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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]