doxepin [Ligand Id: 1225] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL860
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
  • This target only has 1 pki data point
  • 7.6
1 CHEMBL860_lig_chart_1 Serotonin 2b (5-HT2b) receptor Human
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  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
  • This target only has 0 pki data point
  • 0
2 CHEMBL860_lig_chart_2 Tyrosine-protein kinase receptor RET Human
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  • H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
  • This target only has 1 pki data point
  • 10
3 CHEMBL860_lig_chart_3 H1 receptor Human
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  • NET in Human [GtoPdb: 926] [UniProtKB: P23975]
  • This target only has 1 pki data point
  • 7.54
4 CHEMBL860_lig_chart_4 NET Human
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  • SERT in Human [GtoPdb: 928] [UniProtKB: P31645]
  • This target only has 1 pki data point
  • 7.17
5 CHEMBL860_lig_chart_5 SERT Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method B 7.6 pKi 25.3 nM Ki ACS Med Chem Lett (2018) 9: 1019-1024 [PMID:30344910]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Kinase Assay: Approximately 5-20 μg of purified GST-RET proteins were incubated with 1 mM ATP in 20 μL kinase buffer (10 mM Tris-HCl, 5 mM MgCl2, pH 7.4), at 30° C. for 30 minutes. The kinase reactions were terminated by boiling the samples in SDS-PAGE sample buffer. Samples were resolved on 10% acrylamide gels by SDS-PAGE followed by Western blotting. Phosphorylation was detected using a pan-phosphotyrosine pY99 antibody (available from Santa Cruz Biotechnology) or RET phospho-specific antibody (pY905, available from Cell Signaling, Beverly, Mass., USA). B 4.7 pIC50 >20000 nM IC50 US-8629135-B2. Pharmaceutical compositions comprising RET inhibitors and methods for the treatment of cancer (2014)
H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 10 pKi - - - J Pharmacol Exp Ther (2002) 302: 328-36 [PMID:12065734]
NET in Human [GtoPdb: 926] [UniProtKB: P23975]
GtoPdb - - 7.54 pKi 29 nM Ki National Toxicology Program: Dept of Health and Human Services.. DrugMatrix
SERT in Human [GtoPdb: 928] [UniProtKB: P31645]
GtoPdb - - 7.17 pKi 68 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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]