carbachol [Ligand Id: 298] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL965 (Carbachol, Carbastat, Miostat) |
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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 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]
