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

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ChEMBL ligand: CHEMBL978 (Provocholine, Methacholine)
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
  • This target only has 0 pki data point
  • 0
1 CHEMBL978_lig_chart_1 Muscarinic acetylcholine receptor M1 Rat
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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]
  • 7.23
2 CHEMBL978_lig_chart_2 Muscarinic acetylcholine receptor M2 HumanRat
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Rat [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
  • This target only has 0 pki data point
  • 0
3 CHEMBL978_lig_chart_3 Muscarinic acetylcholine receptor M3 Rat
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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]
  • 5.8
4 CHEMBL978_lig_chart_4 Muscarinic acetylcholine receptor M4 HumanRat
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]