aclidinium [Ligand Id: 7449] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1194325 (Aclidinium, Aclidinium cation, Aclidinium ion) |
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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) |
| ChEMBL | [3H]-NMS Binding Assay: 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. For determination of IC, membrane preparations were suspended in DPBS to a final concentration of 89 μg/ml for the Hm3 subtype. The membrane suspension was incubated with the tritiated compound for 60 min. After incubation the membrane fraction was separated by filtration and the bound radioactivity determined. Non specific binding was determined by addition of 10^−4 M atropine. At least six concentrations were assayed in duplicate to generate individual displacement curves. | B | 8.36 | pIC50 | 4.4 | nM | IC50 | US-9687478-B2. Quinuclidine derivatives and medicinal compositions containing the same (2017) |
| 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 36:
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]
