Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 1410 | 2274 | None | 38 | Human | Functional | pEC50 | = | 6 | 6.0 | -2 | 8 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/acs.jmedchem.7b01438 | ||
| 1412 | 2274 | None | 38 | Human | Functional | pEC50 | = | 6 | 6.0 | -2 | 8 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/acs.jmedchem.7b01438 | ||
| 179394 | 2274 | None | 38 | Human | Functional | pEC50 | = | 6 | 6.0 | -2 | 8 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/acs.jmedchem.7b01438 | ||
| 57689795 | 2274 | None | 38 | Human | Functional | pEC50 | = | 6 | 6.0 | -2 | 8 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/acs.jmedchem.7b01438 | ||
| CHEMBL33567 | 2274 | None | 38 | Human | Functional | pEC50 | = | 6 | 6.0 | -2 | 8 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/acs.jmedchem.7b01438 | ||
| 1410 | 2274 | None | 38 | Rat | Functional | pEC50 | = | 6 | 6.0 | -5 | 8 | Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/jm901523t | ||
| 1412 | 2274 | None | 38 | Rat | Functional | pEC50 | = | 6 | 6.0 | -5 | 8 | Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/jm901523t | ||
| 179394 | 2274 | None | 38 | Rat | Functional | pEC50 | = | 6 | 6.0 | -5 | 8 | Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/jm901523t | ||
| 57689795 | 2274 | None | 38 | Rat | Functional | pEC50 | = | 6 | 6.0 | -5 | 8 | Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/jm901523t | ||
| CHEMBL33567 | 2274 | None | 38 | Rat | Functional | pEC50 | = | 6 | 6.0 | -5 | 8 | Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/jm901523t | ||
| 2207 | 99919 | None | 47 | Rat | Functional | pEC50 | = | 6 | 6.0 | -194 | 4 | Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6 |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | NC(CCP(=O)(O)O)C(=O)O | 10.1016/S0960-894X(97)00068-1 | ||
| CHEMBL285843 | 99919 | None | 47 | Rat | Functional | pEC50 | = | 6 | 6.0 | -194 | 4 | Tested for the agonistic activity against Metabotropic glutamate receptor 6Tested for the agonistic activity against Metabotropic glutamate receptor 6 |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | NC(CCP(=O)(O)O)C(=O)O | 10.1016/S0960-894X(97)00068-1 | ||
| 10385210 | 13037 | None | 0 | Rat | Functional | pEC50 | = | 4 | 4.0 | -2 | 3 | Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6 |
ChEMBL | 309 | 5 | 3 | 6 | 0.0 | N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc([N+](=O)[O-])c2)C1 | 10.1016/s0960-894x(01)00329-8 | ||
| CHEMBL1189910 | 13037 | None | 0 | Rat | Functional | pEC50 | = | 4 | 4.0 | -2 | 3 | Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6 |
ChEMBL | 309 | 5 | 3 | 6 | 0.0 | N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc([N+](=O)[O-])c2)C1 | 10.1016/s0960-894x(01)00329-8 | ||
| CHEMBL539760 | 13037 | None | 0 | Rat | Functional | pEC50 | = | 4 | 4.0 | -2 | 3 | Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6 |
ChEMBL | 309 | 5 | 3 | 6 | 0.0 | N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc([N+](=O)[O-])c2)C1 | 10.1016/s0960-894x(01)00329-8 | ||
| 137655963 | 159115 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -1 | 4 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay |
ChEMBL | 352 | 7 | 5 | 7 | 0.5 | N[C@@H](CCP(=O)(O)[C@@H](O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O | 10.1021/acs.jmedchem.7b01438 | ||
| CHEMBL4096644 | 159115 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -1 | 4 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay |
ChEMBL | 352 | 7 | 5 | 7 | 0.5 | N[C@@H](CCP(=O)(O)[C@@H](O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O | 10.1021/acs.jmedchem.7b01438 | ||
| 1443 | 1318 | None | 30 | Rat | Functional | pEC50 | = | 6.0 | 6.0 | -7 | 5 | Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution. |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@@H](CCP(=O)(O)O)N | nan | ||
| 1550579 | 1318 | None | 30 | Rat | Functional | pEC50 | = | 6.0 | 6.0 | -7 | 5 | Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution. |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@@H](CCP(=O)(O)O)N | nan | ||
| CHEMBL1319383 | 1318 | None | 30 | Rat | Functional | pEC50 | = | 6.0 | 6.0 | -7 | 5 | Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution. |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@@H](CCP(=O)(O)O)N | nan | ||
| 1408 | 265 | None | 24 | Rat | Functional | pEC50 | = | 5.0 | 5.0 | -3 | 7 | Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting |
ChEMBL | 217 | 3 | 4 | 4 | -1.0 | OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O | 10.1021/jm901523t | ||
| 6604820 | 265 | None | 24 | Rat | Functional | pEC50 | = | 5.0 | 5.0 | -3 | 7 | Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting |
ChEMBL | 217 | 3 | 4 | 4 | -1.0 | OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O | 10.1021/jm901523t | ||
| CHEMBL285043 | 265 | None | 24 | Rat | Functional | pEC50 | = | 5.0 | 5.0 | -3 | 7 | Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting |
ChEMBL | 217 | 3 | 4 | 4 | -1.0 | OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O | 10.1021/jm901523t | ||
| CHEMBL288635 | 265 | None | 24 | Rat | Functional | pEC50 | = | 5.0 | 5.0 | -3 | 7 | Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting |
ChEMBL | 217 | 3 | 4 | 4 | -1.0 | OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O | 10.1021/jm901523t | ||
| 137650519 | 157437 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | 1 | 4 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay |
ChEMBL | 352 | 7 | 5 | 7 | 0.5 | N[C@@H](CCP(=O)(O)C(O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O | 10.1021/acs.jmedchem.7b01438 | ||
| CHEMBL4077705 | 157437 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | 1 | 4 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay |
ChEMBL | 352 | 7 | 5 | 7 | 0.5 | N[C@@H](CCP(=O)(O)C(O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O | 10.1021/acs.jmedchem.7b01438 | ||
| 137645989 | 157786 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -1 | 4 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay |
ChEMBL | 364 | 8 | 5 | 8 | 0.4 | COc1cc([C@@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O | 10.1021/acs.jmedchem.7b01438 | ||
| CHEMBL4081842 | 157786 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -1 | 4 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay |
ChEMBL | 364 | 8 | 5 | 8 | 0.4 | COc1cc([C@@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O | 10.1021/acs.jmedchem.7b01438 | ||
| 46197778 | 8220 | None | 0 | Rat | Functional | pEC50 | = | 6.0 | 6.0 | 1 | 5 | Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader |
ChEMBL | 237 | 6 | 4 | 4 | -0.3 | N[C@@H](CCP(=O)(O)/C=C/C(=O)O)C(=O)O | 10.1021/jm901523t | ||
| CHEMBL1092243 | 8220 | None | 0 | Rat | Functional | pEC50 | = | 6.0 | 6.0 | 1 | 5 | Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader |
ChEMBL | 237 | 6 | 4 | 4 | -0.3 | N[C@@H](CCP(=O)(O)/C=C/C(=O)O)C(=O)O | 10.1021/jm901523t | ||
| 1408 | 265 | None | 24 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -2 | 7 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method |
ChEMBL | 217 | 3 | 4 | 4 | -1.0 | OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O | 10.1021/acs.jmedchem.7b01438 | ||
| 6604820 | 265 | None | 24 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -2 | 7 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method |
ChEMBL | 217 | 3 | 4 | 4 | -1.0 | OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O | 10.1021/acs.jmedchem.7b01438 | ||
| CHEMBL285043 | 265 | None | 24 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -2 | 7 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method |
ChEMBL | 217 | 3 | 4 | 4 | -1.0 | OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O | 10.1021/acs.jmedchem.7b01438 | ||
| CHEMBL288635 | 265 | None | 24 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -2 | 7 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method |
ChEMBL | 217 | 3 | 4 | 4 | -1.0 | OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O | 10.1021/acs.jmedchem.7b01438 | ||
| 57765622 | 156195 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | -20 | 3 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay |
ChEMBL | 386 | 7 | 4 | 6 | 1.7 | N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)c([N+](=O)[O-])c1)C(=O)O | 10.1021/acs.jmedchem.7b01438 | ||
| CHEMBL4063142 | 156195 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | -20 | 3 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay |
ChEMBL | 386 | 7 | 4 | 6 | 1.7 | N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)c([N+](=O)[O-])c1)C(=O)O | 10.1021/acs.jmedchem.7b01438 | ||
| 10176324 | 114891 | None | 1 | Rat | Functional | pEC50 | = | 5.9 | 5.9 | -151 | 4 | Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells |
ChEMBL | 173 | 3 | 3 | 3 | -0.6 | C[C@H]1[C@H](C(=O)O)[C@H]1[C@H](N)C(=O)O | 10.1021/jm030967o | ||
| CHEMBL334160 | 114891 | None | 1 | Rat | Functional | pEC50 | = | 5.9 | 5.9 | -151 | 4 | Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells |
ChEMBL | 173 | 3 | 3 | 3 | -0.6 | C[C@H]1[C@H](C(=O)O)[C@H]1[C@H](N)C(=O)O | 10.1021/jm030967o | ||
| 44406220 | 72197 | None | 1 | Rat | Functional | pEC50 | = | 4.9 | 4.9 | -1 | 2 | Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells |
ChEMBL | 195 | 3 | 4 | 3 | -1.0 | N[C@H](C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O | 10.1016/j.bmcl.2005.09.014 | ||
| CHEMBL197976 | 72197 | None | 1 | Rat | Functional | pEC50 | = | 4.9 | 4.9 | -1 | 2 | Activity at rat mGluR6 by measuring cAMP formation in CHO cellsActivity at rat mGluR6 by measuring cAMP formation in CHO cells |
ChEMBL | 195 | 3 | 4 | 3 | -1.0 | N[C@H](C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O | 10.1016/j.bmcl.2005.09.014 | ||
| 11708219 | 169475 | None | 0 | Rat | Functional | pEC50 | = | 4.9 | 4.9 | -1 | 2 | Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production |
ChEMBL | 195 | 3 | 4 | 3 | -1.0 | NC(C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O | 10.1016/j.bmc.2007.02.040 | ||
| CHEMBL442076 | 169475 | None | 0 | Rat | Functional | pEC50 | = | 4.9 | 4.9 | -1 | 2 | Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP productionActivity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production |
ChEMBL | 195 | 3 | 4 | 3 | -1.0 | NC(C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O | 10.1016/j.bmc.2007.02.040 | ||
| 122197960 | 161005 | None | 0 | Rat | Functional | pEC50 | = | 4.9 | 4.9 | -12 | 2 | Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution. |
ChEMBL | 331 | 9 | 4 | 5 | 0.7 | N[C@H](CCP(=O)(O)Cc1ccc(OCC(=O)O)cc1)C(=O)O | nan | ||
| CHEMBL4115286 | 161005 | None | 0 | Rat | Functional | pEC50 | = | 4.9 | 4.9 | -12 | 2 | Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution. |
ChEMBL | 331 | 9 | 4 | 5 | 0.7 | N[C@H](CCP(=O)(O)Cc1ccc(OCC(=O)O)cc1)C(=O)O | nan | ||
| 44361401 | 31349 | None | 0 | Rat | Functional | pEC50 | = | 6.8 | 6.8 | -33 | 5 | Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells |
ChEMBL | 175 | 3 | 4 | 4 | -1.9 | N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O | 10.1021/jm030967o | ||
| CHEMBL140197 | 31349 | None | 0 | Rat | Functional | pEC50 | = | 6.8 | 6.8 | -33 | 5 | Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells |
ChEMBL | 175 | 3 | 4 | 4 | -1.9 | N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O | 10.1021/jm030967o | ||
| 46898088 | 2366 | None | 7 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -11 | 8 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method |
ChEMBL | 364 | 8 | 5 | 8 | 0.4 | COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O | 10.1021/acs.jmedchem.7b01438 | ||
| 6739 | 2366 | None | 7 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -11 | 8 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method |
ChEMBL | 364 | 8 | 5 | 8 | 0.4 | COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O | 10.1021/acs.jmedchem.7b01438 | ||
| CHEMBL3114672 | 2366 | None | 7 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -11 | 8 | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method |
ChEMBL | 364 | 8 | 5 | 8 | 0.4 | COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O | 10.1021/acs.jmedchem.7b01438 | ||
| 127030386 | 139128 | None | 0 | Rat | Functional | pEC50 | = | 4.8 | 4.8 | -7 | 3 | Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay |
ChEMBL | 217 | 5 | 4 | 4 | -1.0 | N[C@@H](C[C@@]1(C(=O)O)C[C@@H]1C(=O)O)C(=O)O | 10.1021/acs.jmedchem.5b01333 | ||
Showing 1 to 50 of 508 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 71681824 | 90090 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay |
ChEMBL | 200 | 2 | 4 | 4 | -1.6 | N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 | 10.1021/jm4000165 | ||
| CHEMBL2381646 | 90090 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay |
ChEMBL | 200 | 2 | 4 | 4 | -1.6 | N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 | 10.1021/jm4000165 | ||
| 10979251 | 90094 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 2 | Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay |
ChEMBL | 293 | 4 | 3 | 4 | 1.3 | N[C@@]1(C(=O)O)C[C@@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 | 10.1021/jm4000165 | ||
| CHEMBL2381650 | 90094 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 2 | Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay |
ChEMBL | 293 | 4 | 3 | 4 | 1.3 | N[C@@]1(C(=O)O)C[C@@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 | 10.1021/jm4000165 | ||
| 139119037 | 90096 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay |
ChEMBL | 203 | 2 | 3 | 3 | -0.5 | N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 | 10.1021/jm4000165 | ||
| 15479143 | 90096 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay |
ChEMBL | 203 | 2 | 3 | 3 | -0.5 | N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 | 10.1021/jm4000165 | ||
| CHEMBL2381652 | 90096 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay |
ChEMBL | 203 | 2 | 3 | 3 | -0.5 | N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 | 10.1021/jm4000165 | ||
| 1310 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.8 | 4.8 | -43 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| 1369 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.8 | 4.8 | -43 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| 33032 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.8 | 4.8 | -43 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| 44272391 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.8 | 4.8 | -43 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| 88747398 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.8 | 4.8 | -43 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| CHEMBL575060 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.8 | 4.8 | -43 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| DB00142 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.8 | 4.8 | -43 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| 139054390 | 207381 | None | 56 | Rat | Binding | pEC50 | = | 4.7 | 4.7 | -1 | 5 | Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | N[C@H](CCC(=O)O)C(=O)O | 10.1021/jm9703597 | ||
| 23327 | 207381 | None | 56 | Rat | Binding | pEC50 | = | 4.7 | 4.7 | -1 | 5 | Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | N[C@H](CCC(=O)O)C(=O)O | 10.1021/jm9703597 | ||
| CHEMBL76232 | 207381 | None | 56 | Rat | Binding | pEC50 | = | 4.7 | 4.7 | -1 | 5 | Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | N[C@H](CCC(=O)O)C(=O)O | 10.1021/jm9703597 | ||
| 1411 | 2361 | None | 44 | Rat | Binding | pEC50 | = | 5.6 | 5.6 | - | 1 | Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat |
ChEMBL | 185 | 4 | 4 | 4 | -1.5 | OC(=O)[C@H](COP(=O)(O)O)N | 10.1021/jm00009a001 | ||
| 4120 | 2361 | None | 44 | Rat | Binding | pEC50 | = | 5.6 | 5.6 | - | 1 | Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat |
ChEMBL | 185 | 4 | 4 | 4 | -1.5 | OC(=O)[C@H](COP(=O)(O)O)N | 10.1021/jm00009a001 | ||
| 57689797 | 2361 | None | 44 | Rat | Binding | pEC50 | = | 5.6 | 5.6 | - | 1 | Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat |
ChEMBL | 185 | 4 | 4 | 4 | -1.5 | OC(=O)[C@H](COP(=O)(O)O)N | 10.1021/jm00009a001 | ||
| 68841 | 2361 | None | 44 | Rat | Binding | pEC50 | = | 5.6 | 5.6 | - | 1 | Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat |
ChEMBL | 185 | 4 | 4 | 4 | -1.5 | OC(=O)[C@H](COP(=O)(O)O)N | 10.1021/jm00009a001 | ||
| CHEMBL284377 | 2361 | None | 44 | Rat | Binding | pEC50 | = | 5.6 | 5.6 | - | 1 | Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat |
ChEMBL | 185 | 4 | 4 | 4 | -1.5 | OC(=O)[C@H](COP(=O)(O)O)N | 10.1021/jm00009a001 | ||
| DB04522 | 2361 | None | 44 | Rat | Binding | pEC50 | = | 5.6 | 5.6 | - | 1 | Concentration for half maximal activation of metabotropic glutamate mGluR6 in ratConcentration for half maximal activation of metabotropic glutamate mGluR6 in rat |
ChEMBL | 185 | 4 | 4 | 4 | -1.5 | OC(=O)[C@H](COP(=O)(O)O)N | 10.1021/jm00009a001 | ||
| 2207 | 99919 | None | 47 | Human | Binding | pEC50 | = | 6.6 | 6.6 | -2 | 7 | Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6 |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | NC(CCP(=O)(O)O)C(=O)O | 10.1021/jm970719q | ||
| CHEMBL285843 | 99919 | None | 47 | Human | Binding | pEC50 | = | 6.6 | 6.6 | -2 | 7 | Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6 |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | NC(CCP(=O)(O)O)C(=O)O | 10.1021/jm970719q | ||
| 71681826 | 90095 | None | 0 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 2 | Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay |
ChEMBL | 293 | 4 | 3 | 4 | 1.3 | N[C@@]1(C(=O)O)C[C@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 | 10.1021/jm4000165 | ||
| CHEMBL2381651 | 90095 | None | 0 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 2 | Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay |
ChEMBL | 293 | 4 | 3 | 4 | 1.3 | N[C@@]1(C(=O)O)C[C@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 | 10.1021/jm4000165 | ||
| 1393 | 1539 | None | 42 | Human | Binding | pEC50 | = | 5.5 | 5.5 | -162 | 6 | Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay |
ChEMBL | 185 | 2 | 3 | 3 | -0.5 | OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O | 10.1021/jm4000165 | ||
| 1396 | 1539 | None | 42 | Human | Binding | pEC50 | = | 5.5 | 5.5 | -162 | 6 | Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay |
ChEMBL | 185 | 2 | 3 | 3 | -0.5 | OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O | 10.1021/jm4000165 | ||
| 213056 | 1539 | None | 42 | Human | Binding | pEC50 | = | 5.5 | 5.5 | -162 | 6 | Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay |
ChEMBL | 185 | 2 | 3 | 3 | -0.5 | OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O | 10.1021/jm4000165 | ||
| CHEMBL8759 | 1539 | None | 42 | Human | Binding | pEC50 | = | 5.5 | 5.5 | -162 | 6 | Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay |
ChEMBL | 185 | 2 | 3 | 3 | -0.5 | OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O | 10.1021/jm4000165 | ||
| 70052526 | 90086 | None | 1 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 1 | Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay |
ChEMBL | 201 | 2 | 4 | 4 | -1.5 | N[C@@]1(C(=O)O)C[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O | 10.1021/jm4000165 | ||
| CHEMBL2381642 | 90086 | None | 1 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 1 | Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay |
ChEMBL | 201 | 2 | 4 | 4 | -1.5 | N[C@@]1(C(=O)O)C[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O | 10.1021/jm4000165 | ||
| 1310 | 2315 | None | 61 | Human | Binding | pEC50 | = | 5.3 | 5.3 | -85 | 18 | Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm970719q | ||
| 1369 | 2315 | None | 61 | Human | Binding | pEC50 | = | 5.3 | 5.3 | -85 | 18 | Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm970719q | ||
| 33032 | 2315 | None | 61 | Human | Binding | pEC50 | = | 5.3 | 5.3 | -85 | 18 | Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm970719q | ||
| 44272391 | 2315 | None | 61 | Human | Binding | pEC50 | = | 5.3 | 5.3 | -85 | 18 | Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm970719q | ||
| 88747398 | 2315 | None | 61 | Human | Binding | pEC50 | = | 5.3 | 5.3 | -85 | 18 | Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm970719q | ||
| CHEMBL575060 | 2315 | None | 61 | Human | Binding | pEC50 | = | 5.3 | 5.3 | -85 | 18 | Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm970719q | ||
| DB00142 | 2315 | None | 61 | Human | Binding | pEC50 | = | 5.3 | 5.3 | -85 | 18 | Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm970719q | ||
| 10846649 | 101285 | None | 2 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6 |
ChEMBL | 185 | 2 | 3 | 3 | -0.5 | N[C@@]1(C(=O)O)C[C@@H]2C[C@H]1[C@H]2C(=O)O | 10.1021/jm970719q | ||
| CHEMBL296054 | 101285 | None | 2 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | Compound was tested for the inhibition of Metabotropic glutamate receptor 6Compound was tested for the inhibition of Metabotropic glutamate receptor 6 |
ChEMBL | 185 | 2 | 3 | 3 | -0.5 | N[C@@]1(C(=O)O)C[C@@H]2C[C@H]1[C@H]2C(=O)O | 10.1021/jm970719q | ||
| 1410 | 2274 | None | 38 | Human | Binding | pEC50 | = | 7.3 | 7.3 | -7 | 6 | Activation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cells |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/acs.jmedchem.8b01120 | ||
| 1412 | 2274 | None | 38 | Human | Binding | pEC50 | = | 7.3 | 7.3 | -7 | 6 | Activation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cells |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/acs.jmedchem.8b01120 | ||
| 179394 | 2274 | None | 38 | Human | Binding | pEC50 | = | 7.3 | 7.3 | -7 | 6 | Activation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cells |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/acs.jmedchem.8b01120 | ||
| 57689795 | 2274 | None | 38 | Human | Binding | pEC50 | = | 7.3 | 7.3 | -7 | 6 | Activation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cells |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/acs.jmedchem.8b01120 | ||
| CHEMBL33567 | 2274 | None | 38 | Human | Binding | pEC50 | = | 7.3 | 7.3 | -7 | 6 | Activation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cells |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/acs.jmedchem.8b01120 | ||
| 1410 | 2274 | None | 38 | Rat | Binding | pEC50 | = | 6.2 | 6.2 | - | 6 | Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6 |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/jm9703597 | ||
| 1412 | 2274 | None | 38 | Rat | Binding | pEC50 | = | 6.2 | 6.2 | - | 6 | Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6 |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/jm9703597 | ||
| 179394 | 2274 | None | 38 | Rat | Binding | pEC50 | = | 6.2 | 6.2 | - | 6 | Effect on Metabotropic glutamate receptor 6Effect on Metabotropic glutamate receptor 6 |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/jm9703597 | ||
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