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 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]