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]
  • This target only has 1 pki data point
  • 7.74
1 CHEMBL108947_lig_chart_1 M1 receptor Human
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  • M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
  • This target only has 1 pki data point
  • 6.96
2 CHEMBL108947_lig_chart_2 M2 receptor Human
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  • M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
  • This target only has 1 pki data point
  • 7.42
3 CHEMBL108947_lig_chart_3 M3 receptor Human
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  • M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
  • This target only has 1 pki data point
  • 7.21
4 CHEMBL108947_lig_chart_4 M4 receptor Human
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  • M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912]
  • This target only has 1 pki data point
  • 7.04
5 CHEMBL108947_lig_chart_5 M5 receptor Human
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  • H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
  • This target only has 1 pki data point
  • 8.4
6 CHEMBL108947_lig_chart_6 H1 receptor Human
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  • NET in Human [GtoPdb: 926] [UniProtKB: P23975]
  • This target only has 1 pki data point
  • 7.34
7 CHEMBL108947_lig_chart_7 NET Human
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  • SERT in Human [GtoPdb: 928] [UniProtKB: P31645]
  • This target only has 1 pki data point
  • 8.07
8 CHEMBL108947_lig_chart_8 SERT Human
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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 28:

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