CDPPB [Ligand Id: 1422] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL190270
  • 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 Displacement of [3H]-MPEP from human mGluR5 B 6.6 pKi 250 nM Ki Bioorg Med Chem Lett (2010) 20: 7381-7384 [PMID:21067920]
ChEMBL Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay F 6.75 pEC50 177.83 nM EC50 J Med Chem (2013) 56: 7243-7259 [PMID:23947773]
ChEMBL Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay F 6.75 pEC50 176 nM EC50 J Med Chem (2013) 56: 7243-7259 [PMID:23947773]
ChEMBL Positive allosteric modulation of human mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay F 7.57 pEC50 27 nM EC50 J Med Chem (2013) 56: 7976-7996 [PMID:24050755]
GtoPdb - - 8 pEC50 - - - J Pharmacol Exp Ther (2005) 313: 199-206 [PMID:15608073];
J Med Chem (2004) 47: 5825-8 [PMID:15537338]
ChEMBL Effective concentration against metabotropic glutamate receptor 5 of human transfected into CHO cells B 8 pEC50 10 nM EC50 J Med Chem (2004) 47: 5825-5828 [PMID:15537338]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
ChEMBL Displacement of [3H]methoxyPEPy from rat mGluR5 expressed in HEK293 cells B 5.42 pKi 3760 nM Ki J Med Chem (2006) 49: 3332-3344 [PMID:16722652]
ChEMBL Positive allosteric modulation of rat mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay F 7.01 pEC50 98 nM EC50 J Med Chem (2013) 56: 7976-7996 [PMID:24050755]
ChEMBL Activity at mGluR5 assessed as potentiation of glutamate-induced calcium flux in rat astrocytes F 7.11 pEC50 77 nM EC50 J Med Chem (2006) 49: 3332-3344 [PMID:16722652]
ChEMBL Effective concentration against metabotropic glutamate receptor 5 of rat B 7.7 pEC50 20 nM EC50 J Med Chem (2004) 47: 5825-5828 [PMID:15537338]
GtoPdb - - 7.7 pEC50 - - - J Med Chem (2004) 47: 5825-8 [PMID:15537338]

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]