCCCOc1ccc(NC(=O)[C@@](C)(N)COP(=O)(O)O)cc1 10.1016/j.bmcl.2008.11.072
CHEMBL475495 180054 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 402 13 4 5 3.2 CCCCCCCCOc1ccc(NC(=O)[C@@](C)(N)COP(=O)(O)O)cc1 10.1016/j.bmcl.2008.11.072
44412415 77813 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 419 8 2 5 5.3 CC(C)Cc1ccc(-c2nc(-c3ccc([C@@H]4CC[C@@H](CCC(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
CHEMBL210468 77813 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]S1P from S1P5 expressed in CHO cellsDisplacement of [33P]S1P from S1P5 expressed in CHO cells
ChEMBL 419 8 2 5 5.3 CC(C)Cc1ccc(-c2nc(-c3ccc([C@@H]4CC[C@@H](CCC(=O)O)N4)cc3)no2)cc1 10.1016/j.bmcl.2006.03.038
46885796 8326 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 538 10 4 5 4.8 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)c(C(F)(F)F)c1 10.1016/j.bmcl.2010.02.098
CHEMBL1093429 8326 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 538 10 4 5 4.8 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)c(C(F)(F)F)c1 10.1016/j.bmcl.2010.02.098
68489165 136086 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 315 6 1 3 2.9 O=C(O)C1CN(Cc2ccc(OCc3ccc(F)cc3)cc2)C1 10.1021/acs.jmedchem.5b00928
CHEMBL3739695 136086 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 315 6 1 3 2.9 O=C(O)C1CN(Cc2ccc(OCc3ccc(F)cc3)cc2)C1 10.1021/acs.jmedchem.5b00928
59451764 136131 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 291 9 1 3 3.2 CCCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3740060 136131 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 291 9 1 3 3.2 CCCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
46872048 136270 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 395 7 1 4 4.1 COc1cc(CN2CC(C(=O)O)C2)ccc1OCc1ccc(Cl)cc1Cl 10.1021/acs.jmedchem.5b00928
CHEMBL3741364 136270 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 395 7 1 4 4.1 COc1cc(CN2CC(C(=O)O)C2)ccc1OCc1ccc(Cl)cc1Cl 10.1021/acs.jmedchem.5b00928
127037696 136284 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 305 10 1 3 3.6 CCCCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
CHEMBL3741496 136284 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB methodDisplacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
ChEMBL 305 10 1 3 3.6 CCCCCCCOc1ccc(CN2CC(C(=O)O)C2)cc1 10.1021/acs.jmedchem.5b00928
44565717 188939 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 479 9 4 5 4.6 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCc3ccc(-c4ccccc4)cc3)cc2)c[nH]1 10.1016/j.bmcl.2009.02.073
CHEMBL514170 188939 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 479 9 4 5 4.6 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCc3ccc(-c4ccccc4)cc3)cc2)c[nH]1 10.1016/j.bmcl.2009.02.073
25008420 8379 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 547 9 4 5 5.6 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCc3ccc(-c4ccccc4)cc3)c(C(F)(F)F)c2)c[nH]1 10.1016/j.bmcl.2010.02.098
CHEMBL1093823 8379 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 547 9 4 5 5.6 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCc3ccc(-c4ccccc4)cc3)c(C(F)(F)F)c2)c[nH]1 10.1016/j.bmcl.2010.02.098
44565717 188939 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 479 9 4 5 4.6 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCc3ccc(-c4ccccc4)cc3)cc2)c[nH]1 10.1016/j.bmcl.2010.02.098
CHEMBL514170 188939 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation countingDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
ChEMBL 479 9 4 5 4.6 C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCc3ccc(-c4ccccc4)cc3)cc2)c[nH]1 10.1016/j.bmcl.2010.02.098
44565715 179861 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 498 12 4 5 4.5 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
CHEMBL475253 179861 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptorDisplacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
ChEMBL 498 12 4 5 4.5 C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCCCc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.02.073
77846754 181960 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assayBinding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assay
ChEMBL 435 5 1 3 6.3 Cc1cc(OC2CCC3(CCCC3)CC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4787458 181960 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assayBinding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assay
ChEMBL 435 5 1 3 6.3 Cc1cc(OC2CCC3(CCCC3)CC2)c(CN2CCC(C(=O)O)CC2)c2ccccc12 10.1021/acsmedchemlett.0c00631
11502996 158181 36 None 1 4 Human 9.2 pKi = 9.2 Binding
Displacement of [33P]-S1P from human S1P5 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting methodDisplacement of [33P]-S1P from human S1P5 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting method
ChEMBL 435 9 1 4 5.0 CCCc1ccc(COc2ccc3c(c2)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1 10.1021/acs.jmedchem.7b00785
CHEMBL4093489 158181 36 None 1 4 Human 9.2 pKi = 9.2 Binding
Displacement of [33P]-S1P from human S1P5 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting methodDisplacement of [33P]-S1P from human S1P5 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting method
ChEMBL 435 9 1 4 5.0 CCCc1ccc(COc2ccc3c(c2)CCC(CN2CC(C(=O)O)C2)=C3C)c(OC)c1 10.1021/acs.jmedchem.7b00785
77847762 182841 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assayBinding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assay
ChEMBL 397 7 2 3 5.7 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNCCC(=O)O)c2ccccc12 10.1021/acsmedchemlett.0c00631
CHEMBL4798593 182841 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assayBinding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assay
ChEMBL 397 7 2 3 5.7 Cc1cc(O[C@H]2CC[C@H](C(C)(C)C)CC2)c(CNCCC(=O)O)c2ccccc12 10.1021/acsmedchemlett.0c00631
12573 980 1 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assayBinding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assay
ChEMBL 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 10.1021/acsmedchemlett.0c00631
77846592 980 1 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assayBinding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assay
ChEMBL 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 10.1021/acsmedchemlett.0c00631
CHEMBL4748198 980 1 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assayBinding affinity to recombinant human S1P5 receptor expressed in Chem-1 cell membrane by 33P-SIP binding assay
ChEMBL 437 5 1 3 6.4 C(C)(C)(C)[C@@H]1CC[C@H](CC1)OC2=C(C3=CC=CC=C3C(=C2)C)CN4CCC(CC4)C(=O)O 10.1021/acsmedchemlett.0c00631
11363176 3100 42 None - 0 Human 6.9 pIC50 = 6.9 Binding
In a radioligand binding assay using membranes from CHO cells expressing human S1P<sub>5</sub>In a radioligand binding assay using membranes from CHO cells expressing human S1P<sub>5</sub>
Guide to Pharmacology 460 8 2 6 4.3 CCCN=C1S/C(=C\c2ccc(c(c2)Cl)OC[C@@H](CO)O)/C(=O)N1c1ccccc1C 20446681
5446 3100 42 None - 0 Human 6.9 pIC50 = 6.9 Binding
In a radioligand binding assay using membranes from CHO cells expressing human S1P<sub>5</sub>In a radioligand binding assay using membranes from CHO cells expressing human S1P<sub>5</sub>
Guide to Pharmacology 460 8 2 6 4.3 CCCN=C1S/C(=C\c2ccc(c(c2)Cl)OC[C@@H](CO)O)/C(=O)N1c1ccccc1C 20446681
9320 3100 42 None - 0 Human 6.9 pIC50 = 6.9 Binding
In a radioligand binding assay using membranes from CHO cells expressing human S1P<sub>5</sub>In a radioligand binding assay using membranes from CHO cells expressing human S1P<sub>5</sub>
Guide to Pharmacology 460 8 2 6 4.3 CCCN=C1S/C(=C\c2ccc(c(c2)Cl)OC[C@@H](CO)O)/C(=O)N1c1ccccc1C 20446681
CHEMBL1096146 3100 42 None - 0 Human 6.9 pIC50 = 6.9 Binding
In a radioligand binding assay using membranes from CHO cells expressing human S1P<sub>5</sub>In a radioligand binding assay using membranes from CHO cells expressing human S1P<sub>5</sub>
Guide to Pharmacology 460 8 2 6 4.3 CCCN=C1S/C(=C\c2ccc(c(c2)Cl)OC[C@@H](CO)O)/C(=O)N1c1ccccc1C 20446681
6992 3946 0 None 7 5 Human 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 11 3 3 4.3 CCCCCCCCc1cccc(c1)C1CC(C1)(N)COP(=O)(O)O 21632869
73755254 3946 0 None 7 5 Human 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 11 3 3 4.3 CCCCCCCCc1cccc(c1)C1CC(C1)(N)COP(=O)(O)O 21632869
10883396 3592 39 None 1 4 Rat 8.7 pKd None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10799507
5283560 3592 39 None 1 4 Rat 8.7 pKd None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10799507
911 3592 39 None 1 4 Rat 8.7 pKd None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10799507
CHEMBL225155 3592 39 None 1 4 Rat 8.7 pKd None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 10799507