dosulepin [Ligand Id: 7549] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL108947 (Dothiepin)
  • M1 receptor in Human [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912]
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  • H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
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  • NET in Human [GtoPdb: 926] [UniProtKB: P23975]
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  • SERT in Human [GtoPdb: 928] [UniProtKB: P31645]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
M1 receptor in Human [GtoPdb: 13] [UniProtKB: P11229]
GtoPdb - - 7.74 pKi 18 nM Ki Biochem Pharmacol (1993) 45: 2352-4 [PMID:8100134]
M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
GtoPdb - - 6.96 pKi 109 nM Ki Biochem Pharmacol (1993) 45: 2352-4 [PMID:8100134]
M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
GtoPdb - - 7.42 pKi 38 nM Ki Biochem Pharmacol (1993) 45: 2352-4 [PMID:8100134]
M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
GtoPdb - - 7.21 pKi 61 nM Ki Biochem Pharmacol (1993) 45: 2352-4 [PMID:8100134]
M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912]
GtoPdb - - 7.04 pKi 92 nM Ki Biochem Pharmacol (1993) 45: 2352-4 [PMID:8100134]
H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 8.4 pKi 4 nM Ki Cell Mol Neurobiol (1999) 19: 467-89 [PMID:10379421]
NET in Human [GtoPdb: 926] [UniProtKB: P23975]
GtoPdb - - 7.34 pKi 46 nM Ki Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821]
SERT in Human [GtoPdb: 928] [UniProtKB: P31645]
GtoPdb - - 8.07 pKi 8.6 nM Ki Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821]

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]