Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
1410 2242 45 None -2 8 Human 6.0 pEC50 = 6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
1412 2242 45 None -2 8 Human 6.0 pEC50 = 6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
179394 2242 45 None -2 8 Human 6.0 pEC50 = 6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
57689795 2242 45 None -2 8 Human 6.0 pEC50 = 6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
CHEMBL33567 2242 45 None -2 8 Human 6.0 pEC50 = 6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
1410 2242 45 None -5 8 Rat 6.0 pEC50 = 6 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
1412 2242 45 None -5 8 Rat 6.0 pEC50 = 6 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
179394 2242 45 None -5 8 Rat 6.0 pEC50 = 6 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
57689795 2242 45 None -5 8 Rat 6.0 pEC50 = 6 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
CHEMBL33567 2242 45 None -5 8 Rat 6.0 pEC50 = 6 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
2207 99403 54 None -194 4 Rat 6.0 pEC50 = 6 Functional
Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O 10.1016/S0960-894X(97)00068-1
CHEMBL285843 99403 54 None -194 4 Rat 6.0 pEC50 = 6 Functional
Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O 10.1016/S0960-894X(97)00068-1
10385210 12922 0 None -2 3 Rat 4.0 pEC50 = 4 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 309 5 3 6 0.0 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc([N+](=O)[O-])c2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1189910 12922 0 None -2 3 Rat 4.0 pEC50 = 4 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 309 5 3 6 0.0 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc([N+](=O)[O-])c2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL539760 12922 0 None -2 3 Rat 4.0 pEC50 = 4 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 309 5 3 6 0.0 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc([N+](=O)[O-])c2)C1 10.1016/s0960-894x(01)00329-8
137655963 158477 0 None -1 4 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)[C@@H](O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4096644 158477 0 None -1 4 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)[C@@H](O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
1443 1291 30 None -7 5 Rat 6.0 pEC50 = 6.0 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@@H](CCP(=O)(O)O)N nan
1550579 1291 30 None -7 5 Rat 6.0 pEC50 = 6.0 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@@H](CCP(=O)(O)O)N nan
CHEMBL1319383 1291 30 None -7 5 Rat 6.0 pEC50 = 6.0 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@@H](CCP(=O)(O)O)N nan
1408 263 28 None -3 7 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/jm901523t
6604820 263 28 None -3 7 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/jm901523t
CHEMBL285043 263 28 None -3 7 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/jm901523t
CHEMBL288635 263 28 None -3 7 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/jm901523t
137650519 156803 0 None 1 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)C(O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4077705 156803 0 None 1 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)C(O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
137645989 157152 0 None -1 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 364 8 5 8 0.4 COc1cc([C@@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
CHEMBL4081842 157152 0 None -1 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 364 8 5 8 0.4 COc1cc([C@@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
46197778 8134 0 None 1 5 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 237 6 4 4 -0.3 N[C@@H](CCP(=O)(O)/C=C/C(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1092243 8134 0 None 1 5 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 237 6 4 4 -0.3 N[C@@H](CCP(=O)(O)/C=C/C(=O)O)C(=O)O 10.1021/jm901523t
1408 263 28 None -2 7 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/acs.jmedchem.7b01438
6604820 263 28 None -2 7 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL285043 263 28 None -2 7 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL288635 263 28 None -2 7 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/acs.jmedchem.7b01438
57765622 155563 0 None -20 3 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4063142 155563 0 None -20 3 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
10176324 114329 1 None -151 4 Rat 5.9 pEC50 = 5.9 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 173 3 3 3 -0.6 C[C@H]1[C@H](C(=O)O)[C@H]1[C@H](N)C(=O)O 10.1021/jm030967o
CHEMBL334160 114329 1 None -151 4 Rat 5.9 pEC50 = 5.9 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 173 3 3 3 -0.6 C[C@H]1[C@H](C(=O)O)[C@H]1[C@H](N)C(=O)O 10.1021/jm030967o
44406220 71829 1 None -1 2 Rat 4.9 pEC50 = 4.9 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 195 3 4 3 -1.0 N[C@H](C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O 10.1016/j.bmcl.2005.09.014
CHEMBL197976 71829 1 None -1 2 Rat 4.9 pEC50 = 4.9 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 195 3 4 3 -1.0 N[C@H](C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O 10.1016/j.bmcl.2005.09.014
11708219 168806 0 None -1 2 Rat 4.9 pEC50 = 4.9 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 195 3 4 3 -1.0 NC(C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O 10.1016/j.bmc.2007.02.040
CHEMBL442076 168806 0 None -1 2 Rat 4.9 pEC50 = 4.9 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 195 3 4 3 -1.0 NC(C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O 10.1016/j.bmc.2007.02.040
122197960 160364 0 None -12 2 Rat 4.9 pEC50 = 4.9 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 331 9 4 5 0.7 N[C@H](CCP(=O)(O)Cc1ccc(OCC(=O)O)cc1)C(=O)O nan
CHEMBL4115286 160364 0 None -12 2 Rat 4.9 pEC50 = 4.9 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 331 9 4 5 0.7 N[C@H](CCP(=O)(O)Cc1ccc(OCC(=O)O)cc1)C(=O)O nan
44361401 31126 0 None -33 5 Rat 6.8 pEC50 = 6.8 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 175 3 4 4 -1.9 N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O 10.1021/jm030967o
CHEMBL140197 31126 0 None -33 5 Rat 6.8 pEC50 = 6.8 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 175 3 4 4 -1.9 N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O 10.1021/jm030967o
46898088 2334 4 None -11 8 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
6739 2334 4 None -11 8 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
CHEMBL3114672 2334 4 None -11 8 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
127030386 138512 0 None -7 3 Rat 4.8 pEC50 = 4.8 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 217 5 4 4 -1.0 N[C@@H](C[C@@]1(C(=O)O)C[C@@H]1C(=O)O)C(=O)O 10.1021/acs.jmedchem.5b01333
CHEMBL3786026 138512 0 None -7 3 Rat 4.8 pEC50 = 4.8 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 217 5 4 4 -1.0 N[C@@H](C[C@@]1(C(=O)O)C[C@@H]1C(=O)O)C(=O)O 10.1021/acs.jmedchem.5b01333
57765535 157262 0 None -5 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 352 7 4 6 1.3 N[C@@H](CCP(=O)(O)C(O)c1ccc(Cl)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4083240 157262 0 None -5 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 352 7 4 6 1.3 N[C@@H](CCP(=O)(O)C(O)c1ccc(Cl)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
1408 263 28 None -3 7 Rat 4.7 pEC50 = 4.7 Functional
Activity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cells
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2006.06.062
6604820 263 28 None -3 7 Rat 4.7 pEC50 = 4.7 Functional
Activity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cells
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2006.06.062
CHEMBL285043 263 28 None -3 7 Rat 4.7 pEC50 = 4.7 Functional
Activity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cells
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2006.06.062
CHEMBL288635 263 28 None -3 7 Rat 4.7 pEC50 = 4.7 Functional
Activity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cells
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2006.06.062
122197942 159520 0 None -34 4 Rat 4.7 pEC50 = 4.7 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 375 9 5 6 0.8 Cc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(C)c1OCC(=O)O nan
CHEMBL4108384 159520 0 None -34 4 Rat 4.7 pEC50 = 4.7 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 375 9 5 6 0.8 Cc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(C)c1OCC(=O)O nan
1410 2242 45 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.5b01333
1412 2242 45 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.5b01333
179394 2242 45 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.5b01333
57689795 2242 45 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.5b01333
CHEMBL33567 2242 45 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.5b01333
60096231 157113 11 None -831 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human mGlu6 receptor expressed in hamster AV12 cells co-expressing rat EAAT1 assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu6 receptor expressed in hamster AV12 cells co-expressing rat EAAT1 assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 334 5 4 5 -0.1 COc1cccc(C(=O)N[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)c1 10.1021/acs.jmedchem.7b01481
CHEMBL4081453 157113 11 None -831 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human mGlu6 receptor expressed in hamster AV12 cells co-expressing rat EAAT1 assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu6 receptor expressed in hamster AV12 cells co-expressing rat EAAT1 assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 334 5 4 5 -0.1 COc1cccc(C(=O)N[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)c1 10.1021/acs.jmedchem.7b01481
16747847 85415 1 None -64 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at mGlu6 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu6 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 195 3 4 3 -1.0 N[C@@]1(C(=O)O)C[C@H]1CP(=O)(O)O 10.1021/jm070262c
CHEMBL229697 85415 1 None -64 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at mGlu6 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu6 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 195 3 4 3 -1.0 N[C@@]1(C(=O)O)C[C@H]1CP(=O)(O)O 10.1021/jm070262c
1310 2286 108 None -354 17 Human 4.7 pEC50 = 4.7 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
1369 2286 108 None -354 17 Human 4.7 pEC50 = 4.7 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
33032 2286 108 None -354 17 Human 4.7 pEC50 = 4.7 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
44272391 2286 108 None -354 17 Human 4.7 pEC50 = 4.7 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
88747398 2286 108 None -354 17 Human 4.7 pEC50 = 4.7 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
CHEMBL575060 2286 108 None -354 17 Human 4.7 pEC50 = 4.7 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
DB00142 2286 108 None -354 17 Human 4.7 pEC50 = 4.7 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
1436 31 7 None - 1 Rat 4.7 pEC50 = 4.7 Functional
Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6
ChEMBL 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
15508178 31 7 None - 1 Rat 4.7 pEC50 = 4.7 Functional
Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6
ChEMBL 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
CHEMBL60238 31 7 None - 1 Rat 4.7 pEC50 = 4.7 Functional
Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6
ChEMBL 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
1410 2242 45 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070400y
1412 2242 45 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070400y
179394 2242 45 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070400y
57689795 2242 45 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070400y
CHEMBL33567 2242 45 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070400y
10091203 12842 0 None -1 3 Rat 4.7 pEC50 = 4.7 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(C(C(=O)O)c2ccccc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1189303 12842 0 None -1 3 Rat 4.7 pEC50 = 4.7 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(C(C(=O)O)c2ccccc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL538489 12842 0 None -1 3 Rat 4.7 pEC50 = 4.7 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(C(C(=O)O)c2ccccc2)C1 10.1016/s0960-894x(01)00329-8
137644345 157573 0 None -3 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 303 7 4 5 0.8 COc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1 10.1021/acs.jmedchem.7b01438
CHEMBL4086929 157573 0 None -3 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 303 7 4 5 0.8 COc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1 10.1021/acs.jmedchem.7b01438
1410 2242 45 None -2 8 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
1412 2242 45 None -2 8 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
179394 2242 45 None -2 8 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
57689795 2242 45 None -2 8 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
CHEMBL33567 2242 45 None -2 8 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
137640190 156412 0 None -2 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)[C@H](O)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4072781 156412 0 None -2 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)[C@H](O)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
124425164 157471 0 None 1 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 364 8 5 8 0.4 COc1cc([C@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
CHEMBL4085558 157471 0 None 1 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 364 8 5 8 0.4 COc1cc([C@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
10198133 204782 10 None -630 4 Human 5.6 pEC50 = 5.6 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm980616n
CHEMBL8839 204782 10 None -630 4 Human 5.6 pEC50 = 5.6 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm980616n
122197958 159977 0 None -7 4 Rat 5.6 pEC50 = 5.6 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 383 9 5 6 0.5 N[C@H](CCP(=O)(O)C(O)c1cc(F)c(OCC(=O)O)c(F)c1)C(=O)O nan
CHEMBL4112299 159977 0 None -7 4 Rat 5.6 pEC50 = 5.6 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 383 9 5 6 0.5 N[C@H](CCP(=O)(O)C(O)c1cc(F)c(OCC(=O)O)c(F)c1)C(=O)O nan
57765613 157944 0 None -19 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 336 7 4 6 0.8 N[C@@H](CCP(=O)(O)C(O)c1ccc(F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4091029 157944 0 None -19 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 336 7 4 6 0.8 N[C@@H](CCP(=O)(O)C(O)c1ccc(F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
58058356 158248 0 None -5 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 350 7 6 8 0.1 N[C@@H](CCP(=O)(O)C(O)c1cc(O)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4094241 158248 0 None -5 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 350 7 6 8 0.1 N[C@@H](CCP(=O)(O)C(O)c1cc(O)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
6330803 91690 9 None -15 3 Rat 4.6 pEC50 = 4.6 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 167 4 3 3 -0.7 N[C@@H](CC[PH](=O)O)C(=O)O 10.1021/jm070400y
CHEMBL241972 91690 9 None -15 3 Rat 4.6 pEC50 = 4.6 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 167 4 3 3 -0.7 N[C@@H](CC[PH](=O)O)C(=O)O 10.1021/jm070400y
57765616 156876 0 None -7 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])c(C(F)(F)F)c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4078629 156876 0 None -7 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])c(C(F)(F)F)c1)C(=O)O 10.1021/acs.jmedchem.7b01438
1393 1510 58 None -346 6 Human 5.5 pEC50 = 5.5 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
1396 1510 58 None -346 6 Human 5.5 pEC50 = 5.5 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
213056 1510 58 None -346 6 Human 5.5 pEC50 = 5.5 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
CHEMBL8759 1510 58 None -346 6 Human 5.5 pEC50 = 5.5 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
24780225 155392 0 None -5 3 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 363 6 4 4 1.4 N[C@@H](CCP(=O)(O)C(O)c1c(F)c(F)c(F)c(F)c1F)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4061016 155392 0 None -5 3 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 363 6 4 4 1.4 N[C@@H](CCP(=O)(O)C(O)c1c(F)c(F)c(F)c(F)c1F)C(=O)O 10.1021/acs.jmedchem.7b01438
6348408 7738 1 None -2 8 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL1089515 7738 1 None -2 8 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
24780088 158363 0 None -3 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 317 7 5 5 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(=O)O)cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4095462 158363 0 None -3 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 317 7 5 5 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(=O)O)cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
6348408 7738 1 None -2 8 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1089515 7738 1 None -2 8 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
1407 2048 34 None -114 7 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
16062593 2048 34 None -114 7 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL143210 2048 34 None -114 7 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
46898088 2334 4 None -11 8 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
6739 2334 4 None -11 8 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
CHEMBL3114672 2334 4 None -11 8 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
58058372 155656 0 None -5 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 302 7 3 5 1.2 N[C@@H](CCP(=O)(O)Cc1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4064187 155656 0 None -5 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 302 7 3 5 1.2 N[C@@H](CCP(=O)(O)Cc1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
137642874 157490 0 None -10 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)[C@@H](O)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4085750 157490 0 None -10 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)[C@@H](O)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
3756397 8230 2 None -4 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 NC(CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
4041087 8230 2 None -4 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 NC(CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1092727 8230 2 None -4 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 NC(CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
1410 2242 45 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
1412 2242 45 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
179394 2242 45 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
57689795 2242 45 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
CHEMBL33567 2242 45 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
1410 2242 45 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
1412 2242 45 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
179394 2242 45 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
57689795 2242 45 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
CHEMBL33567 2242 45 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
1410 2242 45 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
1412 2242 45 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
179394 2242 45 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
57689795 2242 45 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
CHEMBL33567 2242 45 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
16747848 85090 0 None -1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu6 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 195 3 4 3 -1.0 N[C@@]1(C(=O)O)C[C@@H]1CP(=O)(O)O 10.1021/jm070262c
CHEMBL227288 85090 0 None -1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu6 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 195 3 4 3 -1.0 N[C@@]1(C(=O)O)C[C@@H]1CP(=O)(O)O 10.1021/jm070262c
53240406 122880 13 None -158 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant mGlu6 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu6 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616847 122880 13 None -158 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant mGlu6 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu6 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
1410 2242 45 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2015.04.043
1412 2242 45 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2015.04.043
179394 2242 45 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2015.04.043
57689795 2242 45 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2015.04.043
CHEMBL33567 2242 45 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2015.04.043
92044496 155426 0 None -20 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1csc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4061423 155426 0 None -20 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1csc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
137639752 156373 0 None -7 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)[C@H](O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4072316 156373 0 None -7 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)[C@H](O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
1407 2048 34 None -117 7 Rat 5.4 pEC50 = 5.4 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
16062593 2048 34 None -117 7 Rat 5.4 pEC50 = 5.4 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
CHEMBL143210 2048 34 None -117 7 Rat 5.4 pEC50 = 5.4 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
122197943 160033 0 None -7 3 Rat 5.4 pEC50 = 5.4 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 343 8 5 5 0.8 N[C@H](CCP(=O)(O)C(O)c1ccc(/C=C/C(=O)O)cc1)C(=O)O nan
CHEMBL4112699 160033 0 None -7 3 Rat 5.4 pEC50 = 5.4 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 343 8 5 5 0.8 N[C@H](CCP(=O)(O)C(O)c1ccc(/C=C/C(=O)O)cc1)C(=O)O nan
137647077 157453 0 None -2 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 348 8 4 7 0.7 COc1ccc([C@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
CHEMBL4085327 157453 0 None -2 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 348 8 4 7 0.7 COc1ccc([C@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
57765613 157944 0 None -19 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 336 7 4 6 0.8 N[C@@H](CCP(=O)(O)C(O)c1ccc(F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4091029 157944 0 None -19 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 336 7 4 6 0.8 N[C@@H](CCP(=O)(O)C(O)c1ccc(F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
57765525 158907 0 None -1 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 332 7 4 6 1.0 Cc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
CHEMBL4101241 158907 0 None -1 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 332 7 4 6 1.0 Cc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
1377 1313 19 None -60 8 Rat 4.4 pEC50 = 4.4 Functional
Metabotropic glutamate receptor 6 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
5310979 1313 19 None -60 8 Rat 4.4 pEC50 = 4.4 Functional
Metabotropic glutamate receptor 6 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
CHEMBL284193 1313 19 None -60 8 Rat 4.4 pEC50 = 4.4 Functional
Metabotropic glutamate receptor 6 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
10197984 2388 37 None -147 5 Human 6.4 pEC50 = 6.4 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
1394 2388 37 None -147 5 Human 6.4 pEC50 = 6.4 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
CHEMBL275079 2388 37 None -147 5 Human 6.4 pEC50 = 6.4 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
6706 2335 4 None -38 8 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
71041983 2335 4 None -38 8 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
CHEMBL3114673 2335 4 None -38 8 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
57765633 157866 0 None -8 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])s1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4090179 157866 0 None -8 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])s1)C(=O)O 10.1021/acs.jmedchem.7b01438
6706 2335 4 None -38 8 Rat 5.4 pEC50 = 5.4 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O nan
71041983 2335 4 None -38 8 Rat 5.4 pEC50 = 5.4 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O nan
CHEMBL3114673 2335 4 None -38 8 Rat 5.4 pEC50 = 5.4 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O nan
24779945 8157 0 None -12 3 Rat 4.4 pEC50 = 4.4 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 297 9 5 5 -0.8 N[C@@H](CCP(=O)(O)CC(CC(=O)O)C(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1092315 8157 0 None -12 3 Rat 4.4 pEC50 = 4.4 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 297 9 5 5 -0.8 N[C@@H](CCP(=O)(O)CC(CC(=O)O)C(=O)O)C(=O)O 10.1021/jm901523t
46197776 8271 0 None -4 3 Rat 4.4 pEC50 = 4.4 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 253 8 4 4 -0.1 N[C@@H](CCP(=O)(O)CCCC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1093009 8271 0 None -4 3 Rat 4.4 pEC50 = 4.4 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 253 8 4 4 -0.1 N[C@@H](CCP(=O)(O)CCCC(=O)O)C(=O)O 10.1021/jm901523t
137634883 155609 0 None -2 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 348 8 4 7 0.7 COc1ccc([C@@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
CHEMBL4063720 155609 0 None -2 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 348 8 4 7 0.7 COc1ccc([C@@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
57765536 157726 0 None -9 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4088782 157726 0 None -9 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
44406221 72331 1 None 1 2 Rat 4.3 pEC50 = 4.3 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 195 3 4 3 -1.0 N[C@H](C(=O)O)[C@@H]1C[C@H]1P(=O)(O)O 10.1016/j.bmcl.2005.09.014
CHEMBL199626 72331 1 None 1 2 Rat 4.3 pEC50 = 4.3 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 195 3 4 3 -1.0 N[C@H](C(=O)O)[C@@H]1C[C@H]1P(=O)(O)O 10.1016/j.bmcl.2005.09.014
1406 2042 32 None -23 7 Rat 5.3 pEC50 = 5.3 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm030967o
4545574 2042 32 None -23 7 Rat 5.3 pEC50 = 5.3 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm030967o
CHEMBL277475 2042 32 None -23 7 Rat 5.3 pEC50 = 5.3 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm030967o
122197935 159305 0 None -46 4 Rat 5.3 pEC50 = 5.3 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 377 10 5 7 0.2 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)ccc1OCC(=O)O nan
CHEMBL4106637 159305 0 None -46 4 Rat 5.3 pEC50 = 5.3 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 377 10 5 7 0.2 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)ccc1OCC(=O)O nan
127030387 138576 0 None -3 3 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 217 5 4 4 -1.0 N[C@@H](C[C@]1(C(=O)O)C[C@H]1C(=O)O)C(=O)O 10.1021/acs.jmedchem.5b01333
CHEMBL3786667 138576 0 None -3 3 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 217 5 4 4 -1.0 N[C@@H](C[C@]1(C(=O)O)C[C@H]1C(=O)O)C(=O)O 10.1021/acs.jmedchem.5b01333
16739372 146197 0 None 1 2 Rat 4.3 pEC50 = 4.3 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 271 4 4 3 0.4 NC(C(=O)O)[C@@H]1[C@@H](P(=O)(O)O)[C@H]1c1ccccc1 10.1016/j.bmc.2007.02.040
CHEMBL392420 146197 0 None 1 2 Rat 4.3 pEC50 = 4.3 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 271 4 4 3 0.4 NC(C(=O)O)[C@@H]1[C@@H](P(=O)(O)O)[C@H]1c1ccccc1 10.1016/j.bmc.2007.02.040
122197945 159682 0 None -4 3 Rat 4.3 pEC50 = 4.3 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 333 9 5 6 0.1 N[C@H](CCP(=O)(O)C(O)c1ccc(OCCO)cc1)C(=O)O nan
CHEMBL4109799 159682 0 None -4 3 Rat 4.3 pEC50 = 4.3 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 333 9 5 6 0.1 N[C@H](CCP(=O)(O)C(O)c1ccc(OCCO)cc1)C(=O)O nan
1410 2242 45 None -5 8 Rat 7.3 pEC50 = 7.3 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm030967o
1412 2242 45 None -5 8 Rat 7.3 pEC50 = 7.3 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm030967o
179394 2242 45 None -5 8 Rat 7.3 pEC50 = 7.3 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm030967o
57689795 2242 45 None -5 8 Rat 7.3 pEC50 = 7.3 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm030967o
CHEMBL33567 2242 45 None -5 8 Rat 7.3 pEC50 = 7.3 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm030967o
57765622 155563 0 None -20 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4063142 155563 0 None -20 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
44300256 13612 0 None - 1 Rat 4.2 pEC50 = 4.2 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc(C(=O)O)c2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1195052 13612 0 None - 1 Rat 4.2 pEC50 = 4.2 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc(C(=O)O)c2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL553774 13612 0 None - 1 Rat 4.2 pEC50 = 4.2 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc(C(=O)O)c2)C1 10.1016/s0960-894x(01)00329-8
44300587 12923 0 None -12 2 Rat 4.2 pEC50 = 4.2 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccc(C(=O)O)cc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1189911 12923 0 None -12 2 Rat 4.2 pEC50 = 4.2 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccc(C(=O)O)cc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL539761 12923 0 None -12 2 Rat 4.2 pEC50 = 4.2 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccc(C(=O)O)cc2)C1 10.1016/s0960-894x(01)00329-8
122197937 159761 0 None -21 3 Rat 5.2 pEC50 = 5.2 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 422 11 5 9 0.1 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc([N+](=O)[O-])c1OCC(=O)O nan
CHEMBL4110535 159761 0 None -21 3 Rat 5.2 pEC50 = 5.2 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 422 11 5 9 0.1 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc([N+](=O)[O-])c1OCC(=O)O nan
1368 2258 31 None -5 11 Rat 6.2 pEC50 = 6.2 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
5310956 2258 31 None -5 11 Rat 6.2 pEC50 = 6.2 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
CHEMBL280563 2258 31 None -5 11 Rat 6.2 pEC50 = 6.2 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
46918015 155327 0 None -3 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4060360 155327 0 None -3 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
104766 34 36 None -17 14 Rat 4.2 pEC50 = 4.2 Functional
Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
1365 34 36 None -17 14 Rat 4.2 pEC50 = 4.2 Functional
Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
CHEMBL34453 34 36 None -17 14 Rat 4.2 pEC50 = 4.2 Functional
Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
57519364 118615 0 None -13 3 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 213 3 4 3 -0.9 NC1(C(=O)O)CC1(F)CP(=O)(O)O 10.1016/j.bmcl.2015.04.043
CHEMBL3427499 118615 0 None -13 3 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 213 3 4 3 -0.9 NC1(C(=O)O)CC1(F)CP(=O)(O)O 10.1016/j.bmcl.2015.04.043
16061421 155980 0 None -40 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 308 7 4 7 0.3 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])o1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4067923 155980 0 None -40 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 308 7 4 7 0.3 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])o1)C(=O)O 10.1021/acs.jmedchem.7b01438
46918015 155327 0 None -3 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4060360 155327 0 None -3 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
1310 2286 108 None -1148 17 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
1369 2286 108 None -1148 17 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
33032 2286 108 None -1148 17 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
44272391 2286 108 None -1148 17 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
88747398 2286 108 None -1148 17 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
CHEMBL575060 2286 108 None -1148 17 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
DB00142 2286 108 None -1148 17 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
6348408 7738 1 None -2 8 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL1089515 7738 1 None -2 8 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
6348408 7738 1 None -2 8 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1089515 7738 1 None -2 8 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
137654697 158141 0 None -15 3 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)[C@@H](O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4093081 158141 0 None -15 3 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)[C@@H](O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
17759041 92429 8 None -18 3 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 199 4 4 3 -0.9 N[C@@H](CCP(O)(O)=S)C(=O)O 10.1021/jm070400y
CHEMBL243925 92429 8 None -18 3 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 199 4 4 3 -0.9 N[C@@H](CCP(O)(O)=S)C(=O)O 10.1021/jm070400y
44300605 13244 0 None -9 3 Rat 4.1 pEC50 = 4.1 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccc(O)cc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1192345 13244 0 None -9 3 Rat 4.1 pEC50 = 4.1 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccc(O)cc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL543568 13244 0 None -9 3 Rat 4.1 pEC50 = 4.1 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccc(O)cc2)C1 10.1016/s0960-894x(01)00329-8
137661528 158960 0 None 3 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)[C@H](O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4101970 158960 0 None 3 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)[C@H](O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
1310 2286 108 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
1369 2286 108 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
33032 2286 108 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
44272391 2286 108 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
88747398 2286 108 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
CHEMBL575060 2286 108 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
DB00142 2286 108 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
1310 2286 108 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
1369 2286 108 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
33032 2286 108 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
44272391 2286 108 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
88747398 2286 108 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
CHEMBL575060 2286 108 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
DB00142 2286 108 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
3359 1908 6 None 1 2 Human 4.1 pEC50 = 4.1 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 10.1021/jm9602569
4236420 1908 6 None 1 2 Human 4.1 pEC50 = 4.1 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 10.1021/jm9602569
CHEMBL107768 1908 6 None 1 2 Human 4.1 pEC50 = 4.1 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 10.1021/jm9602569
1310 2286 108 None -1148 17 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
1369 2286 108 None -1148 17 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
33032 2286 108 None -1148 17 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
44272391 2286 108 None -1148 17 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
88747398 2286 108 None -1148 17 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
CHEMBL575060 2286 108 None -1148 17 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
DB00142 2286 108 None -1148 17 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
46918013 158183 0 None -15 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)C(O)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4093492 158183 0 None -15 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)C(O)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
10473248 14071 0 None -14 3 Rat 4.1 pEC50 = 4.1 Functional
Effective concentration required for partial agonistic activity at Metabotropic glutamate receptor 6; Partial agonistEffective concentration required for partial agonistic activity at Metabotropic glutamate receptor 6; Partial agonist
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2O)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1198741 14071 0 None -14 3 Rat 4.1 pEC50 = 4.1 Functional
Effective concentration required for partial agonistic activity at Metabotropic glutamate receptor 6; Partial agonistEffective concentration required for partial agonistic activity at Metabotropic glutamate receptor 6; Partial agonist
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2O)C1 10.1016/s0960-894x(01)00329-8
CHEMBL540015 14071 0 None -14 3 Rat 4.1 pEC50 = 4.1 Functional
Effective concentration required for partial agonistic activity at Metabotropic glutamate receptor 6; Partial agonistEffective concentration required for partial agonistic activity at Metabotropic glutamate receptor 6; Partial agonist
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2O)C1 10.1016/s0960-894x(01)00329-8
46197780 5507 0 None -4 4 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 273 7 4 4 -0.2 N[C@@H](CCP(=O)(O)CC(Cl)C(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1076865 5507 0 None -4 4 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 273 7 4 4 -0.2 N[C@@H](CCP(=O)(O)CC(Cl)C(=O)O)C(=O)O 10.1021/jm901523t
122197936 160229 0 None -17 3 Rat 5.1 pEC50 = 5.1 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 407 11 5 8 0.2 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(OC)c1OCC(=O)O nan
CHEMBL4114200 160229 0 None -17 3 Rat 5.1 pEC50 = 5.1 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 407 11 5 8 0.2 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(OC)c1OCC(=O)O nan
1608415 7737 8 None -5 3 Rat 4.0 pEC50 = 4 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 N[C@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
44660046 7737 8 None -5 3 Rat 4.0 pEC50 = 4 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 N[C@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1089514 7737 8 None -5 3 Rat 4.0 pEC50 = 4 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 N[C@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
44817558 196516 1 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 280 3 0 3 4.6 CCOC(=O)c1c(Cl)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL575059 196516 1 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 280 3 0 3 4.6 CCOC(=O)c1c(Cl)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
44817627 195253 2 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 293 3 1 3 4.5 Cc1c(-c2ccccc2)sc(N)c1C(=O)c1ccccc1 10.1016/j.ejmech.2009.09.025
CHEMBL566318 195253 2 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 293 3 1 3 4.5 Cc1c(-c2ccccc2)sc(N)c1C(=O)c1ccccc1 10.1016/j.ejmech.2009.09.025
44817595 195110 1 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 279 3 1 4 3.6 CCOC(=O)c1c(N)sc(-c2ccc(F)cc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL565503 195110 1 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 279 3 1 4 3.6 CCOC(=O)c1c(N)sc(-c2ccc(F)cc2)c1C 10.1016/j.ejmech.2009.09.025
9794208 89619 4 None -12589 4 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assayAntagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assay
ChEMBL 199 2 3 4 -1.3 N[C@@]1(C(=O)O)CC(=O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
CHEMBL2381640 89619 4 None -12589 4 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assayAntagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assay
ChEMBL 199 2 3 4 -1.3 N[C@@]1(C(=O)O)CC(=O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
71681825 89624 0 None -154 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assayAntagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assay
ChEMBL 226 3 3 4 -0.2 [N-]=[N+]=N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL2381645 89624 0 None -154 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assayAntagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assay
ChEMBL 226 3 3 4 -0.2 [N-]=[N+]=N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
44817688 197214 1 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 299 4 0 6 4.5 CCOC(=O)c1c(N=NC#N)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL584345 197214 1 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 299 4 0 6 4.5 CCOC(=O)c1c(N=NC#N)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
5353536 206369 17 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 230 1 0 5 -1.2 N#Cc1cc2c(cc1[N+](=O)[O-])=NC(=O)C(=O)N=2 10.1016/j.ejmech.2009.09.025
CHEMBL9790 206369 17 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 230 1 0 5 -1.2 N#Cc1cc2c(cc1[N+](=O)[O-])=NC(=O)C(=O)N=2 10.1016/j.ejmech.2009.09.025
44817597 195593 1 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 275 4 1 4 3.9 CCCOC(=O)c1c(N)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL568515 195593 1 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 275 4 1 4 3.9 CCCOC(=O)c1c(N)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
70051926 89620 2 None -208 4 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assayAntagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assay
ChEMBL 197 2 3 3 -0.3 C=C1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL2381641 89620 2 None -208 4 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assayAntagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assay
ChEMBL 197 2 3 3 -0.3 C=C1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
11084869 89622 2 None -467 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assayAntagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assay
ChEMBL 201 2 4 4 -1.5 N[C@@]1(C(=O)O)C[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
CHEMBL2381643 89622 2 None -467 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assayAntagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assay
ChEMBL 201 2 4 4 -1.5 N[C@@]1(C(=O)O)C[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
57338826 149095 0 None -72 5 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human mGlu6 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as inhibition of L-AP4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu6 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as inhibition of L-AP4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 375 5 4 5 1.0 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
CHEMBL3947221 149095 0 None -72 5 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human mGlu6 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as inhibition of L-AP4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu6 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as inhibition of L-AP4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 375 5 4 5 1.0 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
44817555 196955 1 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 303 4 0 5 4.6 CCOC(=O)c1c(N=C=S)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL579009 196955 1 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 303 4 0 5 4.6 CCOC(=O)c1c(N=C=S)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
44817625 196742 3 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 289 2 1 4 4.3 Cc1c(-c2ccccc2)sc(N)c1C(=O)OC(C)(C)C 10.1016/j.ejmech.2009.09.025
CHEMBL577069 196742 3 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 289 2 1 4 4.3 Cc1c(-c2ccccc2)sc(N)c1C(=O)OC(C)(C)C 10.1016/j.ejmech.2009.09.025
45483692 195467 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 317 5 0 5 4.5 CCOC(=O)c1c(N=NN(C)C)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL567862 195467 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 317 5 0 5 4.5 CCOC(=O)c1c(N=NN(C)C)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
95883 99724 43 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 161 4 3 3 -0.5 C[C@H](C[C@H](N)C(=O)O)C(=O)O 10.1016/j.ejmech.2009.09.025
CHEMBL288166 99724 43 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 161 4 3 3 -0.5 C[C@H](C[C@H](N)C(=O)O)C(=O)O 10.1016/j.ejmech.2009.09.025
69669747 183071 7 None -1023 4 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant mGlu6 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assayAntagonist activity at human recombinant mGlu6 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4751065 183071 7 None -1023 4 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant mGlu6 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assayAntagonist activity at human recombinant mGlu6 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4802733 183071 7 None -1023 4 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant mGlu6 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assayAntagonist activity at human recombinant mGlu6 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
921213 195553 18 None 7 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 247 2 1 4 3.1 COC(=O)c1c(N)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL568300 195553 18 None 7 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 247 2 1 4 3.1 COC(=O)c1c(N)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
3997004 100159 20 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 323 4 1 4 4.8 CCOC(=O)c1c(N)sc(-c2ccccc2)c1-c1ccccc1 10.1016/j.ejmech.2009.09.025
CHEMBL291935 100159 20 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 323 4 1 4 4.8 CCOC(=O)c1c(N)sc(-c2ccccc2)c1-c1ccccc1 10.1016/j.ejmech.2009.09.025
45483698 195316 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 359 5 0 6 4.2 CCOC(=O)c1c(N=NN2CCOCC2)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL566754 195316 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 359 5 0 6 4.2 CCOC(=O)c1c(N=NN2CCOCC2)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
44817596 195290 15 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 295 3 1 4 4.1 CCOC(=O)c1c(N)sc(-c2ccccc2Cl)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL566530 195290 15 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 295 3 1 4 4.1 CCOC(=O)c1c(N)sc(-c2ccccc2Cl)c1C 10.1016/j.ejmech.2009.09.025
4189 205195 91 None -26 35 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 10.1016/j.ejmech.2009.09.025
CHEMBL1559 205195 91 None -26 35 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 10.1016/j.ejmech.2009.09.025
CHEMBL91 205195 91 None -26 35 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 10.1016/j.ejmech.2009.09.025
308248 195109 26 None - 1 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 214 1 1 3 3.2 Cc1c(-c2ccccc2)sc(N)c1C#N 10.1016/j.ejmech.2009.09.025
CHEMBL565502 195109 26 None - 1 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 214 1 1 3 3.2 Cc1c(-c2ccccc2)sc(N)c1C#N 10.1016/j.ejmech.2009.09.025
3272524 84259 54 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 336 2 3 8 0.8 NS(=O)(=O)c1cccc2c1c([N+](=O)[O-])cc1nc(O)c(O)nc12 10.1016/j.ejmech.2009.09.025
CHEMBL222519 84259 54 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 336 2 3 8 0.8 NS(=O)(=O)c1cccc2c1c([N+](=O)[O-])cc1nc(O)c(O)nc12 10.1016/j.ejmech.2009.09.025
674768 195216 54 None -190 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 261 3 1 4 3.5 CCOC(=O)c1c(N)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL566136 195216 54 None -190 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 261 3 1 4 3.5 CCOC(=O)c1c(N)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
10684992 196760 39 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 291 4 1 5 3.5 CCOC(=O)c1c(N)sc(-c2ccc(OC)cc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL577248 196760 39 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 291 4 1 5 3.5 CCOC(=O)c1c(N)sc(-c2ccc(OC)cc2)c1C 10.1016/j.ejmech.2009.09.025
1436 31 7 None - 1 Human 4.7 pKi = 4.7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O 10.1021/jm000007r
15508178 31 7 None - 1 Human 4.7 pKi = 4.7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O 10.1021/jm000007r
CHEMBL60238 31 7 None - 1 Human 4.7 pKi = 4.7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O 10.1021/jm000007r
10058694 204877 0 None - 0 Human 5.6 pKi = 5.6 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CSC2C1[C@H]2C(=O)O 10.1021/jm000007r
CHEMBL88999 204877 0 None - 0 Human 5.6 pKi = 5.6 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CSC2C1[C@H]2C(=O)O 10.1021/jm000007r
1393 1510 58 None -346 6 Human 5.5 pKi = 5.5 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000007r
1396 1510 58 None -346 6 Human 5.5 pKi = 5.5 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000007r
213056 1510 58 None -346 6 Human 5.5 pKi = 5.5 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000007r
CHEMBL8759 1510 58 None -346 6 Human 5.5 pKi = 5.5 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000007r
1310 2286 108 None -354 17 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
1369 2286 108 None -354 17 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
33032 2286 108 None -354 17 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
44272391 2286 108 None -354 17 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
88747398 2286 108 None -354 17 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
CHEMBL575060 2286 108 None -354 17 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
DB00142 2286 108 None -354 17 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
10197984 2388 37 None -147 5 Human 6.4 pKi = 6.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm000007r
1394 2388 37 None -147 5 Human 6.4 pKi = 6.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm000007r
CHEMBL275079 2388 37 None -147 5 Human 6.4 pKi = 6.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm000007r
1406 2042 32 None -25 7 Human 5.3 pKi = 5.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm000007r
4545574 2042 32 None -25 7 Human 5.3 pKi = 5.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm000007r
CHEMBL277475 2042 32 None -25 7 Human 5.3 pKi = 5.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm000007r
44322921 205110 1 None - 0 Human 5.3 pKi = 5.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)CC2CC1[C@H]2C(=O)O 10.1021/jm000007r
CHEMBL90501 205110 1 None - 0 Human 5.3 pKi = 5.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)CC2CC1[C@H]2C(=O)O 10.1021/jm000007r
1368 2258 31 None -1 11 Human 5.2 pKi = 5.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm000007r
5310956 2258 31 None -1 11 Human 5.2 pKi = 5.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm000007r
CHEMBL280563 2258 31 None -1 11 Human 5.2 pKi = 5.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm000007r
6604795 106515 1 None - 1 Human 4.2 pKi = 4.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 200 4 3 5 0.0 Cc1onc(O)c1CC[C@H](N)C(=O)O 10.1021/jm000007r
CHEMBL315268 106515 1 None - 1 Human 4.2 pKi = 4.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 200 4 3 5 0.0 Cc1onc(O)c1CC[C@H](N)C(=O)O 10.1021/jm000007r
104766 34 36 None -11 14 Human 4.2 pKi = 4.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm000007r
1365 34 36 None -11 14 Human 4.2 pKi = 4.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm000007r
CHEMBL34453 34 36 None -11 14 Human 4.2 pKi = 4.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm000007r
1410 2242 45 None -2 8 Human 6.1 pKi = 6.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm000007r
1412 2242 45 None -2 8 Human 6.1 pKi = 6.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm000007r
179394 2242 45 None -2 8 Human 6.1 pKi = 6.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm000007r
57689795 2242 45 None -2 8 Human 6.1 pKi = 6.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm000007r
CHEMBL33567 2242 45 None -2 8 Human 6.1 pKi = 6.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm000007r
1310 2286 108 None -1148 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 2286 108 None -1148 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 2286 108 None -1148 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 2286 108 None -1148 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 2286 108 None -1148 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 2286 108 None -1148 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 2286 108 None -1148 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1310 2286 108 None -354 17 Human 8.3 pEC50 = 8.3 Functional
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 2286 108 None -354 17 Human 8.3 pEC50 = 8.3 Functional
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 2286 108 None -354 17 Human 8.3 pEC50 = 8.3 Functional
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 2286 108 None -354 17 Human 8.3 pEC50 = 8.3 Functional
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 2286 108 None -354 17 Human 8.3 pEC50 = 8.3 Functional
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 2286 108 None -354 17 Human 8.3 pEC50 = 8.3 Functional
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 2286 108 None -354 17 Human 8.3 pEC50 = 8.3 Functional
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1411 2329 61 None -3 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
4120 2329 61 None -3 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
57689797 2329 61 None -3 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
68841 2329 61 None -3 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
CHEMBL284377 2329 61 None -3 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
DB04522 2329 61 None -3 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
1411 2329 61 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
4120 2329 61 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
57689797 2329 61 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
68841 2329 61 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
CHEMBL284377 2329 61 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
DB04522 2329 61 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
3359 1908 6 None 1 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 8759641
4236420 1908 6 None 1 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 8759641
CHEMBL107768 1908 6 None 1 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 8759641
1436 31 7 None - 1 Rat 4.7 pEC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O None
15508178 31 7 None - 1 Rat 4.7 pEC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O None
CHEMBL60238 31 7 None - 1 Rat 4.7 pEC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O None
1310 2286 108 None -354 17 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
1369 2286 108 None -354 17 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
33032 2286 108 None -354 17 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
44272391 2286 108 None -354 17 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
88747398 2286 108 None -354 17 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
CHEMBL575060 2286 108 None -354 17 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
DB00142 2286 108 None -354 17 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
1416 3044 37 None -6 4 Rat 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 294 2 2 4 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1 18593581
5866327 3044 37 None -6 4 Rat 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 294 2 2 4 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1 18593581
CHEMBL164770 3044 37 None -6 4 Rat 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 294 2 2 4 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1 18593581
1368 2258 31 None -5 11 Rat 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 9833633
5310956 2258 31 None -5 11 Rat 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 9833633
CHEMBL280563 2258 31 None -5 11 Rat 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 9833633
6706 2335 4 None -38 8 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 22223752
71041983 2335 4 None -38 8 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 22223752
CHEMBL3114673 2335 4 None -38 8 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 22223752
1407 2048 34 None -114 7 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 11166323
16062593 2048 34 None -114 7 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 11166323
CHEMBL143210 2048 34 None -114 7 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 11166323
46898088 2334 4 None -8 8 Rat 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 19525404
6739 2334 4 None -8 8 Rat 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 19525404
CHEMBL3114672 2334 4 None -8 8 Rat 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 19525404
1368 2258 31 None -1 11 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 9144651
5310956 2258 31 None -1 11 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 9144651
CHEMBL280563 2258 31 None -1 11 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 9144651
1411 2329 61 None -1 6 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
4120 2329 61 None -1 6 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
57689797 2329 61 None -1 6 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
68841 2329 61 None -1 6 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
CHEMBL284377 2329 61 None -1 6 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
DB04522 2329 61 None -1 6 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
1398 362 0 None -15 2 Rat 4.1 pEC50 None 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 199 4 4 4 -1.1 OC(=O)C(COP(=O)(O)O)(N)C 12769621
3964633 362 0 None -15 2 Rat 4.1 pEC50 None 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 199 4 4 4 -1.1 OC(=O)C(COP(=O)(O)O)(N)C 12769621
CHEMBL1437137 362 0 None -15 2 Rat 4.1 pEC50 None 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 199 4 4 4 -1.1 OC(=O)C(COP(=O)(O)O)(N)C 12769621
104766 34 36 None -17 14 Rat 4.2 pEC50 None 4.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O None
1365 34 36 None -17 14 Rat 4.2 pEC50 None 4.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O None
CHEMBL34453 34 36 None -17 14 Rat 4.2 pEC50 None 4.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O None
1310 2286 108 None -1148 17 Rat 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
1369 2286 108 None -1148 17 Rat 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
33032 2286 108 None -1148 17 Rat 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
44272391 2286 108 None -1148 17 Rat 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
88747398 2286 108 None -1148 17 Rat 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
CHEMBL575060 2286 108 None -1148 17 Rat 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
DB00142 2286 108 None -1148 17 Rat 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
1378 2384 48 None -4265 14 Human 4.5 pEC50 None 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 11138847
1399 2384 48 None -4265 14 Human 4.5 pEC50 None 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 11138847
9819927 2384 48 None -4265 14 Human 4.5 pEC50 None 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 11138847
CHEMBL432038 2384 48 None -4265 14 Human 4.5 pEC50 None 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 11138847
104766 34 36 None -11 14 Human 4.7 pEC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 9144651
1365 34 36 None -11 14 Human 4.7 pEC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 9144651
CHEMBL34453 34 36 None -11 14 Human 4.7 pEC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 9144651
1310 2286 108 None -354 17 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
1369 2286 108 None -354 17 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
33032 2286 108 None -354 17 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
44272391 2286 108 None -354 17 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
88747398 2286 108 None -354 17 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
CHEMBL575060 2286 108 None -354 17 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
DB00142 2286 108 None -354 17 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
1406 2042 32 None -25 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10336568
1406 2042 32 None -25 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 11166323
4545574 2042 32 None -25 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10336568
4545574 2042 32 None -25 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 11166323
CHEMBL277475 2042 32 None -25 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10336568
CHEMBL277475 2042 32 None -25 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 11166323
1377 1313 19 None -60 8 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 9833633
5310979 1313 19 None -60 8 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 9833633
CHEMBL284193 1313 19 None -60 8 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 9833633
1410 2242 45 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11166323
1410 2242 45 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144651
1412 2242 45 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11166323
1412 2242 45 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144651
179394 2242 45 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11166323
179394 2242 45 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144651
57689795 2242 45 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11166323
57689795 2242 45 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144651
CHEMBL33567 2242 45 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11166323
CHEMBL33567 2242 45 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144651
1414 2425 0 None -707 2 Rat 3.5 pIC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 12769621
1795545 2425 0 None -707 2 Rat 3.5 pIC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 12769621
CHEMBL1488784 2425 0 None -707 2 Rat 3.5 pIC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 12769621
1415 2576 36 None -10 2 Human 3.3 pIC50 None 3.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C None
3972752 2576 36 None -10 2 Human 3.3 pIC50 None 3.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C None
CHEMBL86508 2576 36 None -10 2 Human 3.3 pIC50 None 3.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C None
1408 263 28 None -3 7 Rat 4.7 pIC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O None
6604820 263 28 None -3 7 Rat 4.7 pIC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O None
CHEMBL285043 263 28 None -3 7 Rat 4.7 pIC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O None
CHEMBL288635 263 28 None -3 7 Rat 4.7 pIC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O None
1393 1510 58 None -346 6 Human 5.5 pIC50 None 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10090786
1396 1510 58 None -346 6 Human 5.5 pIC50 None 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10090786
213056 1510 58 None -346 6 Human 5.5 pIC50 None 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10090786
CHEMBL8759 1510 58 None -346 6 Human 5.5 pIC50 None 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10090786
10197984 2388 37 None -147 5 Human 6.4 pIC50 None 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10090786
1394 2388 37 None -147 5 Human 6.4 pIC50 None 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10090786
CHEMBL275079 2388 37 None -147 5 Human 6.4 pIC50 None 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10090786




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
71681824 89625 0 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 200 2 4 4 -1.6 N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
CHEMBL2381646 89625 0 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 200 2 4 4 -1.6 N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
10979251 89629 0 None - 2 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
CHEMBL2381650 89629 0 None - 2 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
139119037 89631 2 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
15479143 89631 2 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
CHEMBL2381652 89631 2 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
1310 2286 108 None -43 18 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
1369 2286 108 None -43 18 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
33032 2286 108 None -43 18 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
44272391 2286 108 None -43 18 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
88747398 2286 108 None -43 18 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
CHEMBL575060 2286 108 None -43 18 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
DB00142 2286 108 None -43 18 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
139054390 203215 101 None -1 5 Rat 4.7 pEC50 = 4.7 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O 10.1021/jm9703597
23327 203215 101 None -1 5 Rat 4.7 pEC50 = 4.7 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O 10.1021/jm9703597
CHEMBL76232 203215 101 None -1 5 Rat 4.7 pEC50 = 4.7 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O 10.1021/jm9703597
1411 2329 61 None - 1 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
4120 2329 61 None - 1 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
57689797 2329 61 None - 1 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
68841 2329 61 None - 1 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
CHEMBL284377 2329 61 None - 1 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
DB04522 2329 61 None - 1 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
2207 99403 54 None -2 7 Human 6.6 pEC50 = 6.6 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O 10.1021/jm970719q
CHEMBL285843 99403 54 None -2 7 Human 6.6 pEC50 = 6.6 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O 10.1021/jm970719q
71681826 89630 0 None - 2 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
CHEMBL2381651 89630 0 None - 2 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
1393 1510 58 None -162 6 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm4000165
1396 1510 58 None -162 6 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm4000165
213056 1510 58 None -162 6 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm4000165
CHEMBL8759 1510 58 None -162 6 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm4000165
70052526 89621 2 None - 1 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 201 2 4 4 -1.5 N[C@@]1(C(=O)O)C[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
CHEMBL2381642 89621 2 None - 1 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 201 2 4 4 -1.5 N[C@@]1(C(=O)O)C[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
1310 2286 108 None -85 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
1369 2286 108 None -85 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
33032 2286 108 None -85 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
44272391 2286 108 None -85 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
88747398 2286 108 None -85 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
CHEMBL575060 2286 108 None -85 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
DB00142 2286 108 None -85 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
10846649 100761 4 None - 0 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H]2C[C@H]1[C@H]2C(=O)O 10.1021/jm970719q
CHEMBL296054 100761 4 None - 0 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H]2C[C@H]1[C@H]2C(=O)O 10.1021/jm970719q
1410 2242 45 None -7 6 Human 7.3 pEC50 = 7.3 Binding
Activation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.8b01120
1412 2242 45 None -7 6 Human 7.3 pEC50 = 7.3 Binding
Activation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.8b01120
179394 2242 45 None -7 6 Human 7.3 pEC50 = 7.3 Binding
Activation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.8b01120
57689795 2242 45 None -7 6 Human 7.3 pEC50 = 7.3 Binding
Activation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.8b01120
CHEMBL33567 2242 45 None -7 6 Human 7.3 pEC50 = 7.3 Binding
Activation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.8b01120
1410 2242 45 None - 6 Rat 6.2 pEC50 = 6.2 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm9703597
1412 2242 45 None - 6 Rat 6.2 pEC50 = 6.2 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm9703597
179394 2242 45 None - 6 Rat 6.2 pEC50 = 6.2 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm9703597
57689795 2242 45 None - 6 Rat 6.2 pEC50 = 6.2 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm9703597
CHEMBL33567 2242 45 None - 6 Rat 6.2 pEC50 = 6.2 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm9703597
6604795 106515 1 None - 1 Rat 4.2 pEC50 = 4.2 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 200 4 3 5 0.0 Cc1onc(O)c1CC[C@H](N)C(=O)O 10.1021/jm9703597
CHEMBL315268 106515 1 None - 1 Rat 4.2 pEC50 = 4.2 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 200 4 3 5 0.0 Cc1onc(O)c1CC[C@H](N)C(=O)O 10.1021/jm9703597
70051296 89627 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
CHEMBL2381648 89627 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
60096211 89628 0 None - 2 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL2381649 89628 0 None - 2 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
11310142 2389 16 None - 2 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm4000165
11614 2389 16 None - 2 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm4000165
CHEMBL192051 2389 16 None - 2 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm4000165
71681823 89623 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 226 3 3 4 -0.2 [N-]=[N+]=N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
CHEMBL2381644 89623 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 226 3 3 4 -0.2 [N-]=[N+]=N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
104766 34 36 None -38 11 Human 4.1 pEC50 = 4.1 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm970719q
1365 34 36 None -38 11 Human 4.1 pEC50 = 4.1 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm970719q
CHEMBL34453 34 36 None -38 11 Human 4.1 pEC50 = 4.1 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm970719q
3359 1908 6 None - 0 Rat 4.1 pEC50 = 4.1 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 10.1021/jm9703597
4236420 1908 6 None - 0 Rat 4.1 pEC50 = 4.1 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 10.1021/jm9703597
CHEMBL107768 1908 6 None - 0 Rat 4.1 pEC50 = 4.1 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 10.1021/jm9703597
1410 2242 45 None - 6 Rat 6.1 pEC50 = 6.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
1412 2242 45 None - 6 Rat 6.1 pEC50 = 6.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
179394 2242 45 None - 6 Rat 6.1 pEC50 = 6.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
57689795 2242 45 None - 6 Rat 6.1 pEC50 = 6.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
CHEMBL33567 2242 45 None - 6 Rat 6.1 pEC50 = 6.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
11344646 126255 1 None - 2 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 199 2 3 3 -0.2 C[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL365368 126255 1 None - 2 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 199 2 3 3 -0.2 C[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
11275666 89626 1 None - 2 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 200 2 4 4 -1.6 N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL2381647 89626 1 None - 2 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 200 2 4 4 -1.6 N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
1378 2384 48 None - 10 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
1399 2384 48 None - 10 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
9819927 2384 48 None - 10 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
CHEMBL432038 2384 48 None - 10 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
1397 2493 11 None - 5 Rat 5.7 pIC50 = 5.7 Binding
Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
9886034 2493 11 None - 5 Rat 5.7 pIC50 = 5.7 Binding
Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
CHEMBL186453 2493 11 None - 5 Rat 5.7 pIC50 = 5.7 Binding
Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
71566598 142158 10 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at mGluR6 (unknown origin) by FLIPR assayAntagonist activity at mGluR6 (unknown origin) by FLIPR assay
ChEMBL 377 4 1 4 2.8 NC(=O)c1cc(-c2ccc(F)cc2)c2ccc(CN3C(=O)CCC3=O)cc2n1 10.1016/j.bmcl.2020.127066
CHEMBL3892073 142158 10 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at mGluR6 (unknown origin) by FLIPR assayAntagonist activity at mGluR6 (unknown origin) by FLIPR assay
ChEMBL 377 4 1 4 2.8 NC(=O)c1cc(-c2ccc(F)cc2)c2ccc(CN3C(=O)CCC3=O)cc2n1 10.1016/j.bmcl.2020.127066
12310764 1939 59 Functional -14 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
1233 1939 59 Functional -14 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
1371 1939 59 Functional -14 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
CHEMBL284895 1939 59 Functional -14 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
1310 2286 108 Functional -85 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1310 2286 108 Functional -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 2286 108 Functional -85 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 2286 108 Functional -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 2286 108 Functional -85 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 2286 108 Functional -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 2286 108 Functional -85 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 2286 108 Functional -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 2286 108 Functional -85 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 2286 108 Functional -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 2286 108 Functional -85 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 2286 108 Functional -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 2286 108 Functional -85 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 2286 108 Functional -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1370 3212 62 Functional -602 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
1372 3212 62 Functional -602 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
40539 3212 62 Functional -602 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
6971145 3212 62 Functional -602 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
CHEMBL279956 3212 62 Functional -602 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
DB02999 3212 62 Functional -602 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
128563 3408 28 Functional -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 3408 28 Functional -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 3408 28 Functional -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 3408 28 Functional -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
10297 26905 29 Functional -38 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 26905 29 Functional -38 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
446220 132998 13 Functional -1778 45 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 132998 13 Functional -1778 45 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
162265 200587 19 Functional -239 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 200587 19 Functional -239 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 200587 19 Functional -239 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
139054390 203215 101 Functional -1 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O None
23327 203215 101 Functional -1 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O None
CHEMBL76232 203215 101 Functional -1 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O None
None 214412 0 Functional -2 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 173 2 3 3 -0.3 C1CC(CC1C(=O)O)(C(=O)O)N None
25137849 214425 0 Functional -4 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 214425 0 Functional -4 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 214565 0 Functional -1 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 214566 0 Functional -1 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 214574 0 Functional -13 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 214575 0 Functional -16 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 214748 0 Functional -1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 144 2 2 2 -0.7 CC(C(=O)NC)NC(=O)C None
None 214749 0 Functional -1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 161 5 3 3 -0.3 C(CC(C(=O)O)N)CC(=O)O None
None 214587 0 Functional -2 4 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 185 4 4 4 -1.5 C(C(C(=O)O)N)OP(=O)(O)O None
2207 99403 54 Functional -1 7 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
CHEMBL285843 99403 54 Functional -1 7 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
2207 99403 54 Functional -2 7 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
CHEMBL285843 99403 54 Functional -2 7 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None