methacholine [Ligand Id: 7438] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL978 (Methacholine, Methacholine cation, Methacholine ion, Provocholine)
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Rat [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
  • M4 receptor/Muscarinic acetylcholine receptor M4 in Rat [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
ChEMBL Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1 F 6.4 pEC50 400 nM EC50 J Med Chem (1998) 41: 2047-2055 [PMID:9622546]
GtoPdb - - 6.4 pEC50 400 nM EC50 Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715];
J Med Chem (1998) 41: 2047-55 [PMID:9622546]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M2 B 7.23 pKi 59 nM Ki J Med Chem (1998) 41: 2047-2055 [PMID:9622546]
ChEMBL Inhibitory activity against [3H]quinuclidinyl Benzilate binding to Muscarinic acetylcholine receptor M2 in the presence of GTP B 5.28 pIC50 5200 nM IC50 J Med Chem (1998) 41: 2047-2055 [PMID:9622546]
ChEMBL Inhibitory activity against [3H]quinuclidinyl Benzilate binding to Muscarinic acetylcholine receptor M2 in the absence of GTP B 6.42 pIC50 380 nM IC50 J Med Chem (1998) 41: 2047-2055 [PMID:9622546]
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
ChEMBL Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M2 in rat cerebral cortical membranes B 7.23 pKi 59 nM Ki J Med Chem (1998) 41: 2047-2055 [PMID:9622546]
GtoPdb - - 7.23 pKi 59 nM Ki Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715];
J Med Chem (1998) 41: 2047-55 [PMID:9622546]
ChEMBL Inhibition of binding of 0.1 nM [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M2 in rat cerebral cortical membranes of transfected CHO cells in the presence of 10 uM GTP B 5.28 pIC50 5200 nM IC50 J Med Chem (1998) 41: 2047-2055 [PMID:9622546]
ChEMBL Inhibition of binding of 0.1 nM [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M2 in rat cerebral cortical membranes of transfected CHO cells in the absence of GTP B 6.42 pIC50 380 nM IC50 J Med Chem (1998) 41: 2047-2055 [PMID:9622546]
M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
GtoPdb - - 6.92 pEC50 120 nM EC50 Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715];
J Med Chem (1998) 41: 2047-55 [PMID:9622546]
ChEMBL Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3 F 6.92 pEC50 120 nM EC50 J Med Chem (1998) 41: 2047-2055 [PMID:9622546]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4 B 5.8 pKi 1600 nM Ki J Med Chem (1998) 41: 2047-2055 [PMID:9622546]
M4 receptor/Muscarinic acetylcholine receptor M4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485]
ChEMBL Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes B 5.8 pKi 1600 nM Ki J Med Chem (1998) 41: 2047-2055 [PMID:9622546]
GtoPdb - - 5.8 pKi 1600 nM Ki Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715];
J Med Chem (1998) 41: 2047-55 [PMID:9622546]
ChEMBL Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4 F 6.15 pIC50 700 nM IC50 J Med Chem (1998) 41: 2047-2055 [PMID:9622546]

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]