AQW051 [Ligand Id: 7371] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4532388
  • nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
GtoPdb - - 7.57 pKi 27 nM Ki MEDI 222: Identification of AQW051, an alpha7 nicotinic acetylcholine receptor partial agonist for the treatment of cognitive impairment associated with schizophrenia.. ACS Med Chem Meeting Abstracts, March 2014
ChEMBL Partial agonist activity at human alpha7 nAChR expressed in Xenopus laevis oocytes at holding potential of -90 mV by patch clamp electrophysiological method B 7.41 pEC50 39 nM EC50 Eur J Med Chem (2018) 160: 37-48 [PMID:30317024]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]