A-794278 [Ligand Id: 6354] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL225032
  • 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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  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
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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 pIC50 10 nM IC50 J Med Chem (2005) 48: 7374-88 [PMID:16279797]
ChEMBL Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization F 9 pIC50 1 nM IC50 J. Med. Chem. (2005) 48: 7374-7388 [PMID:16279797]
mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
GtoPdb - - 8.27 pKi 5.4 nM Ki Eur J Pharmacol (2008) 580: 314-21 [PMID:18054908]
ChEMBL Inhibition of rat mGluR1 B 9 pIC50 1 nM IC50 Eur. J. Med. Chem. (2008) 43: 1025-1034 [PMID:17822809]
ChEMBL Inhibition of rat mGluR1 B 9 pIC50 1 nM IC50 Eur. J. Med. Chem. (2008) 43: 1025-1034 [PMID:17822809]
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 assessed as effect on L-glutamate-induced calcium mobilization F 6.83 pIC50 147 nM IC50 J. Med. Chem. (2005) 48: 7374-7388 [PMID:16279797]

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]