Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

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 DOI
1410 2274 None 38 Human Functional pEC50 = 6 6.0 -2 8
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 2274 None 38 Human Functional pEC50 = 6 6.0 -2 8
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 2274 None 38 Human Functional pEC50 = 6 6.0 -2 8
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 2274 None 38 Human Functional pEC50 = 6 6.0 -2 8
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 2274 None 38 Human Functional pEC50 = 6 6.0 -2 8
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 2274 None 38 Rat Functional pEC50 = 6 6.0 -5 8
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 2274 None 38 Rat Functional pEC50 = 6 6.0 -5 8
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 2274 None 38 Rat Functional pEC50 = 6 6.0 -5 8
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 2274 None 38 Rat Functional pEC50 = 6 6.0 -5 8
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 2274 None 38 Rat Functional pEC50 = 6 6.0 -5 8
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 99919 None 47 Rat Functional pEC50 = 6 6.0 -194 4
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 99919 None 47 Rat Functional pEC50 = 6 6.0 -194 4
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 13037 None 0 Rat Functional pEC50 = 4 4.0 -2 3
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 13037 None 0 Rat Functional pEC50 = 4 4.0 -2 3
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 13037 None 0 Rat Functional pEC50 = 4 4.0 -2 3
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 159115 None 0 Human Functional pEC50 = 5.0 5.0 -1 4
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 159115 None 0 Human Functional pEC50 = 5.0 5.0 -1 4
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 1318 None 30 Rat Functional pEC50 = 6.0 6.0 -7 5
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 1318 None 30 Rat Functional pEC50 = 6.0 6.0 -7 5
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 1318 None 30 Rat Functional pEC50 = 6.0 6.0 -7 5
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 265 None 24 Rat Functional pEC50 = 5.0 5.0 -3 7
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 265 None 24 Rat Functional pEC50 = 5.0 5.0 -3 7
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 265 None 24 Rat Functional pEC50 = 5.0 5.0 -3 7
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 265 None 24 Rat Functional pEC50 = 5.0 5.0 -3 7
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 157437 None 0 Human Functional pEC50 = 6.0 6.0 1 4
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 157437 None 0 Human Functional pEC50 = 6.0 6.0 1 4
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 157786 None 0 Human Functional pEC50 = 6.0 6.0 -1 4
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 157786 None 0 Human Functional pEC50 = 6.0 6.0 -1 4
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 8220 None 0 Rat Functional pEC50 = 6.0 6.0 1 5
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 8220 None 0 Rat Functional pEC50 = 6.0 6.0 1 5
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 265 None 24 Human Functional pEC50 = 5.0 5.0 -2 7
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 265 None 24 Human Functional pEC50 = 5.0 5.0 -2 7
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 265 None 24 Human Functional pEC50 = 5.0 5.0 -2 7
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 265 None 24 Human Functional pEC50 = 5.0 5.0 -2 7
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 156195 None 0 Human Functional pEC50 = 4.9 4.9 -20 3
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 156195 None 0 Human Functional pEC50 = 4.9 4.9 -20 3
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 114891 None 1 Rat Functional pEC50 = 5.9 5.9 -151 4
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 114891 None 1 Rat Functional pEC50 = 5.9 5.9 -151 4
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 72197 None 1 Rat Functional pEC50 = 4.9 4.9 -1 2
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 72197 None 1 Rat Functional pEC50 = 4.9 4.9 -1 2
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 169475 None 0 Rat Functional pEC50 = 4.9 4.9 -1 2
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 169475 None 0 Rat Functional pEC50 = 4.9 4.9 -1 2
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 161005 None 0 Rat Functional pEC50 = 4.9 4.9 -12 2
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 161005 None 0 Rat Functional pEC50 = 4.9 4.9 -12 2
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 31349 None 0 Rat Functional pEC50 = 6.8 6.8 -33 5
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 31349 None 0 Rat Functional pEC50 = 6.8 6.8 -33 5
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 2366 None 7 Human Functional pEC50 = 5.8 5.8 -11 8
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 2366 None 7 Human Functional pEC50 = 5.8 5.8 -11 8
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 2366 None 7 Human Functional pEC50 = 5.8 5.8 -11 8
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 139128 None 0 Rat Functional pEC50 = 4.8 4.8 -7 3
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 139128 None 0 Rat Functional pEC50 = 4.8 4.8 -7 3
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 157896 None 0 Human Functional pEC50 = 4.8 4.8 -5 3
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 157896 None 0 Human Functional pEC50 = 4.8 4.8 -5 3
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 265 None 24 Rat Functional pEC50 = 4.7 4.7 -3 7
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 265 None 24 Rat Functional pEC50 = 4.7 4.7 -3 7
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 265 None 24 Rat Functional pEC50 = 4.7 4.7 -3 7
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 265 None 24 Rat Functional pEC50 = 4.7 4.7 -3 7
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 160161 None 0 Rat Functional pEC50 = 4.7 4.7 -34 4
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 160161 None 0 Rat Functional pEC50 = 4.7 4.7 -34 4
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 2274 None 38 Rat Functional pEC50 = 5.7 5.7 -5 8
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 2274 None 38 Rat Functional pEC50 = 5.7 5.7 -5 8
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 2274 None 38 Rat Functional pEC50 = 5.7 5.7 -5 8
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 2274 None 38 Rat Functional pEC50 = 5.7 5.7 -5 8
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 2274 None 38 Rat Functional pEC50 = 5.7 5.7 -5 8
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 157747 None 19 Human Functional pEC50 = 5.7 5.7 -831 4
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 157747 None 19 Human Functional pEC50 = 5.7 5.7 -831 4
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 85876 None 0 Human Functional pEC50 = 5.7 5.7 -64 4
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 85876 None 0 Human Functional pEC50 = 5.7 5.7 -64 4
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 2315 None 61 Human Functional pEC50 = 4.7 4.7 -354 17
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 2315 None 61 Human Functional pEC50 = 4.7 4.7 -354 17
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 2315 None 61 Human Functional pEC50 = 4.7 4.7 -354 17
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 2315 None 61 Human Functional pEC50 = 4.7 4.7 -354 17
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 2315 None 61 Human Functional pEC50 = 4.7 4.7 -354 17
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 2315 None 61 Human Functional pEC50 = 4.7 4.7 -354 17
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 2315 None 61 Human Functional pEC50 = 4.7 4.7 -354 17
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 30 None 2 Rat Functional pEC50 = 4.7 4.7 - 1
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 30 None 2 Rat Functional pEC50 = 4.7 4.7 - 1
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 30 None 2 Rat Functional pEC50 = 4.7 4.7 - 1
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 2274 None 38 Rat Functional pEC50 = 5.7 5.7 -5 8
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 2274 None 38 Rat Functional pEC50 = 5.7 5.7 -5 8
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 2274 None 38 Rat Functional pEC50 = 5.7 5.7 -5 8
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 2274 None 38 Rat Functional pEC50 = 5.7 5.7 -5 8
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 2274 None 38 Rat Functional pEC50 = 5.7 5.7 -5 8
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 12956 None 0 Rat Functional pEC50 = 4.7 4.7 -1 3
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 12956 None 0 Rat Functional pEC50 = 4.7 4.7 -1 3
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 12956 None 0 Rat Functional pEC50 = 4.7 4.7 -1 3
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 158210 None 0 Human Functional pEC50 = 4.6 4.6 -3 3
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 158210 None 0 Human Functional pEC50 = 4.6 4.6 -3 3
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 2274 None 38 Human Functional pEC50 = 5.6 5.6 -2 8
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 2274 None 38 Human Functional pEC50 = 5.6 5.6 -2 8
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 2274 None 38 Human Functional pEC50 = 5.6 5.6 -2 8
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 2274 None 38 Human Functional pEC50 = 5.6 5.6 -2 8
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 2274 None 38 Human Functional pEC50 = 5.6 5.6 -2 8
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 157046 None 0 Human Functional pEC50 = 5.6 5.6 -2 3
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 157046 None 0 Human Functional pEC50 = 5.6 5.6 -2 3
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 158107 None 0 Human Functional pEC50 = 5.6 5.6 1 4
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 158107 None 0 Human Functional pEC50 = 5.6 5.6 1 4
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 208966 None 10 Human Functional pEC50 = 5.6 5.6 -630 4
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 208966 None 10 Human Functional pEC50 = 5.6 5.6 -630 4
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 160618 None 0 Rat Functional pEC50 = 5.6 5.6 -7 4
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 160618 None 0 Rat Functional pEC50 = 5.6 5.6 -7 4
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 158582 None 0 Human Functional pEC50 = 4.6 4.6 -19 3
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 158582 None 0 Human Functional pEC50 = 4.6 4.6 -19 3
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 158886 None 0 Human Functional pEC50 = 4.6 4.6 -5 3
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 158886 None 0 Human Functional pEC50 = 4.6 4.6 -5 3
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 92156 None 7 Rat Functional pEC50 = 4.6 4.6 -15 3
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 92156 None 7 Rat Functional pEC50 = 4.6 4.6 -15 3
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 157510 None 0 Human Functional pEC50 = 5.5 5.5 -7 3
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 157510 None 0 Human Functional pEC50 = 5.5 5.5 -7 3
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 1539 None 42 Human Functional pEC50 = 5.5 5.5 -346 6
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 1539 None 42 Human Functional pEC50 = 5.5 5.5 -346 6
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 1539 None 42 Human Functional pEC50 = 5.5 5.5 -346 6
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 1539 None 42 Human Functional pEC50 = 5.5 5.5 -346 6
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 156023 None 0 Human Functional pEC50 = 4.5 4.5 -5 3
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 156023 None 0 Human Functional pEC50 = 4.5 4.5 -5 3
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 7822 None 0 Human Functional pEC50 = 4.5 4.5 -2 8
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 7822 None 0 Human Functional pEC50 = 4.5 4.5 -2 8
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 159001 None 0 Human Functional pEC50 = 4.5 4.5 -3 2
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 159001 None 0 Human Functional pEC50 = 4.5 4.5 -3 2
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 7822 None 0 Rat Functional pEC50 = 4.5 4.5 -2 8
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 7822 None 0 Rat Functional pEC50 = 4.5 4.5 -2 8
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 2079 None 36 Human Functional pEC50 = 5.5 5.5 -114 7
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 2079 None 36 Human Functional pEC50 = 5.5 5.5 -114 7
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 2079 None 36 Human Functional pEC50 = 5.5 5.5 -114 7
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 2366 None 7 Human Functional pEC50 = 5.5 5.5 -11 8
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 2366 None 7 Human Functional pEC50 = 5.5 5.5 -11 8
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 2366 None 7 Human Functional pEC50 = 5.5 5.5 -11 8
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 156288 None 0 Human Functional pEC50 = 5.5 5.5 -5 3
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 156288 None 0 Human Functional pEC50 = 5.5 5.5 -5 3
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 158126 None 0 Human Functional pEC50 = 5.5 5.5 -10 3
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 158126 None 0 Human Functional pEC50 = 5.5 5.5 -10 3
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 8316 None 0 Rat Functional pEC50 = 4.5 4.5 -4 4
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 8316 None 0 Rat Functional pEC50 = 4.5 4.5 -4 4
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 8316 None 0 Rat Functional pEC50 = 4.5 4.5 -4 4
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 2274 None 38 Rat Functional pEC50 = 5.5 5.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 5.5 5.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 5.5 5.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 5.5 5.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 5.5 5.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 6.5 6.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 6.5 6.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 6.5 6.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 6.5 6.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 6.5 6.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 6.5 6.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 6.5 6.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 6.5 6.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 6.5 6.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 6.5 6.5 -5 8
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 85549 None 0 Human Functional pEC50 = 5.5 5.5 -1 3
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 85549 None 0 Human Functional pEC50 = 5.5 5.5 -1 3
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 123463 None 21 Human Functional pEC50 = 5.5 5.5 -158 4
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 123463 None 21 Human Functional pEC50 = 5.5 5.5 -158 4
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 2274 None 38 Rat Functional pEC50 = 5.5 5.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 5.5 5.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 5.5 5.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 5.5 5.5 -5 8
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 2274 None 38 Rat Functional pEC50 = 5.5 5.5 -5 8
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 156058 None 0 Human Functional pEC50 = 5.4 5.4 -20 4
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 156058 None 0 Human Functional pEC50 = 5.4 5.4 -20 4
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 157007 None 0 Human Functional pEC50 = 5.4 5.4 -7 4
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 157007 None 0 Human Functional pEC50 = 5.4 5.4 -7 4
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 2079 None 36 Rat Functional pEC50 = 5.4 5.4 -117 7
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 2079 None 36 Rat Functional pEC50 = 5.4 5.4 -117 7
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 2079 None 36 Rat Functional pEC50 = 5.4 5.4 -117 7
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 160674 None 0 Rat Functional pEC50 = 5.4 5.4 -7 3
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 160674 None 0 Rat Functional pEC50 = 5.4 5.4 -7 3
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 158089 None 0 Human Functional pEC50 = 5.4 5.4 -2 3
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 158089 None 0 Human Functional pEC50 = 5.4 5.4 -2 3
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 158582 None 0 Human Functional pEC50 = 5.4 5.4 -19 3
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 158582 None 0 Human Functional pEC50 = 5.4 5.4 -19 3
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 159548 None 0 Human Functional pEC50 = 5.4 5.4 -1 3
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 159548 None 0 Human Functional pEC50 = 5.4 5.4 -1 3
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 1340 None 23 Rat Functional pEC50 = 4.4 4.4 -60 8
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 1340 None 23 Rat Functional pEC50 = 4.4 4.4 -60 8
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 1340 None 23 Rat Functional pEC50 = 4.4 4.4 -60 8
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 2421 None 36 Human Functional pEC50 = 6.4 6.4 -147 5
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 2421 None 36 Human Functional pEC50 = 6.4 6.4 -147 5
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 2421 None 36 Human Functional pEC50 = 6.4 6.4 -147 5
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 2367 None 9 Human Functional pEC50 = 5.4 5.4 -38 8
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 2367 None 9 Human Functional pEC50 = 5.4 5.4 -38 8
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 2367 None 9 Human Functional pEC50 = 5.4 5.4 -38 8
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 158504 None 0 Human Functional pEC50 = 5.4 5.4 -8 3
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 158504 None 0 Human Functional pEC50 = 5.4 5.4 -8 3
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 2367 None 9 Rat Functional pEC50 = 5.4 5.4 -38 8
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 2367 None 9 Rat Functional pEC50 = 5.4 5.4 -38 8
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 2367 None 9 Rat Functional pEC50 = 5.4 5.4 -38 8
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 8243 None 0 Rat Functional pEC50 = 4.4 4.4 -12 3
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 8243 None 0 Rat Functional pEC50 = 4.4 4.4 -12 3
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 8358 None 0 Rat Functional pEC50 = 4.4 4.4 -4 3
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 8358 None 0 Rat Functional pEC50 = 4.4 4.4 -4 3
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 156241 None 0 Human Functional pEC50 = 5.4 5.4 -2 3
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 156241 None 0 Human Functional pEC50 = 5.4 5.4 -2 3
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 158363 None 0 Human Functional pEC50 = 5.3 5.3 -9 3
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 158363 None 0 Human Functional pEC50 = 5.3 5.3 -9 3
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 72701 None 1 Rat Functional pEC50 = 4.3 4.3 1 2
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 72701 None 1 Rat Functional pEC50 = 4.3 4.3 1 2
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 2073 None 26 Rat Functional pEC50 = 5.3 5.3 -23 7
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 2073 None 26 Rat Functional pEC50 = 5.3 5.3 -23 7
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 2073 None 26 Rat Functional pEC50 = 5.3 5.3 -23 7
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 159946 None 0 Rat Functional pEC50 = 5.3 5.3 -46 4
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 159946 None 0 Rat Functional pEC50 = 5.3 5.3 -46 4
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 139193 None 0 Rat Functional pEC50 = 6.3 6.3 -3 3
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 139193 None 0 Rat Functional pEC50 = 6.3 6.3 -3 3
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 146818 None 0 Rat Functional pEC50 = 4.3 4.3 1 2
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 146818 None 0 Rat Functional pEC50 = 4.3 4.3 1 2
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 160323 None 0 Rat Functional pEC50 = 4.3 4.3 -4 3
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 160323 None 0 Rat Functional pEC50 = 4.3 4.3 -4 3
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 2274 None 38 Rat Functional pEC50 = 7.3 7.3 -5 8
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 2274 None 38 Rat Functional pEC50 = 7.3 7.3 -5 8
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 2274 None 38 Rat Functional pEC50 = 7.3 7.3 -5 8
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 2274 None 38 Rat Functional pEC50 = 7.3 7.3 -5 8
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 2274 None 38 Rat Functional pEC50 = 7.3 7.3 -5 8
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 156195 None 0 Human Functional pEC50 = 5.2 5.2 -20 3
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 156195 None 0 Human Functional pEC50 = 5.2 5.2 -20 3
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 13729 None 0 Rat Functional pEC50 = 4.2 4.2 - 1
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 13729 None 0 Rat Functional pEC50 = 4.2 4.2 - 1
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 13729 None 0 Rat Functional pEC50 = 4.2 4.2 - 1
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 13038 None 0 Rat Functional pEC50 = 4.2 4.2 -12 2
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 13038 None 0 Rat Functional pEC50 = 4.2 4.2 -12 2
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 13038 None 0 Rat Functional pEC50 = 4.2 4.2 -12 2
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 160402 None 0 Rat Functional pEC50 = 5.2 5.2 -21 3
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 160402 None 0 Rat Functional pEC50 = 5.2 5.2 -21 3
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 2290 None 30 Rat Functional pEC50 = 6.2 6.2 -5 11
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 2290 None 30 Rat Functional pEC50 = 6.2 6.2 -5 11
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 2290 None 30 Rat Functional pEC50 = 6.2 6.2 -5 11
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 155958 None 0 Human Functional pEC50 = 5.2 5.2 -3 4
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 155958 None 0 Human Functional pEC50 = 5.2 5.2 -3 4
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 33 None 30 Rat Functional pEC50 = 4.2 4.2 -17 14
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 33 None 30 Rat Functional pEC50 = 4.2 4.2 -17 14
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 33 None 30 Rat Functional pEC50 = 4.2 4.2 -17 14
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 119184 None 0 Rat Functional pEC50 = 5.2 5.2 -13 3
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 119184 None 0 Rat Functional pEC50 = 5.2 5.2 -13 3
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 156612 None 0 Human Functional pEC50 = 5.2 5.2 -40 3
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 156612 None 0 Human Functional pEC50 = 5.2 5.2 -40 3
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 155958 None 0 Human Functional pEC50 = 5.2 5.2 -3 4
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 155958 None 0 Human Functional pEC50 = 5.2 5.2 -3 4
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 2315 None 61 Rat Functional pEC50 = 4.2 4.2 -1148 17
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 2315 None 61 Rat Functional pEC50 = 4.2 4.2 -1148 17
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 2315 None 61 Rat Functional pEC50 = 4.2 4.2 -1148 17
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 2315 None 61 Rat Functional pEC50 = 4.2 4.2 -1148 17
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 2315 None 61 Rat Functional pEC50 = 4.2 4.2 -1148 17
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 2315 None 61 Rat Functional pEC50 = 4.2 4.2 -1148 17
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 2315 None 61 Rat Functional pEC50 = 4.2 4.2 -1148 17
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 7822 None 0 Human Functional pEC50 = 5.2 5.2 -2 8
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 7822 None 0 Human Functional pEC50 = 5.2 5.2 -2 8
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 7822 None 0 Rat Functional pEC50 = 5.2 5.2 -2 8
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 7822 None 0 Rat Functional pEC50 = 5.2 5.2 -2 8
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 158779 None 0 Human Functional pEC50 = 4.2 4.2 -15 3
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 158779 None 0 Human Functional pEC50 = 4.2 4.2 -15 3
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 92914 None 6 Rat Functional pEC50 = 6.1 6.1 -18 3
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 92914 None 6 Rat Functional pEC50 = 6.1 6.1 -18 3
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 13360 None 0 Rat Functional pEC50 = 4.1 4.1 -9 3
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 13360 None 0 Rat Functional pEC50 = 4.1 4.1 -9 3
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 13360 None 0 Rat Functional pEC50 = 4.1 4.1 -9 3
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 159601 None 0 Human Functional pEC50 = 6.1 6.1 3 4
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 159601 None 0 Human Functional pEC50 = 6.1 6.1 3 4
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 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -1148 17
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 1939 None 3 Human Functional pEC50 = 4.1 4.1 1 2
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 1939 None 3 Human Functional pEC50 = 4.1 4.1 1 2
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 1939 None 3 Human Functional pEC50 = 4.1 4.1 1 2
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 2315 None 61 Rat Functional pEC50 = 4.1 4.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 4.1 4.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 4.1 4.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 4.1 4.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 4.1 4.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 4.1 4.1 -1148 17
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 2315 None 61 Rat Functional pEC50 = 4.1 4.1 -1148 17
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 158821 None 0 Human Functional pEC50 = 5.1 5.1 -15 3
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 158821 None 0 Human Functional pEC50 = 5.1 5.1 -15 3
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 14191 None 0 Rat Functional pEC50 = 4.1 4.1 -14 3
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 14191 None 0 Rat Functional pEC50 = 4.1 4.1 -14 3
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 14191 None 0 Rat Functional pEC50 = 4.1 4.1 -14 3
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 5584 None 0 Rat Functional pEC50 = 5.1 5.1 -4 4
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 5584 None 0 Rat Functional pEC50 = 5.1 5.1 -4 4
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 160870 None 0 Rat Functional pEC50 = 5.1 5.1 -17 3
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 160870 None 0 Rat Functional pEC50 = 5.1 5.1 -17 3
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 7821 None 5 Rat Functional pEC50 = 4 4.0 -5 3
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 7821 None 5 Rat Functional pEC50 = 4 4.0 -5 3
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 7821 None 5 Rat Functional pEC50 = 4 4.0 -5 3
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 200649 None 0 Human Functional pIC50 = 5 5.0 - 1
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 200649 None 0 Human Functional pIC50 = 5 5.0 - 1
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 199384 None 1 Human Functional pIC50 = 5.0 5.0 - 1
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 199384 None 1 Human Functional pIC50 = 5.0 5.0 - 1
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 199241 None 0 Human Functional pIC50 = 4.9 4.9 - 1
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 199241 None 0 Human Functional pIC50 = 4.9 4.9 - 1
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 90084 None 2 Human Functional pIC50 = 5.9 5.9 -12589 4
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 90084 None 2 Human Functional pIC50 = 5.9 5.9 -12589 4
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 90089 None 0 Human Functional pIC50 = 5.7 5.7 -154 4
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 90089 None 0 Human Functional pIC50 = 5.7 5.7 -154 4
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 201348 None 0 Human Functional pIC50 = 4.7 4.7 - 1
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 201348 None 0 Human Functional pIC50 = 4.7 4.7 - 1
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 210568 None 8 Human Functional pIC50 = 4.6 4.6 - 1
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 210568 None 8 Human Functional pIC50 = 4.6 4.6 - 1
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 199725 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 199725 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 90085 None 1 Human Functional pIC50 = 6.6 6.6 -208 4
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 90085 None 1 Human Functional pIC50 = 6.6 6.6 -208 4
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 90087 None 1 Human Functional pIC50 = 5.5 5.5 -467 3
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 90087 None 1 Human Functional pIC50 = 5.5 5.5 -467 3
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 149715 None 0 Human Functional pIC50 = 5.5 5.5 -72 5
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 149715 None 0 Human Functional pIC50 = 5.5 5.5 -72 5
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 201088 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 201088 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 200875 None 2 Human Functional pIC50 = 5.4 5.4 - 1
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 200875 None 2 Human Functional pIC50 = 5.4 5.4 - 1
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 199599 None 0 Human Functional pIC50 = 4.4 4.4 - 1
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 199599 None 0 Human Functional pIC50 = 4.4 4.4 - 1
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 100241 None 37 Human Functional pIC50 = 5.4 5.4 - 1
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 100241 None 37 Human Functional pIC50 = 5.4 5.4 - 1
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 183759 None 14 Human Functional pIC50 = 5.4 5.4 -1023 4
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 183759 None 14 Human Functional pIC50 = 5.4 5.4 -1023 4
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 183759 None 14 Human Functional pIC50 = 5.4 5.4 -1023 4
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 199685 None 13 Human Functional pIC50 = 5.4 5.4 7 2
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 199685 None 13 Human Functional pIC50 = 5.4 5.4 7 2
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 100680 None 22 Human Functional pIC50 = 5.4 5.4 - 1
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 100680 None 22 Human Functional pIC50 = 5.4 5.4 - 1
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 199447 None 0 Human Functional pIC50 = 4.3 4.3 - 1
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 199447 None 0 Human Functional pIC50 = 4.3 4.3 - 1
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 199421 None 9 Human Functional pIC50 = 5.2 5.2 - 1
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 199421 None 9 Human Functional pIC50 = 5.2 5.2 - 1
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 209380 None 58 Human Functional pIC50 = 5.2 5.2 -26 35
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 209380 None 58 Human Functional pIC50 = 5.2 5.2 -26 35
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 209380 None 58 Human Functional pIC50 = 5.2 5.2 -26 35
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 199240 None 24 Human Functional pIC50 = 4.2 4.2 - 1
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 199240 None 24 Human Functional pIC50 = 4.2 4.2 - 1
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 84716 None 42 Human Functional pIC50 = 4.1 4.1 - 1
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 84716 None 42 Human Functional pIC50 = 4.1 4.1 - 1
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 199347 None 45 Human Functional pIC50 = 6.1 6.1 -190 2
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 199347 None 45 Human Functional pIC50 = 6.1 6.1 -190 2
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 200893 None 33 Human Functional pIC50 = 5.1 5.1 - 1
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 200893 None 33 Human Functional pIC50 = 5.1 5.1 - 1
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 30 None 2 Human Functional pKi = 4.7 4.7 - 1
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 30 None 2 Human Functional pKi = 4.7 4.7 - 1
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 30 None 2 Human Functional pKi = 4.7 4.7 - 1
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 209061 None 1 Human Functional pKi = 5.6 5.6 - 0
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 209061 None 1 Human Functional pKi = 5.6 5.6 - 0
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 1539 None 42 Human Functional pKi = 5.5 5.5 -346 6
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 1539 None 42 Human Functional pKi = 5.5 5.5 -346 6
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 1539 None 42 Human Functional pKi = 5.5 5.5 -346 6
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 1539 None 42 Human Functional pKi = 5.5 5.5 -346 6
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 2315 None 61 Human Functional pKi = 4.4 4.4 -354 17
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 2315 None 61 Human Functional pKi = 4.4 4.4 -354 17
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 2315 None 61 Human Functional pKi = 4.4 4.4 -354 17
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 2315 None 61 Human Functional pKi = 4.4 4.4 -354 17
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 2315 None 61 Human Functional pKi = 4.4 4.4 -354 17
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 2315 None 61 Human Functional pKi = 4.4 4.4 -354 17
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 2315 None 61 Human Functional pKi = 4.4 4.4 -354 17
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 2421 None 36 Human Functional pKi = 6.4 6.4 -147 5
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 2421 None 36 Human Functional pKi = 6.4 6.4 -147 5
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 2421 None 36 Human Functional pKi = 6.4 6.4 -147 5
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 2073 None 26 Human Functional pKi = 5.3 5.3 -25 7
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 2073 None 26 Human Functional pKi = 5.3 5.3 -25 7
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 2073 None 26 Human Functional pKi = 5.3 5.3 -25 7
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 209295 None 1 Human Functional pKi = 5.3 5.3 - 0
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 209295 None 1 Human Functional pKi = 5.3 5.3 - 0
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 2290 None 30 Human Functional pKi = 5.2 5.2 -1 11
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 2290 None 30 Human Functional pKi = 5.2 5.2 -1 11
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 2290 None 30 Human Functional pKi = 5.2 5.2 -1 11
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 107054 None 0 Human Functional pKi = 4.2 4.2 - 1
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 107054 None 0 Human Functional pKi = 4.2 4.2 - 1
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 33 None 30 Human Functional pKi = 4.2 4.2 -11 14
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 33 None 30 Human Functional pKi = 4.2 4.2 -11 14
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 33 None 30 Human Functional pKi = 4.2 4.2 -11 14
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 2274 None 38 Human Functional pKi = 6.1 6.1 -2 8
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 2274 None 38 Human Functional pKi = 6.1 6.1 -2 8
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 2274 None 38 Human Functional pKi = 6.1 6.1 -2 8
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 2274 None 38 Human Functional pKi = 6.1 6.1 -2 8
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 2274 None 38 Human Functional pKi = 6.1 6.1 -2 8
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 2315 None 61 Rat Functional pEC50 = 8.3 8.3 -1148 17
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 2315 None 61 Rat Functional pEC50 = 8.3 8.3 -1148 17
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 2315 None 61 Rat Functional pEC50 = 8.3 8.3 -1148 17
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 2315 None 61 Rat Functional pEC50 = 8.3 8.3 -1148 17
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 2315 None 61 Rat Functional pEC50 = 8.3 8.3 -1148 17
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 2315 None 61 Rat Functional pEC50 = 8.3 8.3 -1148 17
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 2315 None 61 Rat Functional pEC50 = 8.3 8.3 -1148 17
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1310 2315 None 61 Human Functional pEC50 = 8.3 8.3 -354 17
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 2315 None 61 Human Functional pEC50 = 8.3 8.3 -354 17
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 2315 None 61 Human Functional pEC50 = 8.3 8.3 -354 17
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 2315 None 61 Human Functional pEC50 = 8.3 8.3 -354 17
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 2315 None 61 Human Functional pEC50 = 8.3 8.3 -354 17
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 2315 None 61 Human Functional pEC50 = 8.3 8.3 -354 17
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 2315 None 61 Human Functional pEC50 = 8.3 8.3 -354 17
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 2361 None 44 Rat Functional pEC50 = 8.3 8.3 -3 6
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 2361 None 44 Rat Functional pEC50 = 8.3 8.3 -3 6
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 2361 None 44 Rat Functional pEC50 = 8.3 8.3 -3 6
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 2361 None 44 Rat Functional pEC50 = 8.3 8.3 -3 6
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 2361 None 44 Rat Functional pEC50 = 8.3 8.3 -3 6
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 2361 None 44 Rat Functional pEC50 = 8.3 8.3 -3 6
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 2361 None 44 Human Functional pEC50 = 8.2 8.2 -1 6
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
4120 2361 None 44 Human Functional pEC50 = 8.2 8.2 -1 6
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
57689797 2361 None 44 Human Functional pEC50 = 8.2 8.2 -1 6
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
68841 2361 None 44 Human Functional pEC50 = 8.2 8.2 -1 6
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
CHEMBL284377 2361 None 44 Human Functional pEC50 = 8.2 8.2 -1 6
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
DB04522 2361 None 44 Human Functional pEC50 = 8.2 8.2 -1 6
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
3359 1939 None 3 Human Functional pEC50 = 4.1 4.1 1 2
UnclassifiedUnclassified
Guide to Pharmacology 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 8759641
4236420 1939 None 3 Human Functional pEC50 = 4.1 4.1 1 2
UnclassifiedUnclassified
Guide to Pharmacology 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 8759641
CHEMBL107768 1939 None 3 Human Functional pEC50 = 4.1 4.1 1 2
UnclassifiedUnclassified
Guide to Pharmacology 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 8759641
1436 30 None 2 Rat Functional pEC50 = 4.7 4.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O None
15508178 30 None 2 Rat Functional pEC50 = 4.7 4.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O None
CHEMBL60238 30 None 2 Rat Functional pEC50 = 4.7 4.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O None
1310 2315 None 61 Human Functional pEC50 = 4.8 4.8 -354 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
1369 2315 None 61 Human Functional pEC50 = 4.8 4.8 -354 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
33032 2315 None 61 Human Functional pEC50 = 4.8 4.8 -354 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
44272391 2315 None 61 Human Functional pEC50 = 4.8 4.8 -354 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
88747398 2315 None 61 Human Functional pEC50 = 4.8 4.8 -354 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
CHEMBL575060 2315 None 61 Human Functional pEC50 = 4.8 4.8 -354 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
DB00142 2315 None 61 Human Functional pEC50 = 4.8 4.8 -354 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
1416 3093 None 32 Rat Functional pEC50 = 4.8 4.8 -6 4
UnclassifiedUnclassified
Guide to Pharmacology 294 2 2 4 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1 18593581
5866327 3093 None 32 Rat Functional pEC50 = 4.8 4.8 -6 4
UnclassifiedUnclassified
Guide to Pharmacology 294 2 2 4 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1 18593581
CHEMBL164770 3093 None 32 Rat Functional pEC50 = 4.8 4.8 -6 4
UnclassifiedUnclassified
Guide to Pharmacology 294 2 2 4 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1 18593581
1368 2290 None 30 Rat Functional pEC50 = 5.2 5.2 -5 11
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 2290 None 30 Rat Functional pEC50 = 5.2 5.2 -5 11
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 2290 None 30 Rat Functional pEC50 = 5.2 5.2 -5 11
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 2367 None 9 Human Functional pEC50 = 5.4 5.4 -38 8
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 2367 None 9 Human Functional pEC50 = 5.4 5.4 -38 8
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 2367 None 9 Human Functional pEC50 = 5.4 5.4 -38 8
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 2079 None 36 Human Functional pEC50 = 5.4 5.4 -114 7
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 2079 None 36 Human Functional pEC50 = 5.4 5.4 -114 7
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 2079 None 36 Human Functional pEC50 = 5.4 5.4 -114 7
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 2366 None 7 Rat Functional pEC50 = 5.8 5.8 -8 8
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 2366 None 7 Rat Functional pEC50 = 5.8 5.8 -8 8
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 2366 None 7 Rat Functional pEC50 = 5.8 5.8 -8 8
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 2290 None 30 Human Functional pEC50 = 6.2 6.2 -1 11
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 2290 None 30 Human Functional pEC50 = 6.2 6.2 -1 11
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 2290 None 30 Human Functional pEC50 = 6.2 6.2 -1 11
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 2361 None 44 Human Functional pEC50 = 6.4 6.4 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
4120 2361 None 44 Human Functional pEC50 = 6.4 6.4 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
57689797 2361 None 44 Human Functional pEC50 = 6.4 6.4 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
68841 2361 None 44 Human Functional pEC50 = 6.4 6.4 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
CHEMBL284377 2361 None 44 Human Functional pEC50 = 6.4 6.4 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
DB04522 2361 None 44 Human Functional pEC50 = 6.4 6.4 -1 6
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
1398 365 None 0 Rat Functional pEC50 None 4.1 4.1 -15 2
UnclassifiedUnclassified
Guide to Pharmacology 199 4 4 4 -1.1 OC(=O)C(COP(=O)(O)O)(N)C 12769621
3964633 365 None 0 Rat Functional pEC50 None 4.1 4.1 -15 2
UnclassifiedUnclassified
Guide to Pharmacology 199 4 4 4 -1.1 OC(=O)C(COP(=O)(O)O)(N)C 12769621
CHEMBL1437137 365 None 0 Rat Functional pEC50 None 4.1 4.1 -15 2
UnclassifiedUnclassified
Guide to Pharmacology 199 4 4 4 -1.1 OC(=O)C(COP(=O)(O)O)(N)C 12769621
104766 33 None 30 Rat Functional pEC50 None 4.2 4.2 -17 14
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O None
1365 33 None 30 Rat Functional pEC50 None 4.2 4.2 -17 14
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O None
CHEMBL34453 33 None 30 Rat Functional pEC50 None 4.2 4.2 -17 14
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O None
1310 2315 None 61 Rat Functional pEC50 None 4.4 4.4 -1148 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
1369 2315 None 61 Rat Functional pEC50 None 4.4 4.4 -1148 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
33032 2315 None 61 Rat Functional pEC50 None 4.4 4.4 -1148 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
44272391 2315 None 61 Rat Functional pEC50 None 4.4 4.4 -1148 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
88747398 2315 None 61 Rat Functional pEC50 None 4.4 4.4 -1148 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
CHEMBL575060 2315 None 61 Rat Functional pEC50 None 4.4 4.4 -1148 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
DB00142 2315 None 61 Rat Functional pEC50 None 4.4 4.4 -1148 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
1378 2417 None 39 Human Functional pEC50 None 4.5 4.5 -4265 14
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 2417 None 39 Human Functional pEC50 None 4.5 4.5 -4265 14
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 2417 None 39 Human Functional pEC50 None 4.5 4.5 -4265 14
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 2417 None 39 Human Functional pEC50 None 4.5 4.5 -4265 14
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 33 None 30 Human Functional pEC50 None 4.7 4.7 -11 14
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 9144651
1365 33 None 30 Human Functional pEC50 None 4.7 4.7 -11 14
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 9144651
CHEMBL34453 33 None 30 Human Functional pEC50 None 4.7 4.7 -11 14
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 9144651
1310 2315 None 61 Human Functional pEC50 None 5.2 5.2 -354 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
1369 2315 None 61 Human Functional pEC50 None 5.2 5.2 -354 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
33032 2315 None 61 Human Functional pEC50 None 5.2 5.2 -354 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
44272391 2315 None 61 Human Functional pEC50 None 5.2 5.2 -354 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
88747398 2315 None 61 Human Functional pEC50 None 5.2 5.2 -354 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
CHEMBL575060 2315 None 61 Human Functional pEC50 None 5.2 5.2 -354 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
DB00142 2315 None 61 Human Functional pEC50 None 5.2 5.2 -354 17
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
1406 2073 None 26 Human Functional pEC50 None 5.3 5.3 -25 7
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10336568
1406 2073 None 26 Human Functional pEC50 None 5.3 5.3 -25 7
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 11166323
4545574 2073 None 26 Human Functional pEC50 None 5.3 5.3 -25 7
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10336568
4545574 2073 None 26 Human Functional pEC50 None 5.3 5.3 -25 7
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 11166323
CHEMBL277475 2073 None 26 Human Functional pEC50 None 5.3 5.3 -25 7
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10336568
CHEMBL277475 2073 None 26 Human Functional pEC50 None 5.3 5.3 -25 7
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 11166323
1377 1340 None 23 Rat Functional pEC50 None 5.6 5.6 -60 8
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 1340 None 23 Rat Functional pEC50 None 5.6 5.6 -60 8
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 1340 None 23 Rat Functional pEC50 None 5.6 5.6 -60 8
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 2274 None 38 Human Functional pEC50 None 7 7.0 -2 8
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11166323
1410 2274 None 38 Human Functional pEC50 None 7 7.0 -2 8
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144651
1412 2274 None 38 Human Functional pEC50 None 7 7.0 -2 8
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11166323
1412 2274 None 38 Human Functional pEC50 None 7 7.0 -2 8
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144651
179394 2274 None 38 Human Functional pEC50 None 7 7.0 -2 8
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11166323
179394 2274 None 38 Human Functional pEC50 None 7 7.0 -2 8
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144651
57689795 2274 None 38 Human Functional pEC50 None 7 7.0 -2 8
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11166323
57689795 2274 None 38 Human Functional pEC50 None 7 7.0 -2 8
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144651
CHEMBL33567 2274 None 38 Human Functional pEC50 None 7 7.0 -2 8
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11166323
CHEMBL33567 2274 None 38 Human Functional pEC50 None 7 7.0 -2 8
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144651
1414 2459 None 0 Rat Functional pIC50 = 3.5 3.5 -707 2
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 12769621
1795545 2459 None 0 Rat Functional pIC50 = 3.5 3.5 -707 2
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 12769621
CHEMBL1488784 2459 None 0 Rat Functional pIC50 = 3.5 3.5 -707 2
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 12769621
1415 2614 None 31 Human Functional pIC50 None 3.3 3.3 -10 2
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C None
3972752 2614 None 31 Human Functional pIC50 None 3.3 3.3 -10 2
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C None
CHEMBL86508 2614 None 31 Human Functional pIC50 None 3.3 3.3 -10 2
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C None
1408 265 None 24 Rat Functional pIC50 None 4.7 4.7 -3 7
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 265 None 24 Rat Functional pIC50 None 4.7 4.7 -3 7
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 265 None 24 Rat Functional pIC50 None 4.7 4.7 -3 7
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 265 None 24 Rat Functional pIC50 None 4.7 4.7 -3 7
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 1539 None 42 Human Functional pIC50 None 5.5 5.5 -346 6
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 1539 None 42 Human Functional pIC50 None 5.5 5.5 -346 6
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 1539 None 42 Human Functional pIC50 None 5.5 5.5 -346 6
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 1539 None 42 Human Functional pIC50 None 5.5 5.5 -346 6
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 2421 None 36 Human Functional pIC50 None 6.4 6.4 -147 5
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 2421 None 36 Human Functional pIC50 None 6.4 6.4 -147 5
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 2421 None 36 Human Functional pIC50 None 6.4 6.4 -147 5
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


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
71681824 90090 None 0 Human Binding pEC50 = 4.9 4.9 - 0
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 90090 None 0 Human Binding pEC50 = 4.9 4.9 - 0
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 90094 None 0 Human Binding pEC50 = 5.9 5.9 - 2
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 90094 None 0 Human Binding pEC50 = 5.9 5.9 - 2
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 90096 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 90096 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 90096 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 2315 None 61 Rat Binding pEC50 = 4.8 4.8 -43 18
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 2315 None 61 Rat Binding pEC50 = 4.8 4.8 -43 18
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 2315 None 61 Rat Binding pEC50 = 4.8 4.8 -43 18
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 2315 None 61 Rat Binding pEC50 = 4.8 4.8 -43 18
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 2315 None 61 Rat Binding pEC50 = 4.8 4.8 -43 18
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 2315 None 61 Rat Binding pEC50 = 4.8 4.8 -43 18
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 2315 None 61 Rat Binding pEC50 = 4.8 4.8 -43 18
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 207381 None 56 Rat Binding pEC50 = 4.7 4.7 -1 5
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 207381 None 56 Rat Binding pEC50 = 4.7 4.7 -1 5
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 207381 None 56 Rat Binding pEC50 = 4.7 4.7 -1 5
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 2361 None 44 Rat Binding pEC50 = 5.6 5.6 - 1
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 2361 None 44 Rat Binding pEC50 = 5.6 5.6 - 1
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 2361 None 44 Rat Binding pEC50 = 5.6 5.6 - 1
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 2361 None 44 Rat Binding pEC50 = 5.6 5.6 - 1
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 2361 None 44 Rat Binding pEC50 = 5.6 5.6 - 1
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 2361 None 44 Rat Binding pEC50 = 5.6 5.6 - 1
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 99919 None 47 Human Binding pEC50 = 6.6 6.6 -2 7
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 99919 None 47 Human Binding pEC50 = 6.6 6.6 -2 7
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 90095 None 0 Human Binding pEC50 = 5.5 5.5 - 2
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 90095 None 0 Human Binding pEC50 = 5.5 5.5 - 2
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 1539 None 42 Human Binding pEC50 = 5.5 5.5 -162 6
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 1539 None 42 Human Binding pEC50 = 5.5 5.5 -162 6
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 1539 None 42 Human Binding pEC50 = 5.5 5.5 -162 6
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 1539 None 42 Human Binding pEC50 = 5.5 5.5 -162 6
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 90086 None 1 Human Binding pEC50 = 5.4 5.4 - 1
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 90086 None 1 Human Binding pEC50 = 5.4 5.4 - 1
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 2315 None 61 Human Binding pEC50 = 5.3 5.3 -85 18
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 2315 None 61 Human Binding pEC50 = 5.3 5.3 -85 18
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 2315 None 61 Human Binding pEC50 = 5.3 5.3 -85 18
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 2315 None 61 Human Binding pEC50 = 5.3 5.3 -85 18
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 2315 None 61 Human Binding pEC50 = 5.3 5.3 -85 18
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 2315 None 61 Human Binding pEC50 = 5.3 5.3 -85 18
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 2315 None 61 Human Binding pEC50 = 5.3 5.3 -85 18
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 101285 None 2 Human Binding pEC50 = 5.3 5.3 - 0
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 101285 None 2 Human Binding pEC50 = 5.3 5.3 - 0
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 2274 None 38 Human Binding pEC50 = 7.3 7.3 -7 6
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 2274 None 38 Human Binding pEC50 = 7.3 7.3 -7 6
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 2274 None 38 Human Binding pEC50 = 7.3 7.3 -7 6
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 2274 None 38 Human Binding pEC50 = 7.3 7.3 -7 6
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 2274 None 38 Human Binding pEC50 = 7.3 7.3 -7 6
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 2274 None 38 Rat Binding pEC50 = 6.2 6.2 - 6
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 2274 None 38 Rat Binding pEC50 = 6.2 6.2 - 6
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 2274 None 38 Rat Binding pEC50 = 6.2 6.2 - 6
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 2274 None 38 Rat Binding pEC50 = 6.2 6.2 - 6
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 2274 None 38 Rat Binding pEC50 = 6.2 6.2 - 6
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 107054 None 0 Rat Binding pEC50 = 4.2 4.2 - 1
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 107054 None 0 Rat Binding pEC50 = 4.2 4.2 - 1
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 90092 None 0 Human Binding pEC50 = 5.2 5.2 - 0
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 90092 None 0 Human Binding pEC50 = 5.2 5.2 - 0
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 90093 None 0 Human Binding pEC50 = 6.2 6.2 - 2
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 90093 None 0 Human Binding pEC50 = 6.2 6.2 - 2
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 2422 None 14 Human Binding pEC50 = 5.1 5.1 - 2
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 2422 None 14 Human Binding pEC50 = 5.1 5.1 - 2
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 2422 None 14 Human Binding pEC50 = 5.1 5.1 - 2
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 90088 None 0 Human Binding pEC50 = 6.1 6.1 - 0
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 90088 None 0 Human Binding pEC50 = 6.1 6.1 - 0
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 33 None 30 Human Binding pEC50 = 4.1 4.1 -38 11
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 33 None 30 Human Binding pEC50 = 4.1 4.1 -38 11
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 33 None 30 Human Binding pEC50 = 4.1 4.1 -38 11
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 1939 None 3 Rat Binding pEC50 = 4.1 4.1 - 0
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 1939 None 3 Rat Binding pEC50 = 4.1 4.1 - 0
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 1939 None 3 Rat Binding pEC50 = 4.1 4.1 - 0
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 2274 None 38 Rat Binding pEC50 = 6.1 6.1 - 6
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 2274 None 38 Rat Binding pEC50 = 6.1 6.1 - 6
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 2274 None 38 Rat Binding pEC50 = 6.1 6.1 - 6
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 2274 None 38 Rat Binding pEC50 = 6.1 6.1 - 6
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 2274 None 38 Rat Binding pEC50 = 6.1 6.1 - 6
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 126844 None 0 Human Binding pEC50 = 5.0 5.0 - 2
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 126844 None 0 Human Binding pEC50 = 5.0 5.0 - 2
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 90091 None 1 Human Binding pEC50 = 5.0 5.0 - 2
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 90091 None 1 Human Binding pEC50 = 5.0 5.0 - 2
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 2417 None 39 Rat Binding pIC50 = 5.9 5.9 - 10
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 2417 None 39 Rat Binding pIC50 = 5.9 5.9 - 10
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 2417 None 39 Rat Binding pIC50 = 5.9 5.9 - 10
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 2417 None 39 Rat Binding pIC50 = 5.9 5.9 - 10
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 2529 None 15 Rat Binding pIC50 = 5.7 5.7 - 5
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 2529 None 15 Rat Binding pIC50 = 5.7 5.7 - 5
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 2529 None 15 Rat Binding pIC50 = 5.7 5.7 - 5
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 142777 None 16 Human Binding pIC50 = 5.0 5.0 - 1
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 142777 None 16 Human Binding pIC50 = 5.0 5.0 - 1
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
89554892 150689 None 0 Human Binding pIC50 = 5.0 5.0 - 1
Binding affinity to mGluR6 (unknown origin) by FLIPR assayBinding affinity to mGluR6 (unknown origin) by FLIPR assay
ChEMBL 416 6 1 5 4.0 COc1ccc(-c2cc(C(N)=O)nc3cc(CCc4cnc(C)nc4)ccc23)c(F)c1 10.1021/acsmedchemlett.3c00175
CHEMBL3955188 150689 None 0 Human Binding pIC50 = 5.0 5.0 - 1
Binding affinity to mGluR6 (unknown origin) by FLIPR assayBinding affinity to mGluR6 (unknown origin) by FLIPR assay
ChEMBL 416 6 1 5 4.0 COc1ccc(-c2cc(C(N)=O)nc3cc(CCc4cnc(C)nc4)ccc23)c(F)c1 10.1021/acsmedchemlett.3c00175
12310764 1970 Functional 46 Human Binding pKi = 5 5.0 -14 8
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
1233 1970 Functional 46 Human Binding pKi = 5 5.0 -14 8
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
1371 1970 Functional 46 Human Binding pKi = 5 5.0 -14 8
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
CHEMBL284895 1970 Functional 46 Human Binding pKi = 5 5.0 -14 8
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
1310 2315 Functional 61 Human Binding pKi = 5 5.0 -85 18
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1310 2315 Functional 61 Rat Binding pKi = 5 5.0 -43 18
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 2315 Functional 61 Human Binding pKi = 5 5.0 -85 18
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 2315 Functional 61 Rat Binding pKi = 5 5.0 -43 18
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 2315 Functional 61 Human Binding pKi = 5 5.0 -85 18
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 2315 Functional 61 Rat Binding pKi = 5 5.0 -43 18
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 2315 Functional 61 Human Binding pKi = 5 5.0 -85 18
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 2315 Functional 61 Rat Binding pKi = 5 5.0 -43 18
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 2315 Functional 61 Human Binding pKi = 5 5.0 -85 18
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 2315 Functional 61 Rat Binding pKi = 5 5.0 -43 18
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 2315 Functional 61 Human Binding pKi = 5 5.0 -85 18
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 2315 Functional 61 Rat Binding pKi = 5 5.0 -43 18
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 2315 Functional 61 Human Binding pKi = 5 5.0 -85 18
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 2315 Functional 61 Rat Binding pKi = 5 5.0 -43 18
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1370 3263 Functional 42 Human Binding pKi = 5 5.0 -602 8
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
1372 3263 Functional 42 Human Binding pKi = 5 5.0 -602 8
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
40539 3263 Functional 42 Human Binding pKi = 5 5.0 -602 8
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
6971145 3263 Functional 42 Human Binding pKi = 5 5.0 -602 8
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
CHEMBL279956 3263 Functional 42 Human Binding pKi = 5 5.0 -602 8
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
DB02999 3263 Functional 42 Human Binding pKi = 5 5.0 -602 8
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
128563 3464 Functional 24 Human Binding pKi = 5 5.0 -2344 41
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 3464 Functional 24 Human Binding pKi = 5 5.0 -2344 41
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 3464 Functional 24 Human Binding pKi = 5 5.0 -2344 41
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 3464 Functional 24 Human Binding pKi = 5 5.0 -2344 41
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 27120 Functional 13 Rat Binding pKi = 5 5.0 -38 42
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 27120 Functional 13 Rat Binding pKi = 5 5.0 -38 42
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
446220 133590 Functional 7 Rat Binding pKi = 5 5.0 -1778 45
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 133590 Functional 7 Rat Binding pKi = 5 5.0 -1778 45
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 204731 Functional 11 Rat Binding pKi = 5 5.0 -1949 44
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 204731 Functional 11 Rat Binding pKi = 5 5.0 -1949 44
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 204731 Functional 11 Rat Binding pKi = 5 5.0 -1949 44
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
139054390 207381 Functional 56 Rat Binding pKi = 5 5.0 -1 5
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O None
23327 207381 Functional 56 Rat Binding pKi = 5 5.0 -1 5
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O None
CHEMBL76232 207381 Functional 56 Rat Binding pKi = 5 5.0 -1 5
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O None
None 218660 Functional 0 Human Binding pKi = 5 5.0 -2 7
NoneNone
PDSP KiDatabase 173 2 3 3 -0.3 C1CC(CC1C(=O)O)(C(=O)O)N None
25137849 218667 Functional 0 Rat Binding pKi = 5 5.0 -4 40
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 218667 Functional 0 Rat Binding pKi = 5 5.0 -4 40
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 218803 Functional 0 Rat Binding pKi = 5 5.0 -1 39
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 218804 Functional 0 Rat Binding pKi = 5 5.0 -1 38
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 218812 Functional 0 Rat Binding pKi = 5 5.0 -13 40
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 218813 Functional 0 Rat Binding pKi = 5 5.0 -16 40
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 218976 Functional 0 Rat Binding pKi = 5 5.0 -1 2
NoneNone
PDSP KiDatabase 144 2 2 2 -0.7 CC(C(=O)NC)NC(=O)C None
None 218977 Functional 0 Rat Binding pKi = 5 5.0 -1 2
NoneNone
PDSP KiDatabase 161 5 3 3 -0.3 C(CC(C(=O)O)N)CC(=O)O None
None 218825 Functional 0 Human Binding pKi = 5.6 5.6 -2 4
NoneNone
PDSP KiDatabase 185 4 4 4 -1.5 C(C(C(=O)O)N)OP(=O)(O)O None
2207 99919 Functional 47 Rat Binding pKi = 6.4 6.4 -1 7
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
CHEMBL285843 99919 Functional 47 Rat Binding pKi = 6.4 6.4 -1 7
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
2207 99919 Functional 47 Human Binding pKi = 6.1 6.1 -2 7
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
CHEMBL285843 99919 Functional 47 Human Binding pKi = 6.1 6.1 -2 7
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None