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 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]