carbachol [Ligand Id: 298] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL965 (Carbachol, Carbastat, Miostat)
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • M1 receptor in Rat [GtoPdb: 13] [UniProtKB: P08482]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human [ChEMBL: CHEMBL1907589] [GtoPdb: 472, 465] [UniProtKB: P17787, P43681]
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  • nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
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  • M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
  • M2 receptor in Rat [GtoPdb: 14] [UniProtKB: P10980]
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  • M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
  • M3 receptor in Rat [GtoPdb: 15] [UniProtKB: P08483]
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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
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
GtoPdb - - 5.3 pKi - - - Mol Pharmacol (1997) 52: 172-9 [PMID:9224827];
Mol Pharmacol (1998) 53: 1120-30 [PMID:9614217];
Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594]
ChEMBL Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay B 4.73 pEC50 18620.87 nM EC50 J. Med. Chem. (2014) 57: 9065-9077 [PMID:25275964]
ChEMBL Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay B 5.8 pEC50 1584.89 nM EC50 J. Med. Chem. (2014) 57: 9065-9077 [PMID:25275964]
ChEMBL Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assay B 6.2 pEC50 630.96 nM EC50 J. Med. Chem. (2014) 57: 9065-9077 [PMID:25275964]
M1 receptor in Rat [GtoPdb: 13] [UniProtKB: P08482]
GtoPdb - - 3.9 pKi - - - J Pharmacol Exp Ther (2002) 303: 29-35 [PMID:12235229]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
GtoPdb - - 4.9 pKi - - - Mol Pharmacol (1997) 52: 172-9 [PMID:9224827];
Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594]
ChEMBL Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay B 5.18 pEC50 6606.93 nM EC50 J. Med. Chem. (2014) 57: 9065-9077 [PMID:25275964]
ChEMBL Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay B 5.64 pEC50 2290.87 nM EC50 J. Med. Chem. (2014) 57: 9065-9077 [PMID:25275964]
ChEMBL Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay B 6.81 pEC50 154.88 nM EC50 J. Med. Chem. (2014) 57: 9065-9077 [PMID:25275964]
nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907589] [GtoPdb: 472, 465] [UniProtKB: P17787, P43681]
ChEMBL Binding affinity to alpha4beta2 nAChR (unknown origin) B 6.12 pKi 750 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 6481-6485 [PMID:24128660]
nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
ChEMBL Binding affinity to alpha7 nAChR (unknown origin) B 4.18 pKi 66000 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 6481-6485 [PMID:24128660]
M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
GtoPdb - - 5.7 pKi - - - J Pharmacol Exp Ther (2002) 303: 29-35 [PMID:12235229];
Mol Pharmacol (1997) 52: 172-9 [PMID:9224827]
M2 receptor in Rat [GtoPdb: 14] [UniProtKB: P10980]
GtoPdb - - 5.7 pKi - - - J Pharmacol Exp Ther (1998) 284: 500-7 [PMID:9454790]
M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
GtoPdb - - 4.4 pKi - - - J Pharmacol Exp Ther (2002) 303: 29-35 [PMID:12235229];
Mol Pharmacol (1997) 52: 172-9 [PMID:9224827];
Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594]
M3 receptor in Rat [GtoPdb: 15] [UniProtKB: P08483]
GtoPdb - - 4.2 pKi - - - J Pharmacol Exp Ther (2002) 303: 29-35 [PMID:12235229]
M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912]
GtoPdb - - 4.9 pKi - - - Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594];
J Pharmacol Exp Ther (2005) 315: 313-9 [PMID:16002459];
Mol Pharmacol (2016) 90: 427-36 [PMID:27461343]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]