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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]