bethanechol [Ligand Id: 297] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1482 (Bethanechol)
  • Muscarinic acetylcholine receptor M3 in Guinea pig [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
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  • M1 receptor in Human [GtoPdb: 13] [UniProtKB: P11229]
  • M1 receptor in Rat [GtoPdb: 13] [UniProtKB: P08482]
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  • M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Muscarinic acetylcholine receptor M3 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
ChEMBL Binding affinity to muscarinic M3 receptor in guinea-pig ileum B 4.9 pKd 12589.25 nM Kd Bioorg Med Chem (2007) 15: 7626-7637 [PMID:17889543]
ChEMBL Agonist activity at muscarinic M3 receptor in guinea-pig ileum F 6.37 pEC50 426.58 nM EC50 Bioorg Med Chem (2007) 15: 7626-7637 [PMID:17889543]
Muscarinic receptor 2 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075061] [UniProtKB: Q8VH27]
ChEMBL Agonist activity at muscarinic M2 receptor in albino guinea pig left atrium assessed as stimulation of electrically-induced response B 5.85 pEC50 1412.54 nM EC50 Eur J Med Chem (2014) 75: 222-232 [PMID:24534538]
ChEMBL Agonist activity at muscarinic M3 receptor in albino guinea pig ileum assessed as stimulation of electrically-induced response B 6 pEC50 1000 nM EC50 Eur J Med Chem (2014) 75: 222-232 [PMID:24534538]
M1 receptor in Human [GtoPdb: 13] [UniProtKB: P11229]
GtoPdb - - 4 pKi - - - Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715];
Mol Pharmacol (1997) 52: 172-9 [PMID:9224827]
M1 receptor in Rat [GtoPdb: 13] [UniProtKB: P08482]
GtoPdb - - 3.7 pKi - - - J Pharmacol Exp Ther (1989) 248: 661-70 [PMID:2537406]
M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
GtoPdb - - 4 pKi - - - Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715];
Mol Pharmacol (1997) 52: 172-9 [PMID:9224827]
M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
GtoPdb - - 4.2 pKi - - - Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715];
Mol Pharmacol (1997) 52: 172-9 [PMID:9224827]
M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
GtoPdb - - 4 pKi - - - Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715];
Mol Pharmacol (1997) 52: 172-9 [PMID:9224827]

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]