ADX-47273 [Ligand Id: 1420] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL381055 (ADX-47273)
  • 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 Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay F 6.7 pEC50 199.53 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 6.7 pEC50 199 nM EC50 J. Med. Chem. (2013) 56: 7243-7259 [PMID:23947773]
GtoPdb - - 6.8 pEC50 157 nM EC50 Neuropharmacology (2013) 64: 224-39 [PMID:22884720]
ChEMBL Positive allosteric modulation of human mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay F 6.8 pEC50 157 nM EC50 J. Med. Chem. (2013) 56: 7976-7996 [PMID:24050755]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
GtoPdb - - 5.44 pKi 3650 nM Ki Neuropharmacology (2013) 64: 224-39 [PMID:22884720]
GtoPdb - - 6.5 pIC50 - - - Neuropharmacology (2005) 49 (S1): 252-
ChEMBL Activity at mGluR5 assessed as potentiation of glutamate-induced calcium flux in rat astrocytes F 6.77 pEC50 170 nM EC50 J. Med. Chem. (2006) 49: 3332-3344 [PMID:16722652]
ChEMBL Positive allosteric modulation of rat mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay F 7.26 pEC50 55 nM EC50 J. Med. Chem. (2013) 56: 7976-7996 [PMID:24050755]
GtoPdb - - 7.26 pEC50 55 nM EC50 Neuropharmacology (2013) 64: 224-39 [PMID:22884720]

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]