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Literature summary extracted from

  • Torrie, L.S.; Wyllie, S.; Spinks, D.; Oza, S.L.; Thompson, S.; Harrison, J.R.; Gilbert, I.H.; Wyatt, P.G.; Fairlamb, A.H.; Frearson, J.A.
    Chemical validation of trypanothione synthetase: a potential drug target for human trypanosomiasis (2009), J. Biol. Chem., 284, 36137-36145.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
6.3.1.9 1-[3-(3-fluorophenyl)-1H-indazol-1-yl]-3,3-dimethylbutan-2-one i.e. DDD85811, inhibits growth of bloodstream Trypanosoma brucei in vitro Trypanosoma brucei
6.3.1.9 2-[3-(3-fluorophenyl)-1H-indazol-1-yl]-1-(piperidin-1-yl)ethanone i.e. DDD86243, inhibits growth of bloodstream Trypanosoma brucei in vitro. Exposure to DDD86243 at 2 x EC50 for 72 h decreases intracellular trypanothione levels to less than 10% of wild type, with a corresponding 5fold increase in the precursor metabolite, glutathione Trypanosoma brucei

Organism

EC Number Organism UniProt Comment Textmining
6.3.1.9 Trypanosoma brucei
-
-
-

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
6.3.1.9 0.000095
-
 pH 8.0, 22°C Trypanosoma brucei 1-[3-(3-fluorophenyl)-1H-indazol-1-yl]-3,3-dimethylbutan-2-one
6.3.1.9 0.00014
-
 pH 8.0, 22°C Trypanosoma brucei 2-[3-(3-fluorophenyl)-1H-indazol-1-yl]-1-(piperidin-1-yl)ethanone