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ChEMBL ligand: CHEMBL284193 |
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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] | ||||||||
GtoPdb | - | - | 4.1 | pKi | - | - | - | J Neurochem (2000) 75: 2590-601 [PMID:11080213] |
ChEMBL | Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells | B | 4.11 | pKi | 77000 | nM | Ki | J Med Chem (2002) 45: 3171-3183 [PMID:12109902] |
ChEMBL | Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
GtoPdb | - | - | 6.5 | pKi | - | - | - | Neuropharmacology (1999) 38: 1519-29 [PMID:10530814] |
ChEMBL | Binding affinity at Metabotropic glutamate receptor 2 | B | 6.96 | pKi | 110 | nM | Ki | J Med Chem (2002) 45: 3171-3183 [PMID:12109902] |
mGlu2 receptor/Metabotropic glutamate receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2851] [GtoPdb: 290] [UniProtKB: P31421] | ||||||||
GtoPdb | - | - | 7 | pKi | - | - | - |
Br J Pharmacol (1998) 123: 497-504 [PMID:9504391]; Neuropharmacology (2000) 39: 1700-6 [PMID:10884552] |
ChEMBL | Agonist activity at rat mGlu2 receptor by FRET based mGlu sensor assay | B | 6.46 | pEC50 | 350 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR2 in rat | B | 6.52 | pEC50 | 300 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
ChEMBL | Metabotropic glutamate receptor 2 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells | F | 6.52 | pEC50 | 300 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
ChEMBL | Agonist activity at rat mGlu2 receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader | F | 7.35 | pEC50 | 45 | nM | EC50 | J Med Chem (2010) 53: 2797-2813 [PMID:20218620] |
mGlu3 receptor in Human [GtoPdb: 291] [UniProtKB: Q14832] | ||||||||
GtoPdb | - | - | 7.2 | pKi | - | - | - | Neuropharmacology (1999) 38: 1519-29 [PMID:10530814] |
mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422] | ||||||||
GtoPdb | - | - | 6.8 | pKi | - | - | - | Neuropharmacology (2000) 39: 1700-6 [PMID:10884552] |
ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR3 in rat | B | 6.52 | pEC50 | 300 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
ChEMBL | Metabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells | F | 6.7 | pEC50 | 200 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
ChEMBL | Agonist activity at rat mGlu3 receptor by FRET based mGlu sensor assay | B | 7.1 | pEC50 | 80 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423] | ||||||||
ChEMBL | Metabotropic glutamate receptor 4 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells | F | 4.64 | pEC50 | 23000 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349] | ||||||||
ChEMBL | Metabotropic glutamate receptor 6 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells | F | 4.4 | pEC50 | 40000 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
GtoPdb | - | - | 5.6 | pEC50 | - | - | - | Neuropharmacology (1998) 37: 1043-51 [PMID:9833633] |
mGlu7 receptor in Human [GtoPdb: 295] [UniProtKB: Q14831] | ||||||||
GtoPdb | - | - | 4.7 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2000) 362: 546-54 [PMID:11138847] |
mGlu7 receptor/Metabotropic glutamate receptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879] [GtoPdb: 295] [UniProtKB: P35400] | ||||||||
ChEMBL | Metabotropic glutamate receptor 7 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells | F | 4.4 | pEC50 | 40000 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
mGlu8 receptor in Human [GtoPdb: 296] [UniProtKB: O00222] | ||||||||
GtoPdb | - | - | 5.5 | pIC50 | - | - | - | Brain Res Mol Brain Res (1999) 67: 201-10 [PMID:10216218] |
mGlu8 receptor/Metabotropic glutamate receptor 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2718] [GtoPdb: 296] [UniProtKB: P70579] | ||||||||
ChEMBL | Metabotropic glutamate receptor 8 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells | F | 4.49 | pEC50 | 32000 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
GtoPdb | - | - | 4.7 | pIC50 | - | - | - | J Neurochem (2000) 75: 2590-601 [PMID:11080213] |
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]