triflupromazine [Ligand Id: 4330] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL570 (Fluopromazine, Nivoman, Triflupromazine, Vesprin, Vetame)
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  • Pleiotropic ABC efflux transporter of multiple drugs in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL1697658] [UniProtKB: P33302]
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  • Trypanothione reductase in Trypanosoma cruzi [ChEMBL: CHEMBL5131] [UniProtKB: P28593]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908]
ChEMBL Inhibition of Equine serum BChE using butyrylthiocholine iodide as a substrate after 20 mins by Ellman's assay B 5.13 pIC50 7400 nM IC50 Eur J Med Chem (2011) 46: 2170-2184 [PMID:21459491]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL Concentration giving half of the maximal ATPase activity calculated for the high-affinity binding site of the CHO P-Glycoprotein (P-gp) in two-affinity model B 4.8 pKi 15700 nM Ki J Med Chem (2002) 45: 5671-5686 [PMID:12477351]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL DNDI: Malaria in Vitro, 72 hour F 5.57 pIC50 2720 nM IC50 Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning
Pleiotropic ABC efflux transporter of multiple drugs in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697658] [UniProtKB: P33302]
ChEMBL Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay B 5.31 pIC50 4900 nM IC50 Antimicrob Agents Chemother (2009) 53: 1516-1527 [PMID:19188399]
Trypanothione reductase in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5131] [UniProtKB: P28593]
ChEMBL Inhibitory activity against recombinant Trypanosoma cruzi (Trypanosoma cruzi) Trypanothione reductase (linear competitive type) B 4.52 pKi 30200 nM Ki J Med Chem (1998) 41: 148-156 [PMID:9457238]

ChEMBL data shown on this page come from version 32:

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]