CPPZ [Ligand Id: 6416] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1289113
  • 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]
ChEMBL Displacement of [3H]-MPEP from human mGluR5 B 5.63 pKi 2370 nM Ki Bioorg Med Chem Lett (2010) 20: 7381-7384 [PMID:21067920]
ChEMBL Positive allosteric modulation of human mGluR5 expressed in HEK293 cells assessed as Ca2+ influx by FLIPR assay F 6.26 pEC50 550 nM EC50 Bioorg Med Chem Lett (2010) 20: 7381-7384 [PMID:21067920]
ChEMBL Positive allosteric modulation of human mGluR5 over-expressed in HEK293 cells B 6.26 pEC50 550 nM EC50 J Med Chem (2013) 56: 7976-7996 [PMID:24050755]
GtoPdb - - 6.3 pEC50 500 nM EC50 Eur J Pharmacol (2011) 659: 146-54 [PMID:21335002]
mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424]
GtoPdb - - 5.51 pKi 3100 nM Ki Eur J Pharmacol (2011) 659: 146-54 [PMID:21335002]

ChEMBL data shown on this page come from version 32:

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]