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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

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]
There should be some charts here, you may need to enable JavaScript!
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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]