trimipramine [Ligand Id: 7317] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL644 (7162 RP, 7162-RP, IL 6001, IL-6001, Surmontil, Trimeproprimine, Trimipramina, Trimipramine)
  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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  • Cav2.2/Voltage-gated N-type calcium channel alpha-1B subunit in Human [ChEMBL: CHEMBL4478] [GtoPdb: 533] [UniProtKB: Q00975]
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  • NET in Human [GtoPdb: 926] [UniProtKB: P23975]
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  • DAT in Human [GtoPdb: 927] [UniProtKB: Q01959]
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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
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy B 4.56 pIC50 27700 nM IC50 J Med Chem (2008) 51: 5932-5942 [PMID:18788725]
Cav2.2/Voltage-gated N-type calcium channel alpha-1B subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4478] [GtoPdb: 533] [UniProtKB: Q00975]
ChEMBL Inhibition of endogenous human CaV2.2 in human SH-SY5Y cells in presence of nifedipine by Calcium 4 dye based calcium influx fluorescence-imaging assay B 4.96 pIC50 11000 nM IC50 RSC Med Chem (2022) 13: 183-195 [PMID:35308021]
NET in Human [GtoPdb: 926] [UniProtKB: P23975]
GtoPdb - - 5.61 pKi 2450 nM Ki Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821]
DAT in Human [GtoPdb: 927] [UniProtKB: Q01959]
GtoPdb - - 5.42 pKi 3780 nM Ki Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821]
SERT in Human [GtoPdb: 928] [UniProtKB: P31645]
GtoPdb - - 6.83 pKi 149 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]