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ChEMBL ligand: CHEMBL978 (Methacholine, Methacholine cation, Methacholine ion, Provocholine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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]