aclidinium [Ligand Id: 7449] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1194325 (Aclidinium, Aclidinium cation, Aclidinium ion)
  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M1 receptor in Human [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
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  • M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
GtoPdb - - 10.2 pKi - - - J Med Chem (2009) 52: 5076-92 [PMID:19653626];
Bioorg Med Chem Lett (2010) 20: 7429-34 [PMID:21036042]
ChEMBL [3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used. B 8.36 pIC50 4.4 nM IC50 US-9333195-B2. Quinuclidine derivatives and medicinal compositions containing the same (2016)
M1 receptor in Human [GtoPdb: 13] [UniProtKB: P11229]
GtoPdb - - 10.2 pIC50 - - IC50 J Med Chem (2009) 52: 5076-92 [PMID:19653626];
Bioorg Med Chem Lett (2010) 20: 7429-34 [PMID:21036042]
M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
GtoPdb - - 10.1 pIC50 - - IC50 J Med Chem (2009) 52: 5076-92 [PMID:19653626];
Bioorg Med Chem Lett (2010) 20: 7429-34 [PMID:21036042]
M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
GtoPdb - - 10 pKi - - - Bioorg Med Chem Lett (2010) 20: 7429-34 [PMID:21036042]
M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912]
GtoPdb - - 9.9 pKi - - - Bioorg Med Chem Lett (2010) 20: 7429-34 [PMID:21036042]

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]