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 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]