compound 8 [PMID: 15482908] [Ligand Id: 6448] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL187107
  • 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]
ChEMBL Inhibitory concentration towards human glutamate receptor 5 in calcium flux assay F 8.4 pIC50 4 nM IC50 J. Med. Chem. (2004) 47: 4645-4648 [PMID:15341479]
ChEMBL Antagonistic activity against Metabotropic glutamate receptor 5 in [Ca2+] flux assay using glutamate (10 uM) as agonist F 8.41 pIC50 3.9 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 5473-5476 [PMID:15482906]
GtoPdb - - 8.41 pIC50 3.9 nM IC50 Bioorg Med Chem Lett (2004) 14: 5481-4 [PMID:15482908]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
GtoPdb - - 7.85 pKi 14 nM Ki Bioorg Med Chem Lett (2004) 14: 5481-4 [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 7.85 pKi 14 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 7.85 pKi 14 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 5473-5476 [PMID:15482906]
ChEMBL Binding affinity towards Metabotropic glutamate receptor was determined by displacing [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from rat cortical membranes B 7.85 pKi 14 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 5477-5480 [PMID:15482907]
ChEMBL Ability to displace [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from binding to metabotropic glutamate receptor 5 in rat cortical membranes B 7.85 pKi 14 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 5061-5064 [PMID:16183275]
ChEMBL Displacement of [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from glutamate 5 receptor of rat cortical membranes B 8 pKi 10 nM Ki J. Med. Chem. (2004) 47: 4645-4648 [PMID:15341479]
ChEMBL Antagonistic activity against Metabotropic glutamate receptor 5 in [Ca2+] flux assay using glutamate (10 uM) as agonist F 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 5477-5480 [PMID:15482907]
ChEMBL In vitro functional activity measured by changes in cytosolic [Ca2+] concentrations against rat metabotropic glutamate receptor 5 F 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 5061-5064 [PMID:16183275]

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]