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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
