A-794282 [Ligand Id: 6211] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL385336
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Human [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
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  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Human [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
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  • mGlu4 receptor/Metabotropic glutamate receptor 4 in Human [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833]
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  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
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  • mGlu7 receptor/Metabotropic glutamate receptor 7 in Human [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831]
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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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]