compound 10 [PMID: 15482906] [Ligand Id: 6450] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL186151
  • 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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
GtoPdb - - 7.92 pKi 12 nM Ki Bioorg Med Chem Lett (2004) 14: 5473-6 [PMID:15482906]
GtoPdb - - 8.17 pIC50 6.7 nM IC50 Bioorg Med Chem Lett (2004) 14: 5473-6 [PMID:15482906]
ChEMBL Antagonistic activity against Metabotropic glutamate receptor 5 in [Ca2+] flux assay using glutamate (10 uM) as agonist F 8.17 pIC50 6.7 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 5473-5476 [PMID:15482906]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
ChEMBL Binding affinity towards Metabotropic glutamate receptor was determined by displacing [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from rat cortical membranes B 7.92 pKi 12 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 5481-5484 [PMID:15482908]
ChEMBL Binding affinity towards Metabotropic glutamate receptor was determined by displacing [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from rat cortical membranes B 7.92 pKi 12 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 5473-5476 [PMID:15482906]
ChEMBL Displacement of [3H]-3-methoxy-5-(pyridin-2-ylethynyl)pyridine from mGlu5R in rat cortical membranes by liquid scintillation spectrometric analysis B 7.92 pKi 12 nM Ki Bioorg. Med. Chem. Lett. (2016) 26: 484-494 [PMID:26706173]

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]