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ChEMBL ligand: CHEMBL143210 (4-[Amino(Carboxy)Methyl]Phthalic Acid) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385] | ||||||||
ChEMBL | Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat | F | 4.49 | pEC50 | 32000 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
mGlu2 receptor/Metabotropic glutamate receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2851] [GtoPdb: 290] [UniProtKB: P31421] | ||||||||
ChEMBL | Metabotropic glutamate receptor 2 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422] | ||||||||
ChEMBL | Metabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
mGlu4 receptor/Metabotropic glutamate receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833] | ||||||||
GtoPdb | - | - | 5.1 | pEC50 | - | - | - | Neuropharmacology (2001) 40: 311-8 [PMID:11166323] |
ChEMBL | Agonist activity at mGlu4 (unknown 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 | F | 5.49 | pEC50 | 3200 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
ChEMBL | Agonist activity at mGlu4 (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 | F | 5.71 | pEC50 | 1960 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423] | ||||||||
ChEMBL | Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Active | F | 4 | pEC50 | <100000 | nM | EC50 | J Med Chem (2005) 48: 2534-2547 [PMID:15801843] |
ChEMBL | Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells | F | 5.06 | pEC50 | 8800 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
ChEMBL | Stimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells | F | 5.06 | pEC50 | 8800 | nM | EC50 | J Med Chem (2005) 48: 2534-2547 [PMID:15801843] |
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
ChEMBL | Metabotropic glutamate receptor 5 agonist activity as basal [3H]- IP formation in rat | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
mGlu6 receptor/Metabotropic glutamate receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303] | ||||||||
GtoPdb | - | - | 5.4 | pEC50 | 3980 | nM | EC50 | Neuropharmacology (2001) 40: 311-8 [PMID:11166323] |
ChEMBL | 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 assay | F | 5.49 | pEC50 | 3200 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349] | ||||||||
ChEMBL | Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells | F | 5.44 | pEC50 | 3600 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
mGlu7 receptor/Metabotropic glutamate receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831] | ||||||||
ChEMBL | Agonist activity at mGlu7 (unknown 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 | F | 4.52 | pEC50 | >=30000 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
mGlu7 receptor/Metabotropic glutamate receptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879] [GtoPdb: 295] [UniProtKB: P35400] | ||||||||
ChEMBL | Metabotropic glutamate receptor 7 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
mGlu8 receptor/Metabotropic glutamate receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222] | ||||||||
ChEMBL | Agonist activity at mGlu8 (unknown 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 | F | 7.36 | pEC50 | 44 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
GtoPdb | - | - | 7.5 | pEC50 | - | - | - | Neuropharmacology (2001) 40: 311-8 [PMID:11166323] |
ChEMBL | Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cells | B | 7.51 | pEC50 | 31 | nM | EC50 | J Med Chem (2018) 61: 10040-10052 [PMID:30365309] |
ChEMBL | Agonist activity at mGlu8 (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 | F | 7.64 | pEC50 | 23 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
mGlu8 receptor/Metabotropic glutamate receptor 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2718] [GtoPdb: 296] [UniProtKB: P70579] | ||||||||
ChEMBL | Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells | F | 7.51 | pEC50 | 31 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]