Ligand source activities (1 row/activity)





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

Reference
ligand
Fold
selectivity
# Tested
GPCRs
Species

p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
AssayType

Assay
Description
Source

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

1410 9054 48 None -2 8 Human 6.0 pEC50 = 6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
1412 9054 48 None -2 8 Human 6.0 pEC50 = 6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
179394 9054 48 None -2 8 Human 6.0 pEC50 = 6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
57689795 9054 48 None -2 8 Human 6.0 pEC50 = 6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
CHEMBL33567 9054 48 None -2 8 Human 6.0 pEC50 = 6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
1410 9054 48 None -5 8 Rat 6.0 pEC50 = 6 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
1412 9054 48 None -5 8 Rat 6.0 pEC50 = 6 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
179394 9054 48 None -5 8 Rat 6.0 pEC50 = 6 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
57689795 9054 48 None -5 8 Rat 6.0 pEC50 = 6 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
CHEMBL33567 9054 48 None -5 8 Rat 6.0 pEC50 = 6 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
2207 106641 63 None -194 4 Rat 6.0 pEC50 = 6 Functional
Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O 10.1016/S0960-894X(97)00068-1
CHEMBL285843 106641 63 None -194 4 Rat 6.0 pEC50 = 6 Functional
Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O 10.1016/S0960-894X(97)00068-1
10385210 19804 0 None -2 3 Rat 4.0 pEC50 = 4 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 309 5 3 6 0.0 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc([N+](=O)[O-])c2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1189910 19804 0 None -2 3 Rat 4.0 pEC50 = 4 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 309 5 3 6 0.0 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc([N+](=O)[O-])c2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL539760 19804 0 None -2 3 Rat 4.0 pEC50 = 4 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 309 5 3 6 0.0 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc([N+](=O)[O-])c2)C1 10.1016/s0960-894x(01)00329-8
137655963 165802 0 None -1 4 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)[C@@H](O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4096644 165802 0 None -1 4 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)[C@@H](O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
1443 8100 36 None -7 5 Rat 6.0 pEC50 = 6.0 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@@H](CCP(=O)(O)O)N nan
1550579 8100 36 None -7 5 Rat 6.0 pEC50 = 6.0 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@@H](CCP(=O)(O)O)N nan
CHEMBL1319383 8100 36 None -7 5 Rat 6.0 pEC50 = 6.0 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@@H](CCP(=O)(O)O)N nan
1408 7053 31 None -3 7 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/jm901523t
6604820 7053 31 None -3 7 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/jm901523t
CHEMBL285043 7053 31 None -3 7 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/jm901523t
CHEMBL288635 7053 31 None -3 7 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/jm901523t
137650519 164124 0 None 1 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)C(O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4077705 164124 0 None 1 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)C(O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
137645989 164473 0 None -1 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 364 8 5 8 0.4 COc1cc([C@@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
CHEMBL4081842 164473 0 None -1 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 364 8 5 8 0.4 COc1cc([C@@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
46197778 14990 0 None 1 5 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 237 6 4 4 -0.3 N[C@@H](CCP(=O)(O)/C=C/C(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1092243 14990 0 None 1 5 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 237 6 4 4 -0.3 N[C@@H](CCP(=O)(O)/C=C/C(=O)O)C(=O)O 10.1021/jm901523t
1408 7053 31 None -2 7 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/acs.jmedchem.7b01438
6604820 7053 31 None -2 7 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL285043 7053 31 None -2 7 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL288635 7053 31 None -2 7 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/acs.jmedchem.7b01438
57765622 162883 0 None -20 3 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4063142 162883 0 None -20 3 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
10176324 121605 1 None -151 4 Rat 5.9 pEC50 = 5.9 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 173 3 3 3 -0.6 C[C@H]1[C@H](C(=O)O)[C@H]1[C@H](N)C(=O)O 10.1021/jm030967o
CHEMBL334160 121605 1 None -151 4 Rat 5.9 pEC50 = 5.9 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 173 3 3 3 -0.6 C[C@H]1[C@H](C(=O)O)[C@H]1[C@H](N)C(=O)O 10.1021/jm030967o
44406220 78948 1 None -1 2 Rat 4.9 pEC50 = 4.9 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 195 3 4 3 -1.0 N[C@H](C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O 10.1016/j.bmcl.2005.09.014
CHEMBL197976 78948 1 None -1 2 Rat 4.9 pEC50 = 4.9 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 195 3 4 3 -1.0 N[C@H](C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O 10.1016/j.bmcl.2005.09.014
11708219 176151 0 None -1 2 Rat 4.9 pEC50 = 4.9 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 195 3 4 3 -1.0 NC(C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O 10.1016/j.bmc.2007.02.040
CHEMBL442076 176151 0 None -1 2 Rat 4.9 pEC50 = 4.9 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 195 3 4 3 -1.0 NC(C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O 10.1016/j.bmc.2007.02.040
122197960 167690 0 None -12 2 Rat 4.9 pEC50 = 4.9 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 331 9 4 5 0.7 N[C@H](CCP(=O)(O)Cc1ccc(OCC(=O)O)cc1)C(=O)O nan
CHEMBL4115286 167690 0 None -12 2 Rat 4.9 pEC50 = 4.9 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 331 9 4 5 0.7 N[C@H](CCP(=O)(O)Cc1ccc(OCC(=O)O)cc1)C(=O)O nan
44361401 38115 0 None -33 5 Rat 6.8 pEC50 = 6.8 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 175 3 4 4 -1.9 N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O 10.1021/jm030967o
CHEMBL140197 38115 0 None -33 5 Rat 6.8 pEC50 = 6.8 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 175 3 4 4 -1.9 N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O 10.1021/jm030967o
46898088 9145 6 None -11 8 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
6739 9145 6 None -11 8 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
CHEMBL3114672 9145 6 None -11 8 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
127030386 145819 0 None -7 3 Rat 4.8 pEC50 = 4.8 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 217 5 4 4 -1.0 N[C@@H](C[C@@]1(C(=O)O)C[C@@H]1C(=O)O)C(=O)O 10.1021/acs.jmedchem.5b01333
CHEMBL3786026 145819 0 None -7 3 Rat 4.8 pEC50 = 4.8 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 217 5 4 4 -1.0 N[C@@H](C[C@@]1(C(=O)O)C[C@@H]1C(=O)O)C(=O)O 10.1021/acs.jmedchem.5b01333
57765535 164583 0 None -5 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 352 7 4 6 1.3 N[C@@H](CCP(=O)(O)C(O)c1ccc(Cl)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4083240 164583 0 None -5 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 352 7 4 6 1.3 N[C@@H](CCP(=O)(O)C(O)c1ccc(Cl)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
1408 7053 31 None -3 7 Rat 4.7 pEC50 = 4.7 Functional
Activity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cells
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2006.06.062
6604820 7053 31 None -3 7 Rat 4.7 pEC50 = 4.7 Functional
Activity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cells
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2006.06.062
CHEMBL285043 7053 31 None -3 7 Rat 4.7 pEC50 = 4.7 Functional
Activity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cells
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2006.06.062
CHEMBL288635 7053 31 None -3 7 Rat 4.7 pEC50 = 4.7 Functional
Activity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cells
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2006.06.062
122197942 166846 0 None -34 4 Rat 4.7 pEC50 = 4.7 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 375 9 5 6 0.8 Cc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(C)c1OCC(=O)O nan
CHEMBL4108384 166846 0 None -34 4 Rat 4.7 pEC50 = 4.7 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 375 9 5 6 0.8 Cc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(C)c1OCC(=O)O nan
1410 9054 48 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.5b01333
1412 9054 48 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.5b01333
179394 9054 48 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.5b01333
57689795 9054 48 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.5b01333
CHEMBL33567 9054 48 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.5b01333
60096231 164434 15 None -831 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human mGlu6 receptor expressed in hamster AV12 cells co-expressing rat EAAT1 assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu6 receptor expressed in hamster AV12 cells co-expressing rat EAAT1 assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 334 5 4 5 -0.1 COc1cccc(C(=O)N[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)c1 10.1021/acs.jmedchem.7b01481
CHEMBL4081453 164434 15 None -831 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human mGlu6 receptor expressed in hamster AV12 cells co-expressing rat EAAT1 assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu6 receptor expressed in hamster AV12 cells co-expressing rat EAAT1 assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 334 5 4 5 -0.1 COc1cccc(C(=O)N[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)c1 10.1021/acs.jmedchem.7b01481
16747847 92617 1 None -64 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at mGlu6 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu6 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 195 3 4 3 -1.0 N[C@@]1(C(=O)O)C[C@H]1CP(=O)(O)O 10.1021/jm070262c
CHEMBL229697 92617 1 None -64 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at mGlu6 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu6 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 195 3 4 3 -1.0 N[C@@]1(C(=O)O)C[C@H]1CP(=O)(O)O 10.1021/jm070262c
1310 9095 110 None -354 17 Human 4.7 pEC50 = 4.7 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
1369 9095 110 None -354 17 Human 4.7 pEC50 = 4.7 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
33032 9095 110 None -354 17 Human 4.7 pEC50 = 4.7 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
44272391 9095 110 None -354 17 Human 4.7 pEC50 = 4.7 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
88747398 9095 110 None -354 17 Human 4.7 pEC50 = 4.7 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
CHEMBL575060 9095 110 None -354 17 Human 4.7 pEC50 = 4.7 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
DB00142 9095 110 None -354 17 Human 4.7 pEC50 = 4.7 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
1436 6819 7 None - 1 Rat 4.7 pEC50 = 4.7 Functional
Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6
ChEMBL 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
15508178 6819 7 None - 1 Rat 4.7 pEC50 = 4.7 Functional
Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6
ChEMBL 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
CHEMBL60238 6819 7 None - 1 Rat 4.7 pEC50 = 4.7 Functional
Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6
ChEMBL 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
1410 9054 48 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070400y
1412 9054 48 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070400y
179394 9054 48 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070400y
57689795 9054 48 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070400y
CHEMBL33567 9054 48 None -5 8 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070400y
10091203 19723 0 None -1 3 Rat 4.7 pEC50 = 4.7 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(C(C(=O)O)c2ccccc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1189303 19723 0 None -1 3 Rat 4.7 pEC50 = 4.7 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(C(C(=O)O)c2ccccc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL538489 19723 0 None -1 3 Rat 4.7 pEC50 = 4.7 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(C(C(=O)O)c2ccccc2)C1 10.1016/s0960-894x(01)00329-8
137644345 164897 0 None -3 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 303 7 4 5 0.8 COc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1 10.1021/acs.jmedchem.7b01438
CHEMBL4086929 164897 0 None -3 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 303 7 4 5 0.8 COc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1 10.1021/acs.jmedchem.7b01438
1410 9054 48 None -2 8 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
1412 9054 48 None -2 8 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
179394 9054 48 None -2 8 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
57689795 9054 48 None -2 8 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
CHEMBL33567 9054 48 None -2 8 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
137640190 163733 0 None -2 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)[C@H](O)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4072781 163733 0 None -2 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)[C@H](O)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
124425164 164794 0 None 1 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 364 8 5 8 0.4 COc1cc([C@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
CHEMBL4085558 164794 0 None 1 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 364 8 5 8 0.4 COc1cc([C@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
10198133 213287 12 None -630 4 Human 5.6 pEC50 = 5.6 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm980616n
CHEMBL8839 213287 12 None -630 4 Human 5.6 pEC50 = 5.6 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm980616n
122197958 167303 0 None -7 4 Rat 5.6 pEC50 = 5.6 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 383 9 5 6 0.5 N[C@H](CCP(=O)(O)C(O)c1cc(F)c(OCC(=O)O)c(F)c1)C(=O)O nan
CHEMBL4112299 167303 0 None -7 4 Rat 5.6 pEC50 = 5.6 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 383 9 5 6 0.5 N[C@H](CCP(=O)(O)C(O)c1cc(F)c(OCC(=O)O)c(F)c1)C(=O)O nan
57765613 165269 0 None -19 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 336 7 4 6 0.8 N[C@@H](CCP(=O)(O)C(O)c1ccc(F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4091029 165269 0 None -19 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 336 7 4 6 0.8 N[C@@H](CCP(=O)(O)C(O)c1ccc(F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
58058356 165573 0 None -5 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 350 7 6 8 0.1 N[C@@H](CCP(=O)(O)C(O)c1cc(O)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4094241 165573 0 None -5 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 350 7 6 8 0.1 N[C@@H](CCP(=O)(O)C(O)c1cc(O)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
6330803 98897 10 None -15 3 Rat 4.6 pEC50 = 4.6 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 167 4 3 3 -0.7 N[C@@H](CC[PH](=O)O)C(=O)O 10.1021/jm070400y
CHEMBL241972 98897 10 None -15 3 Rat 4.6 pEC50 = 4.6 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 167 4 3 3 -0.7 N[C@@H](CC[PH](=O)O)C(=O)O 10.1021/jm070400y
57765616 164197 0 None -7 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])c(C(F)(F)F)c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4078629 164197 0 None -7 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])c(C(F)(F)F)c1)C(=O)O 10.1021/acs.jmedchem.7b01438
1393 8321 64 None -346 6 Human 5.5 pEC50 = 5.5 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
1396 8321 64 None -346 6 Human 5.5 pEC50 = 5.5 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
213056 8321 64 None -346 6 Human 5.5 pEC50 = 5.5 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
CHEMBL8759 8321 64 None -346 6 Human 5.5 pEC50 = 5.5 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
24780225 162712 0 None -5 3 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 363 6 4 4 1.4 N[C@@H](CCP(=O)(O)C(O)c1c(F)c(F)c(F)c(F)c1F)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4061016 162712 0 None -5 3 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 363 6 4 4 1.4 N[C@@H](CCP(=O)(O)C(O)c1c(F)c(F)c(F)c(F)c1F)C(=O)O 10.1021/acs.jmedchem.7b01438
6348408 14592 1 None -2 8 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL1089515 14592 1 None -2 8 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
24780088 165688 0 None -3 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 317 7 5 5 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(=O)O)cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4095462 165688 0 None -3 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 317 7 5 5 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(=O)O)cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
6348408 14592 1 None -2 8 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1089515 14592 1 None -2 8 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
1407 8860 42 None -114 7 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
16062593 8860 42 None -114 7 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL143210 8860 42 None -114 7 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
46898088 9145 6 None -11 8 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
6739 9145 6 None -11 8 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
CHEMBL3114672 9145 6 None -11 8 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
58058372 162976 0 None -5 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 302 7 3 5 1.2 N[C@@H](CCP(=O)(O)Cc1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4064187 162976 0 None -5 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 302 7 3 5 1.2 N[C@@H](CCP(=O)(O)Cc1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
137642874 164813 0 None -10 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)[C@@H](O)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4085750 164813 0 None -10 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)[C@@H](O)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
3756397 15086 2 None -4 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 NC(CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
4041087 15086 2 None -4 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 NC(CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1092727 15086 2 None -4 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 NC(CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
1410 9054 48 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
1412 9054 48 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
179394 9054 48 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
57689795 9054 48 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
CHEMBL33567 9054 48 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
1410 9054 48 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
1412 9054 48 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
179394 9054 48 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
57689795 9054 48 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
CHEMBL33567 9054 48 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
1410 9054 48 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
1412 9054 48 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
179394 9054 48 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
57689795 9054 48 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
CHEMBL33567 9054 48 None -5 8 Rat 6.5 pEC50 = 6.5 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
16747848 92290 0 None -1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu6 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 195 3 4 3 -1.0 N[C@@]1(C(=O)O)C[C@@H]1CP(=O)(O)O 10.1021/jm070262c
CHEMBL227288 92290 0 None -1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu6 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu6 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 195 3 4 3 -1.0 N[C@@]1(C(=O)O)C[C@@H]1CP(=O)(O)O 10.1021/jm070262c
53240406 130174 17 None -158 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant mGlu6 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu6 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616847 130174 17 None -158 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant mGlu6 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu6 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
1410 9054 48 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2015.04.043
1412 9054 48 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2015.04.043
179394 9054 48 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2015.04.043
57689795 9054 48 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2015.04.043
CHEMBL33567 9054 48 None -5 8 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2015.04.043
92044496 162746 0 None -20 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1csc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4061423 162746 0 None -20 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1csc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
137639752 163694 0 None -7 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)[C@H](O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4072316 163694 0 None -7 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)[C@H](O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
1407 8860 42 None -117 7 Rat 5.4 pEC50 = 5.4 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
16062593 8860 42 None -117 7 Rat 5.4 pEC50 = 5.4 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
CHEMBL143210 8860 42 None -117 7 Rat 5.4 pEC50 = 5.4 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
122197943 167359 0 None -7 3 Rat 5.4 pEC50 = 5.4 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 343 8 5 5 0.8 N[C@H](CCP(=O)(O)C(O)c1ccc(/C=C/C(=O)O)cc1)C(=O)O nan
CHEMBL4112699 167359 0 None -7 3 Rat 5.4 pEC50 = 5.4 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 343 8 5 5 0.8 N[C@H](CCP(=O)(O)C(O)c1ccc(/C=C/C(=O)O)cc1)C(=O)O nan
137647077 164776 0 None -2 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 348 8 4 7 0.7 COc1ccc([C@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
CHEMBL4085327 164776 0 None -2 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 348 8 4 7 0.7 COc1ccc([C@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
57765613 165269 0 None -19 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 336 7 4 6 0.8 N[C@@H](CCP(=O)(O)C(O)c1ccc(F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4091029 165269 0 None -19 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 336 7 4 6 0.8 N[C@@H](CCP(=O)(O)C(O)c1ccc(F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
57765525 166233 0 None -1 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 332 7 4 6 1.0 Cc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
CHEMBL4101241 166233 0 None -1 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 332 7 4 6 1.0 Cc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
1377 8122 26 None -60 8 Rat 4.4 pEC50 = 4.4 Functional
Metabotropic glutamate receptor 6 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
5310979 8122 26 None -60 8 Rat 4.4 pEC50 = 4.4 Functional
Metabotropic glutamate receptor 6 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
CHEMBL284193 8122 26 None -60 8 Rat 4.4 pEC50 = 4.4 Functional
Metabotropic glutamate receptor 6 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
10197984 9199 44 None -147 5 Human 6.4 pEC50 = 6.4 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
1394 9199 44 None -147 5 Human 6.4 pEC50 = 6.4 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
CHEMBL275079 9199 44 None -147 5 Human 6.4 pEC50 = 6.4 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
6706 9146 8 None -38 8 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
71041983 9146 8 None -38 8 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
CHEMBL3114673 9146 8 None -38 8 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
57765633 165191 0 None -8 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])s1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4090179 165191 0 None -8 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])s1)C(=O)O 10.1021/acs.jmedchem.7b01438
6706 9146 8 None -38 8 Rat 5.4 pEC50 = 5.4 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O nan
71041983 9146 8 None -38 8 Rat 5.4 pEC50 = 5.4 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O nan
CHEMBL3114673 9146 8 None -38 8 Rat 5.4 pEC50 = 5.4 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O nan
24779945 15013 0 None -12 3 Rat 4.4 pEC50 = 4.4 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 297 9 5 5 -0.8 N[C@@H](CCP(=O)(O)CC(CC(=O)O)C(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1092315 15013 0 None -12 3 Rat 4.4 pEC50 = 4.4 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 297 9 5 5 -0.8 N[C@@H](CCP(=O)(O)CC(CC(=O)O)C(=O)O)C(=O)O 10.1021/jm901523t
46197776 15128 0 None -4 3 Rat 4.4 pEC50 = 4.4 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 253 8 4 4 -0.1 N[C@@H](CCP(=O)(O)CCCC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1093009 15128 0 None -4 3 Rat 4.4 pEC50 = 4.4 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 253 8 4 4 -0.1 N[C@@H](CCP(=O)(O)CCCC(=O)O)C(=O)O 10.1021/jm901523t
137634883 162929 0 None -2 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 348 8 4 7 0.7 COc1ccc([C@@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
CHEMBL4063720 162929 0 None -2 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 348 8 4 7 0.7 COc1ccc([C@@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
57765536 165050 0 None -9 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4088782 165050 0 None -9 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
44406221 79451 1 None 1 2 Rat 4.3 pEC50 = 4.3 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 195 3 4 3 -1.0 N[C@H](C(=O)O)[C@@H]1C[C@H]1P(=O)(O)O 10.1016/j.bmcl.2005.09.014
CHEMBL199626 79451 1 None 1 2 Rat 4.3 pEC50 = 4.3 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 195 3 4 3 -1.0 N[C@H](C(=O)O)[C@@H]1C[C@H]1P(=O)(O)O 10.1016/j.bmcl.2005.09.014
1406 8854 38 None -23 7 Rat 5.3 pEC50 = 5.3 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm030967o
4545574 8854 38 None -23 7 Rat 5.3 pEC50 = 5.3 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm030967o
CHEMBL277475 8854 38 None -23 7 Rat 5.3 pEC50 = 5.3 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm030967o
122197935 166631 0 None -46 4 Rat 5.3 pEC50 = 5.3 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 377 10 5 7 0.2 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)ccc1OCC(=O)O nan
CHEMBL4106637 166631 0 None -46 4 Rat 5.3 pEC50 = 5.3 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 377 10 5 7 0.2 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)ccc1OCC(=O)O nan
127030387 145884 0 None -3 3 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 217 5 4 4 -1.0 N[C@@H](C[C@]1(C(=O)O)C[C@H]1C(=O)O)C(=O)O 10.1021/acs.jmedchem.5b01333
CHEMBL3786667 145884 0 None -3 3 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 217 5 4 4 -1.0 N[C@@H](C[C@]1(C(=O)O)C[C@H]1C(=O)O)C(=O)O 10.1021/acs.jmedchem.5b01333
16739372 153508 0 None 1 2 Rat 4.3 pEC50 = 4.3 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 271 4 4 3 0.4 NC(C(=O)O)[C@@H]1[C@@H](P(=O)(O)O)[C@H]1c1ccccc1 10.1016/j.bmc.2007.02.040
CHEMBL392420 153508 0 None 1 2 Rat 4.3 pEC50 = 4.3 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 271 4 4 3 0.4 NC(C(=O)O)[C@@H]1[C@@H](P(=O)(O)O)[C@H]1c1ccccc1 10.1016/j.bmc.2007.02.040
122197945 167008 0 None -4 3 Rat 4.3 pEC50 = 4.3 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 333 9 5 6 0.1 N[C@H](CCP(=O)(O)C(O)c1ccc(OCCO)cc1)C(=O)O nan
CHEMBL4109799 167008 0 None -4 3 Rat 4.3 pEC50 = 4.3 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 333 9 5 6 0.1 N[C@H](CCP(=O)(O)C(O)c1ccc(OCCO)cc1)C(=O)O nan
1410 9054 48 None -5 8 Rat 7.3 pEC50 = 7.3 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm030967o
1412 9054 48 None -5 8 Rat 7.3 pEC50 = 7.3 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm030967o
179394 9054 48 None -5 8 Rat 7.3 pEC50 = 7.3 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm030967o
57689795 9054 48 None -5 8 Rat 7.3 pEC50 = 7.3 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm030967o
CHEMBL33567 9054 48 None -5 8 Rat 7.3 pEC50 = 7.3 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm030967o
57765622 162883 0 None -20 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4063142 162883 0 None -20 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
44300256 20496 0 None - 1 Rat 4.2 pEC50 = 4.2 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc(C(=O)O)c2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1195052 20496 0 None - 1 Rat 4.2 pEC50 = 4.2 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc(C(=O)O)c2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL553774 20496 0 None - 1 Rat 4.2 pEC50 = 4.2 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc(C(=O)O)c2)C1 10.1016/s0960-894x(01)00329-8
44300587 19805 0 None -12 2 Rat 4.2 pEC50 = 4.2 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccc(C(=O)O)cc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1189911 19805 0 None -12 2 Rat 4.2 pEC50 = 4.2 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccc(C(=O)O)cc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL539761 19805 0 None -12 2 Rat 4.2 pEC50 = 4.2 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccc(C(=O)O)cc2)C1 10.1016/s0960-894x(01)00329-8
122197937 167087 0 None -21 3 Rat 5.2 pEC50 = 5.2 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 422 11 5 9 0.1 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc([N+](=O)[O-])c1OCC(=O)O nan
CHEMBL4110535 167087 0 None -21 3 Rat 5.2 pEC50 = 5.2 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 422 11 5 9 0.1 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc([N+](=O)[O-])c1OCC(=O)O nan
1368 9070 37 None -5 11 Rat 6.2 pEC50 = 6.2 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
5310956 9070 37 None -5 11 Rat 6.2 pEC50 = 6.2 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
CHEMBL280563 9070 37 None -5 11 Rat 6.2 pEC50 = 6.2 Functional
Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
46918015 162647 0 None -3 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4060360 162647 0 None -3 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
104766 6822 42 None -17 14 Rat 4.2 pEC50 = 4.2 Functional
Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
1365 6822 42 None -17 14 Rat 4.2 pEC50 = 4.2 Functional
Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
CHEMBL34453 6822 42 None -17 14 Rat 4.2 pEC50 = 4.2 Functional
Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
57519364 125898 0 None -13 3 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 213 3 4 3 -0.9 NC1(C(=O)O)CC1(F)CP(=O)(O)O 10.1016/j.bmcl.2015.04.043
CHEMBL3427499 125898 0 None -13 3 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 213 3 4 3 -0.9 NC1(C(=O)O)CC1(F)CP(=O)(O)O 10.1016/j.bmcl.2015.04.043
16061421 163300 0 None -40 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 308 7 4 7 0.3 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])o1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4067923 163300 0 None -40 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 308 7 4 7 0.3 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])o1)C(=O)O 10.1021/acs.jmedchem.7b01438
46918015 162647 0 None -3 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4060360 162647 0 None -3 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
1310 9095 110 None -1148 17 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
1369 9095 110 None -1148 17 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
33032 9095 110 None -1148 17 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
44272391 9095 110 None -1148 17 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
88747398 9095 110 None -1148 17 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
CHEMBL575060 9095 110 None -1148 17 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
DB00142 9095 110 None -1148 17 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
6348408 14592 1 None -2 8 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL1089515 14592 1 None -2 8 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
6348408 14592 1 None -2 8 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1089515 14592 1 None -2 8 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
137654697 165466 0 None -15 3 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)[C@@H](O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4093081 165466 0 None -15 3 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)[C@@H](O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
17759041 99636 8 None -18 3 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 199 4 4 3 -0.9 N[C@@H](CCP(O)(O)=S)C(=O)O 10.1021/jm070400y
CHEMBL243925 99636 8 None -18 3 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 199 4 4 3 -0.9 N[C@@H](CCP(O)(O)=S)C(=O)O 10.1021/jm070400y
44300605 20127 0 None -9 3 Rat 4.1 pEC50 = 4.1 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccc(O)cc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1192345 20127 0 None -9 3 Rat 4.1 pEC50 = 4.1 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccc(O)cc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL543568 20127 0 None -9 3 Rat 4.1 pEC50 = 4.1 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccc(O)cc2)C1 10.1016/s0960-894x(01)00329-8
137661528 166286 0 None 3 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)[C@H](O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4101970 166286 0 None 3 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay
ChEMBL 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)[C@H](O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
1310 9095 110 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
1369 9095 110 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
33032 9095 110 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
44272391 9095 110 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
88747398 9095 110 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
CHEMBL575060 9095 110 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
DB00142 9095 110 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
1310 9095 110 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
1369 9095 110 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
33032 9095 110 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
44272391 9095 110 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
88747398 9095 110 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
CHEMBL575060 9095 110 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
DB00142 9095 110 None -1148 17 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
3359 8720 6 None 1 2 Human 4.1 pEC50 = 4.1 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 10.1021/jm9602569
4236420 8720 6 None 1 2 Human 4.1 pEC50 = 4.1 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 10.1021/jm9602569
CHEMBL107768 8720 6 None 1 2 Human 4.1 pEC50 = 4.1 Functional
Agonistic activity at mGlu6 receptor expressed in CHO cellsAgonistic activity at mGlu6 receptor expressed in CHO cells
ChEMBL 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 10.1021/jm9602569
1310 9095 110 None -1148 17 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
1369 9095 110 None -1148 17 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
33032 9095 110 None -1148 17 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
44272391 9095 110 None -1148 17 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
88747398 9095 110 None -1148 17 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
CHEMBL575060 9095 110 None -1148 17 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
DB00142 9095 110 None -1148 17 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
46918013 165508 0 None -15 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)C(O)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4093492 165508 0 None -15 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
ChEMBL 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)C(O)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
10473248 20958 0 None -14 3 Rat 4.1 pEC50 = 4.1 Functional
Effective concentration required for partial agonistic activity at Metabotropic glutamate receptor 6; Partial agonistEffective concentration required for partial agonistic activity at Metabotropic glutamate receptor 6; Partial agonist
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2O)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1198741 20958 0 None -14 3 Rat 4.1 pEC50 = 4.1 Functional
Effective concentration required for partial agonistic activity at Metabotropic glutamate receptor 6; Partial agonistEffective concentration required for partial agonistic activity at Metabotropic glutamate receptor 6; Partial agonist
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2O)C1 10.1016/s0960-894x(01)00329-8
CHEMBL540015 20958 0 None -14 3 Rat 4.1 pEC50 = 4.1 Functional
Effective concentration required for partial agonistic activity at Metabotropic glutamate receptor 6; Partial agonistEffective concentration required for partial agonistic activity at Metabotropic glutamate receptor 6; Partial agonist
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2O)C1 10.1016/s0960-894x(01)00329-8
46197780 12354 0 None -4 4 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 273 7 4 4 -0.2 N[C@@H](CCP(=O)(O)CC(Cl)C(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1076865 12354 0 None -4 4 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader
ChEMBL 273 7 4 4 -0.2 N[C@@H](CCP(=O)(O)CC(Cl)C(=O)O)C(=O)O 10.1021/jm901523t
122197936 167555 0 None -17 3 Rat 5.1 pEC50 = 5.1 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 407 11 5 8 0.2 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(OC)c1OCC(=O)O nan
CHEMBL4114200 167555 0 None -17 3 Rat 5.1 pEC50 = 5.1 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 407 11 5 8 0.2 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(OC)c1OCC(=O)O nan
1608415 14591 8 None -5 3 Rat 4.0 pEC50 = 4 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 N[C@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
44660046 14591 8 None -5 3 Rat 4.0 pEC50 = 4 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 N[C@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1089514 14591 8 None -5 3 Rat 4.0 pEC50 = 4 Functional
Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 N[C@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
44817558 204972 1 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 280 3 0 3 4.6 CCOC(=O)c1c(Cl)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL575059 204972 1 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 280 3 0 3 4.6 CCOC(=O)c1c(Cl)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
44817627 203707 2 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 293 3 1 3 4.5 Cc1c(-c2ccccc2)sc(N)c1C(=O)c1ccccc1 10.1016/j.ejmech.2009.09.025
CHEMBL566318 203707 2 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 293 3 1 3 4.5 Cc1c(-c2ccccc2)sc(N)c1C(=O)c1ccccc1 10.1016/j.ejmech.2009.09.025
44817595 203564 1 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 279 3 1 4 3.6 CCOC(=O)c1c(N)sc(-c2ccc(F)cc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL565503 203564 1 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 279 3 1 4 3.6 CCOC(=O)c1c(N)sc(-c2ccc(F)cc2)c1C 10.1016/j.ejmech.2009.09.025
9794208 96825 4 None -12589 4 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assayAntagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assay
ChEMBL 199 2 3 4 -1.3 N[C@@]1(C(=O)O)CC(=O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
CHEMBL2381640 96825 4 None -12589 4 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assayAntagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assay
ChEMBL 199 2 3 4 -1.3 N[C@@]1(C(=O)O)CC(=O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
71681825 96830 0 None -154 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assayAntagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assay
ChEMBL 226 3 3 4 -0.2 [N-]=[N+]=N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL2381645 96830 0 None -154 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assayAntagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assay
ChEMBL 226 3 3 4 -0.2 [N-]=[N+]=N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
44817688 205671 1 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 299 4 0 6 4.5 CCOC(=O)c1c(N=NC#N)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL584345 205671 1 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 299 4 0 6 4.5 CCOC(=O)c1c(N=NC#N)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
5353536 214888 19 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 230 1 0 5 -1.2 N#Cc1cc2c(cc1[N+](=O)[O-])=NC(=O)C(=O)N=2 10.1016/j.ejmech.2009.09.025
CHEMBL9790 214888 19 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 230 1 0 5 -1.2 N#Cc1cc2c(cc1[N+](=O)[O-])=NC(=O)C(=O)N=2 10.1016/j.ejmech.2009.09.025
44817597 204048 1 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 275 4 1 4 3.9 CCCOC(=O)c1c(N)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL568515 204048 1 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 275 4 1 4 3.9 CCCOC(=O)c1c(N)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
70051926 96826 2 None -208 4 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assayAntagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assay
ChEMBL 197 2 3 3 -0.3 C=C1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL2381641 96826 2 None -208 4 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assayAntagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assay
ChEMBL 197 2 3 3 -0.3 C=C1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
11084869 96828 2 None -467 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assayAntagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assay
ChEMBL 201 2 4 4 -1.5 N[C@@]1(C(=O)O)C[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
CHEMBL2381643 96828 2 None -467 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assayAntagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assay
ChEMBL 201 2 4 4 -1.5 N[C@@]1(C(=O)O)C[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
57338826 156406 0 None -72 5 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human mGlu6 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as inhibition of L-AP4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu6 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as inhibition of L-AP4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 375 5 4 5 1.0 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
CHEMBL3947221 156406 0 None -72 5 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human mGlu6 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as inhibition of L-AP4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu6 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as inhibition of L-AP4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 375 5 4 5 1.0 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
44817555 205411 1 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 303 4 0 5 4.6 CCOC(=O)c1c(N=C=S)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL579009 205411 1 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 303 4 0 5 4.6 CCOC(=O)c1c(N=C=S)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
44817625 205198 3 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 289 2 1 4 4.3 Cc1c(-c2ccccc2)sc(N)c1C(=O)OC(C)(C)C 10.1016/j.ejmech.2009.09.025
CHEMBL577069 205198 3 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 289 2 1 4 4.3 Cc1c(-c2ccccc2)sc(N)c1C(=O)OC(C)(C)C 10.1016/j.ejmech.2009.09.025
45483692 203922 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 317 5 0 5 4.5 CCOC(=O)c1c(N=NN(C)C)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL567862 203922 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 317 5 0 5 4.5 CCOC(=O)c1c(N=NN(C)C)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
95883 106963 51 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 161 4 3 3 -0.5 C[C@H](C[C@H](N)C(=O)O)C(=O)O 10.1016/j.ejmech.2009.09.025
CHEMBL288166 106963 51 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 161 4 3 3 -0.5 C[C@H](C[C@H](N)C(=O)O)C(=O)O 10.1016/j.ejmech.2009.09.025
69669747 190432 11 None -1023 4 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant mGlu6 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assayAntagonist activity at human recombinant mGlu6 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4751065 190432 11 None -1023 4 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant mGlu6 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assayAntagonist activity at human recombinant mGlu6 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4802733 190432 11 None -1023 4 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant mGlu6 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assayAntagonist activity at human recombinant mGlu6 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
921213 204008 19 None 7 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 247 2 1 4 3.1 COC(=O)c1c(N)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL568300 204008 19 None 7 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 247 2 1 4 3.1 COC(=O)c1c(N)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
3997004 107402 24 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 323 4 1 4 4.8 CCOC(=O)c1c(N)sc(-c2ccccc2)c1-c1ccccc1 10.1016/j.ejmech.2009.09.025
CHEMBL291935 107402 24 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 323 4 1 4 4.8 CCOC(=O)c1c(N)sc(-c2ccccc2)c1-c1ccccc1 10.1016/j.ejmech.2009.09.025
45483698 203770 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 359 5 0 6 4.2 CCOC(=O)c1c(N=NN2CCOCC2)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL566754 203770 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 359 5 0 6 4.2 CCOC(=O)c1c(N=NN2CCOCC2)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
44817596 203744 16 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 295 3 1 4 4.1 CCOC(=O)c1c(N)sc(-c2ccccc2Cl)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL566530 203744 16 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 295 3 1 4 4.1 CCOC(=O)c1c(N)sc(-c2ccccc2Cl)c1C 10.1016/j.ejmech.2009.09.025
4189 213701 96 None -26 35 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 10.1016/j.ejmech.2009.09.025
CHEMBL1559 213701 96 None -26 35 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 10.1016/j.ejmech.2009.09.025
CHEMBL91 213701 96 None -26 35 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 10.1016/j.ejmech.2009.09.025
308248 203563 29 None - 1 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 214 1 1 3 3.2 Cc1c(-c2ccccc2)sc(N)c1C#N 10.1016/j.ejmech.2009.09.025
CHEMBL565502 203563 29 None - 1 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 214 1 1 3 3.2 Cc1c(-c2ccccc2)sc(N)c1C#N 10.1016/j.ejmech.2009.09.025
3272524 91457 60 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 336 2 3 8 0.8 NS(=O)(=O)c1cccc2c1c([N+](=O)[O-])cc1nc(O)c(O)nc12 10.1016/j.ejmech.2009.09.025
CHEMBL222519 91457 60 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 336 2 3 8 0.8 NS(=O)(=O)c1cccc2c1c([N+](=O)[O-])cc1nc(O)c(O)nc12 10.1016/j.ejmech.2009.09.025
674768 203670 62 None -190 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 261 3 1 4 3.5 CCOC(=O)c1c(N)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL566136 203670 62 None -190 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 261 3 1 4 3.5 CCOC(=O)c1c(N)sc(-c2ccccc2)c1C 10.1016/j.ejmech.2009.09.025
10684992 205216 45 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 291 4 1 5 3.5 CCOC(=O)c1c(N)sc(-c2ccc(OC)cc2)c1C 10.1016/j.ejmech.2009.09.025
CHEMBL577248 205216 45 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assayAntagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
ChEMBL 291 4 1 5 3.5 CCOC(=O)c1c(N)sc(-c2ccc(OC)cc2)c1C 10.1016/j.ejmech.2009.09.025
1436 6819 7 None - 1 Human 4.7 pKi = 4.7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O 10.1021/jm000007r
15508178 6819 7 None - 1 Human 4.7 pKi = 4.7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O 10.1021/jm000007r
CHEMBL60238 6819 7 None - 1 Human 4.7 pKi = 4.7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O 10.1021/jm000007r
10058694 213382 1 None - 0 Human 5.6 pKi = 5.6 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CSC2C1[C@H]2C(=O)O 10.1021/jm000007r
CHEMBL88999 213382 1 None - 0 Human 5.6 pKi = 5.6 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CSC2C1[C@H]2C(=O)O 10.1021/jm000007r
1393 8321 64 None -346 6 Human 5.5 pKi = 5.5 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000007r
1396 8321 64 None -346 6 Human 5.5 pKi = 5.5 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000007r
213056 8321 64 None -346 6 Human 5.5 pKi = 5.5 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000007r
CHEMBL8759 8321 64 None -346 6 Human 5.5 pKi = 5.5 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000007r
1310 9095 110 None -354 17 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
1369 9095 110 None -354 17 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
33032 9095 110 None -354 17 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
44272391 9095 110 None -354 17 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
88747398 9095 110 None -354 17 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
CHEMBL575060 9095 110 None -354 17 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
DB00142 9095 110 None -354 17 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
10197984 9199 44 None -147 5 Human 6.4 pKi = 6.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm000007r
1394 9199 44 None -147 5 Human 6.4 pKi = 6.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm000007r
CHEMBL275079 9199 44 None -147 5 Human 6.4 pKi = 6.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm000007r
1406 8854 38 None -25 7 Human 5.3 pKi = 5.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm000007r
4545574 8854 38 None -25 7 Human 5.3 pKi = 5.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm000007r
CHEMBL277475 8854 38 None -25 7 Human 5.3 pKi = 5.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm000007r
44322921 213616 1 None - 0 Human 5.3 pKi = 5.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)CC2CC1[C@H]2C(=O)O 10.1021/jm000007r
CHEMBL90501 213616 1 None - 0 Human 5.3 pKi = 5.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)CC2CC1[C@H]2C(=O)O 10.1021/jm000007r
1368 9070 37 None -1 11 Human 5.2 pKi = 5.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm000007r
5310956 9070 37 None -1 11 Human 5.2 pKi = 5.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm000007r
CHEMBL280563 9070 37 None -1 11 Human 5.2 pKi = 5.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm000007r
6604795 113775 1 None - 1 Human 4.2 pKi = 4.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 200 4 3 5 0.0 Cc1onc(O)c1CC[C@H](N)C(=O)O 10.1021/jm000007r
CHEMBL315268 113775 1 None - 1 Human 4.2 pKi = 4.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 200 4 3 5 0.0 Cc1onc(O)c1CC[C@H](N)C(=O)O 10.1021/jm000007r
104766 6822 42 None -11 14 Human 4.2 pKi = 4.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm000007r
1365 6822 42 None -11 14 Human 4.2 pKi = 4.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm000007r
CHEMBL34453 6822 42 None -11 14 Human 4.2 pKi = 4.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm000007r
1410 9054 48 None -2 8 Human 6.1 pKi = 6.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm000007r
1412 9054 48 None -2 8 Human 6.1 pKi = 6.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm000007r
179394 9054 48 None -2 8 Human 6.1 pKi = 6.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm000007r
57689795 9054 48 None -2 8 Human 6.1 pKi = 6.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm000007r
CHEMBL33567 9054 48 None -2 8 Human 6.1 pKi = 6.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm000007r
1310 9095 110 None -1148 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 9095 110 None -1148 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 9095 110 None -1148 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 9095 110 None -1148 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 9095 110 None -1148 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 9095 110 None -1148 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 9095 110 None -1148 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1310 9095 110 None -354 17 Human 8.3 pEC50 = 8.3 Functional
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 9095 110 None -354 17 Human 8.3 pEC50 = 8.3 Functional
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 9095 110 None -354 17 Human 8.3 pEC50 = 8.3 Functional
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 9095 110 None -354 17 Human 8.3 pEC50 = 8.3 Functional
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 9095 110 None -354 17 Human 8.3 pEC50 = 8.3 Functional
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 9095 110 None -354 17 Human 8.3 pEC50 = 8.3 Functional
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 9095 110 None -354 17 Human 8.3 pEC50 = 8.3 Functional
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1411 9140 66 None -3 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
4120 9140 66 None -3 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
57689797 9140 66 None -3 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
68841 9140 66 None -3 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
CHEMBL284377 9140 66 None -3 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
DB04522 9140 66 None -3 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
1411 9140 66 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
4120 9140 66 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
57689797 9140 66 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
68841 9140 66 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
CHEMBL284377 9140 66 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
DB04522 9140 66 None -1 6 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
3359 8720 6 None 1 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 8759641
4236420 8720 6 None 1 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 8759641
CHEMBL107768 8720 6 None 1 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 8759641
1436 6819 7 None - 1 Rat 4.7 pEC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O None
15508178 6819 7 None - 1 Rat 4.7 pEC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O None
CHEMBL60238 6819 7 None - 1 Rat 4.7 pEC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 264 4 3 4 0.1 OC(=O)[C@H]1C[C@](CN1Cc1ccccc1)(N)C(=O)O None
1310 9095 110 None -354 17 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
1369 9095 110 None -354 17 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
33032 9095 110 None -354 17 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
44272391 9095 110 None -354 17 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
88747398 9095 110 None -354 17 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
CHEMBL575060 9095 110 None -354 17 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
DB00142 9095 110 None -354 17 Human 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
1416 9867 41 None -6 4 Rat 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 294 2 2 4 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1 18593581
5866327 9867 41 None -6 4 Rat 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 294 2 2 4 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1 18593581
CHEMBL164770 9867 41 None -6 4 Rat 4.8 pEC50 = 4.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 294 2 2 4 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1 18593581
1368 9070 37 None -5 11 Rat 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 9833633
5310956 9070 37 None -5 11 Rat 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 9833633
CHEMBL280563 9070 37 None -5 11 Rat 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 9833633
6706 9146 8 None -38 8 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 22223752
71041983 9146 8 None -38 8 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 22223752
CHEMBL3114673 9146 8 None -38 8 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 22223752
1407 8860 42 None -114 7 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 11166323
16062593 8860 42 None -114 7 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 11166323
CHEMBL143210 8860 42 None -114 7 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 11166323
46898088 9145 6 None -8 8 Rat 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 19525404
6739 9145 6 None -8 8 Rat 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 19525404
CHEMBL3114672 9145 6 None -8 8 Rat 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 19525404
1368 9070 37 None -1 11 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 9144651
5310956 9070 37 None -1 11 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 9144651
CHEMBL280563 9070 37 None -1 11 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 9144651
1411 9140 66 None -1 6 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
4120 9140 66 None -1 6 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
57689797 9140 66 None -1 6 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
68841 9140 66 None -1 6 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
CHEMBL284377 9140 66 None -1 6 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
DB04522 9140 66 None -1 6 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144651
1398 7153 0 None -15 2 Rat 4.1 pEC50 None 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 199 4 4 4 -1.1 OC(=O)C(COP(=O)(O)O)(N)C 12769621
3964633 7153 0 None -15 2 Rat 4.1 pEC50 None 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 199 4 4 4 -1.1 OC(=O)C(COP(=O)(O)O)(N)C 12769621
CHEMBL1437137 7153 0 None -15 2 Rat 4.1 pEC50 None 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 199 4 4 4 -1.1 OC(=O)C(COP(=O)(O)O)(N)C 12769621
104766 6822 42 None -17 14 Rat 4.2 pEC50 None 4.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O None
1365 6822 42 None -17 14 Rat 4.2 pEC50 None 4.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O None
CHEMBL34453 6822 42 None -17 14 Rat 4.2 pEC50 None 4.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O None
1310 9095 110 None -1148 17 Rat 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
1369 9095 110 None -1148 17 Rat 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
33032 9095 110 None -1148 17 Rat 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
44272391 9095 110 None -1148 17 Rat 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
88747398 9095 110 None -1148 17 Rat 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
CHEMBL575060 9095 110 None -1148 17 Rat 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
DB00142 9095 110 None -1148 17 Rat 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9833633
1378 9195 54 None -4265 14 Human 4.5 pEC50 None 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 11138847
1399 9195 54 None -4265 14 Human 4.5 pEC50 None 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 11138847
9819927 9195 54 None -4265 14 Human 4.5 pEC50 None 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 11138847
CHEMBL432038 9195 54 None -4265 14 Human 4.5 pEC50 None 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 11138847
104766 6822 42 None -11 14 Human 4.7 pEC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 9144651
1365 6822 42 None -11 14 Human 4.7 pEC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 9144651
CHEMBL34453 6822 42 None -11 14 Human 4.7 pEC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 9144651
1310 9095 110 None -354 17 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
1369 9095 110 None -354 17 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
33032 9095 110 None -354 17 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
44272391 9095 110 None -354 17 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
88747398 9095 110 None -354 17 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
CHEMBL575060 9095 110 None -354 17 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
DB00142 9095 110 None -354 17 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144651
1406 8854 38 None -25 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10336568
1406 8854 38 None -25 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 11166323
4545574 8854 38 None -25 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10336568
4545574 8854 38 None -25 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 11166323
CHEMBL277475 8854 38 None -25 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10336568
CHEMBL277475 8854 38 None -25 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 11166323
1377 8122 26 None -60 8 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 9833633
5310979 8122 26 None -60 8 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 9833633
CHEMBL284193 8122 26 None -60 8 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 9833633
1410 9054 48 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11166323
1410 9054 48 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144651
1412 9054 48 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11166323
1412 9054 48 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144651
179394 9054 48 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11166323
179394 9054 48 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144651
57689795 9054 48 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11166323
57689795 9054 48 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144651
CHEMBL33567 9054 48 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11166323
CHEMBL33567 9054 48 None -2 8 Human 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144651
1414 9237 0 None -707 2 Rat 3.5 pIC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 12769621
1795545 9237 0 None -707 2 Rat 3.5 pIC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 12769621
CHEMBL1488784 9237 0 None -707 2 Rat 3.5 pIC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 12769621
1415 9392 41 None -10 2 Human 3.3 pIC50 None 3.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C None
3972752 9392 41 None -10 2 Human 3.3 pIC50 None 3.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C None
CHEMBL86508 9392 41 None -10 2 Human 3.3 pIC50 None 3.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C None
1408 7053 31 None -3 7 Rat 4.7 pIC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O None
6604820 7053 31 None -3 7 Rat 4.7 pIC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O None
CHEMBL285043 7053 31 None -3 7 Rat 4.7 pIC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O None
CHEMBL288635 7053 31 None -3 7 Rat 4.7 pIC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O None
1393 8321 64 None -346 6 Human 5.5 pIC50 None 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10090786
1396 8321 64 None -346 6 Human 5.5 pIC50 None 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10090786
213056 8321 64 None -346 6 Human 5.5 pIC50 None 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10090786
CHEMBL8759 8321 64 None -346 6 Human 5.5 pIC50 None 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10090786
10197984 9199 44 None -147 5 Human 6.4 pIC50 None 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10090786
1394 9199 44 None -147 5 Human 6.4 pIC50 None 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10090786
CHEMBL275079 9199 44 None -147 5 Human 6.4 pIC50 None 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10090786




Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
ity
Common
name
GPCRdb
ID
#Vendors

Reference
ligand
Fold
selectivity
# Tested
GPCRs
Species

p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Assay
Type
Assay
Description
Source

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

71681824 96831 0 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 200 2 4 4 -1.6 N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
CHEMBL2381646 96831 0 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 200 2 4 4 -1.6 N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
10979251 96835 0 None - 2 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
CHEMBL2381650 96835 0 None - 2 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
139119037 96837 2 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
15479143 96837 2 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
CHEMBL2381652 96837 2 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
1310 9095 110 None -43 18 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
1369 9095 110 None -43 18 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
33032 9095 110 None -43 18 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
44272391 9095 110 None -43 18 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
88747398 9095 110 None -43 18 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
CHEMBL575060 9095 110 None -43 18 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
DB00142 9095 110 None -43 18 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
139054390 211702 106 None -1 5 Rat 4.7 pEC50 = 4.7 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O 10.1021/jm9703597
23327 211702 106 None -1 5 Rat 4.7 pEC50 = 4.7 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O 10.1021/jm9703597
CHEMBL76232 211702 106 None -1 5 Rat 4.7 pEC50 = 4.7 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O 10.1021/jm9703597
1411 9140 66 None - 1 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
4120 9140 66 None - 1 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
57689797 9140 66 None - 1 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
68841 9140 66 None - 1 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
CHEMBL284377 9140 66 None - 1 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
DB04522 9140 66 None - 1 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
2207 106641 63 None -2 7 Human 6.6 pEC50 = 6.6 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O 10.1021/jm970719q
CHEMBL285843 106641 63 None -2 7 Human 6.6 pEC50 = 6.6 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O 10.1021/jm970719q
71681826 96836 0 None - 2 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
CHEMBL2381651 96836 0 None - 2 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
1393 8321 64 None -162 6 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm4000165
1396 8321 64 None -162 6 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm4000165
213056 8321 64 None -162 6 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm4000165
CHEMBL8759 8321 64 None -162 6 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm4000165
70052526 96827 2 None - 1 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 201 2 4 4 -1.5 N[C@@]1(C(=O)O)C[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
CHEMBL2381642 96827 2 None - 1 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 201 2 4 4 -1.5 N[C@@]1(C(=O)O)C[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
1310 9095 110 None -85 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
1369 9095 110 None -85 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
33032 9095 110 None -85 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
44272391 9095 110 None -85 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
88747398 9095 110 None -85 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
CHEMBL575060 9095 110 None -85 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
DB00142 9095 110 None -85 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
10846649 108008 4 None - 0 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H]2C[C@H]1[C@H]2C(=O)O 10.1021/jm970719q
CHEMBL296054 108008 4 None - 0 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H]2C[C@H]1[C@H]2C(=O)O 10.1021/jm970719q
1410 9054 48 None -7 6 Human 7.3 pEC50 = 7.3 Binding
Activation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.8b01120
1412 9054 48 None -7 6 Human 7.3 pEC50 = 7.3 Binding
Activation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.8b01120
179394 9054 48 None -7 6 Human 7.3 pEC50 = 7.3 Binding
Activation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.8b01120
57689795 9054 48 None -7 6 Human 7.3 pEC50 = 7.3 Binding
Activation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.8b01120
CHEMBL33567 9054 48 None -7 6 Human 7.3 pEC50 = 7.3 Binding
Activation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.8b01120
1410 9054 48 None - 6 Rat 6.2 pEC50 = 6.2 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm9703597
1412 9054 48 None - 6 Rat 6.2 pEC50 = 6.2 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm9703597
179394 9054 48 None - 6 Rat 6.2 pEC50 = 6.2 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm9703597
57689795 9054 48 None - 6 Rat 6.2 pEC50 = 6.2 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm9703597
CHEMBL33567 9054 48 None - 6 Rat 6.2 pEC50 = 6.2 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm9703597
6604795 113775 1 None - 1 Rat 4.2 pEC50 = 4.2 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 200 4 3 5 0.0 Cc1onc(O)c1CC[C@H](N)C(=O)O 10.1021/jm9703597
CHEMBL315268 113775 1 None - 1 Rat 4.2 pEC50 = 4.2 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 200 4 3 5 0.0 Cc1onc(O)c1CC[C@H](N)C(=O)O 10.1021/jm9703597
70051296 96833 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
CHEMBL2381648 96833 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
60096211 96834 0 None - 2 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL2381649 96834 0 None - 2 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
11310142 9200 19 None - 2 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm4000165
11614 9200 19 None - 2 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm4000165
CHEMBL192051 9200 19 None - 2 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm4000165
71681823 96829 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 226 3 3 4 -0.2 [N-]=[N+]=N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
CHEMBL2381644 96829 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 226 3 3 4 -0.2 [N-]=[N+]=N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
104766 6822 42 None -38 11 Human 4.1 pEC50 = 4.1 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm970719q
1365 6822 42 None -38 11 Human 4.1 pEC50 = 4.1 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm970719q
CHEMBL34453 6822 42 None -38 11 Human 4.1 pEC50 = 4.1 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm970719q
3359 8720 6 None - 0 Rat 4.1 pEC50 = 4.1 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 10.1021/jm9703597
4236420 8720 6 None - 0 Rat 4.1 pEC50 = 4.1 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 10.1021/jm9703597
CHEMBL107768 8720 6 None - 0 Rat 4.1 pEC50 = 4.1 Binding
Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6
ChEMBL 200 4 3 4 -0.4 OC(=O)C(CCc1c(C)o[nH]c1=O)N 10.1021/jm9703597
1410 9054 48 None - 6 Rat 6.1 pEC50 = 6.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
1412 9054 48 None - 6 Rat 6.1 pEC50 = 6.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
179394 9054 48 None - 6 Rat 6.1 pEC50 = 6.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
57689795 9054 48 None - 6 Rat 6.1 pEC50 = 6.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
CHEMBL33567 9054 48 None - 6 Rat 6.1 pEC50 = 6.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
11344646 133554 1 None - 2 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 199 2 3 3 -0.2 C[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL365368 133554 1 None - 2 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 199 2 3 3 -0.2 C[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
11275666 96832 1 None - 2 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 200 2 4 4 -1.6 N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL2381647 96832 1 None - 2 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 200 2 4 4 -1.6 N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
1378 9195 54 None - 10 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
1399 9195 54 None - 10 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
9819927 9195 54 None - 10 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
CHEMBL432038 9195 54 None - 10 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
1397 9307 15 None - 5 Rat 5.7 pIC50 = 5.7 Binding
Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
9886034 9307 15 None - 5 Rat 5.7 pIC50 = 5.7 Binding
Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
CHEMBL186453 9307 15 None - 5 Rat 5.7 pIC50 = 5.7 Binding
Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
71566598 149468 15 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at mGluR6 (unknown origin) by FLIPR assayAntagonist activity at mGluR6 (unknown origin) by FLIPR assay
ChEMBL 377 4 1 4 2.8 NC(=O)c1cc(-c2ccc(F)cc2)c2ccc(CN3C(=O)CCC3=O)cc2n1 10.1016/j.bmcl.2020.127066
CHEMBL3892073 149468 15 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at mGluR6 (unknown origin) by FLIPR assayAntagonist activity at mGluR6 (unknown origin) by FLIPR assay
ChEMBL 377 4 1 4 2.8 NC(=O)c1cc(-c2ccc(F)cc2)c2ccc(CN3C(=O)CCC3=O)cc2n1 10.1016/j.bmcl.2020.127066
12310764 8751 64 Functional -14 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
1233 8751 64 Functional -14 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
1371 8751 64 Functional -14 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
CHEMBL284895 8751 64 Functional -14 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
1310 9095 110 Functional -85 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1310 9095 110 Functional -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 9095 110 Functional -85 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 9095 110 Functional -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 9095 110 Functional -85 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 9095 110 Functional -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 9095 110 Functional -85 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 9095 110 Functional -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 9095 110 Functional -85 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 9095 110 Functional -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 9095 110 Functional -85 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 9095 110 Functional -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 9095 110 Functional -85 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 9095 110 Functional -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1370 10037 67 Functional -602 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
1372 10037 67 Functional -602 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
40539 10037 67 Functional -602 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
6971145 10037 67 Functional -602 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
CHEMBL279956 10037 67 Functional -602 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
DB02999 10037 67 Functional -602 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
128563 10237 33 Functional -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 10237 33 Functional -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 10237 33 Functional -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 10237 33 Functional -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
10297 33885 30 Functional -38 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 33885 30 Functional -38 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
446220 140299 14 Functional -1778 45 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 140299 14 Functional -1778 45 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
162265 209053 22 Functional -239 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 209053 22 Functional -239 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 209053 22 Functional -239 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
139054390 211702 106 Functional -1 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O None
23327 211702 106 Functional -1 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O None
CHEMBL76232 211702 106 Functional -1 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O None
None 222951 0 Functional -2 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 173 2 3 3 -0.3 C1CC(CC1C(=O)O)(C(=O)O)N None
25137849 222958 0 Functional -4 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 222958 0 Functional -4 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 223095 0 Functional -1 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 223096 0 Functional -1 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 223104 0 Functional -13 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 223105 0 Functional -16 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 223269 0 Functional -1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 144 2 2 2 -0.7 CC(C(=O)NC)NC(=O)C None
None 223270 0 Functional -1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 161 5 3 3 -0.3 C(CC(C(=O)O)N)CC(=O)O None
None 223117 0 Functional -2 4 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 185 4 4 4 -1.5 C(C(C(=O)O)N)OP(=O)(O)O None
2207 106641 63 Functional -1 7 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
CHEMBL285843 106641 63 Functional -1 7 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
2207 106641 63 Functional -2 7 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
CHEMBL285843 106641 63 Functional -2 7 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None