compound 30 [PMID: 21757343] [Ligand Id: 6407] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1808901
  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
  • mGlu5 receptor in Rat [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 (2011) 21: 4891-9 [PMID:21757343]
ChEMBL Displacement of [3H]-MPEP from human mGluR5 expressed in CHO cells after 60 mins B 7.92 pKi 12 nM Ki Bioorg Med Chem Lett (2011) 21: 4891-4899 [PMID:21757343]
ChEMBL Negative allosteric modulation of human mGlu5 receptor expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization after 1 hr by FLIPR assay F 7.77 pIC50 17 nM IC50 Bioorg Med Chem Lett (2011) 21: 4891-4899 [PMID:21757343]
GtoPdb - - 7.77 pIC50 17 nM IC50 Bioorg Med Chem Lett (2011) 21: 4891-9 [PMID:21757343]
mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424]
GtoPdb - - 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2011) 21: 4891-9 [PMID:21757343]

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]