glycopyrrolate [Ligand Id: 7459] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1201335 (Glycopyrrolate cation, Glycopyrrolate ion, Glycopyrronium, Glycopyrronium cation, Glycopyrronium, erythro-, Glycopyrronium ion)
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • 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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  • 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
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
GtoPdb - - 9.5 pIC50 - - IC50 Bioorg Med Chem Lett (2010) 20: 7458-61 [PMID:21036043];
J Pharmacol Exp Ther (2012) 343: 520-8 [PMID:22854200]
ChEMBL Displacement of [3H]NMS from recombinant human M2 receptor expressed in CHO-K1 cells after 16 hrs B 9.8 pIC50 0.16 nM IC50 Bioorg Med Chem Lett (2011) 21: 7440-7446 [PMID:22047691]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs B 9.6 pIC50 0.25 nM IC50 Bioorg Med Chem Lett (2011) 21: 7440-7446 [PMID:22047691]
GtoPdb Assay uses glycopyrronium bromide - 9.8 pIC50 - - IC50 Bioorg Med Chem Lett (2010) 20: 7458-61 [PMID:21036043];
J Pharmacol Exp Ther (2012) 343: 520-8 [PMID:22854200]
ChEMBL Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method B 9.9 pIC50 0.13 nM IC50 Bioorg Med Chem Lett (2013) 23: 6248-6253 [PMID:24144851]
M1 receptor in Human [GtoPdb: 13] [UniProtKB: P11229]
GtoPdb Assay uses glycopyrronium bromide - 10.1 pIC50 - - IC50 Bioorg Med Chem Lett (2010) 20: 7458-61 [PMID:21036043];
J Pharmacol Exp Ther (2012) 343: 520-8 [PMID:22854200]
M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
GtoPdb - - 10 pKi - - - Bioorg Med Chem Lett (2010) 20: 7458-61 [PMID:21036043];
J Pharmacol Exp Ther (2012) 343: 520-8 [PMID:22854200]
M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912]
GtoPdb - - 9.9 pKi - - - Bioorg Med Chem Lett (2010) 20: 7458-61 [PMID:21036043];
J Pharmacol Exp Ther (2012) 343: 520-8 [PMID:22854200]

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]