A-794282 [Ligand Id: 6211] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL385336 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255] | ||||||||
| GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2005) 48: 7374-88 [PMID:16279797] |
| ChEMBL | Antagonist activity at human mGluR1 expressed in 1321N1 cells | F | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4936-4940 [PMID:16809035] |
| ChEMBL | Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization | F | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2005) 48: 7374-7388 [PMID:16279797] |
| ChEMBL | Antagonist activity at mGlu1 receptor | F | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2007) 50: 2563-2568 [PMID:17489573] |
| mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385] | ||||||||
| ChEMBL | Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranes | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2005) 48: 7374-7388 [PMID:16279797] |
| ChEMBL | Antagonist activity at rat mGluR1 expressed in 1321N1 cells | F | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4936-4940 [PMID:16809035] |
| GtoPdb | - | - | 8.33 | pIC50 | 4.7 | nM | IC50 | Eur J Pharmacol (2008) 580: 314-21 [PMID:18054908] |
| ChEMBL | Inhibition of rat mGluR1 | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2008) 43: 1025-1034 [PMID:17822809] |
| ChEMBL | Inhibition of rat mGluR1 | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2008) 43: 1025-1034 [PMID:17822809] |
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
| ChEMBL | Antagonist activity at human mGluR2 expressed in 1321N1 cells | F | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4936-4940 [PMID:16809035] |
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833] | ||||||||
| ChEMBL | Antagonist activity at human mGluR4 expressed in 1321N1 cells | F | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4936-4940 [PMID:16809035] |
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594] | ||||||||
| ChEMBL | Antagonist activity at human mGluR5 expressed in 1321N1 cells | F | 6.35 | pIC50 | 442 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4936-4940 [PMID:16809035] |
| ChEMBL | Antagonist activity at human mGluR5 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization | F | 6.35 | pIC50 | 442 | nM | IC50 | J Med Chem (2005) 48: 7374-7388 [PMID:16279797] |
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
| ChEMBL | Displacement of [3H]MPEP from rat cortex mGluR5 | B | 6.71 | pKi | 194 | nM | Ki | J Med Chem (2005) 48: 7374-7388 [PMID:16279797] |
| ChEMBL | Antagonist activity at rat mGluR5 expressed in 1321N1 cells | F | 5.88 | pIC50 | 1330 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4936-4940 [PMID:16809035] |
| mGlu7 receptor/Metabotropic glutamate receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831] | ||||||||
| ChEMBL | Antagonist activity at human mGluR7 expressed in 1321N1 cells | F | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4936-4940 [PMID:16809035] |
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]
