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 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]
