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Literature summary extracted from

  • Fujii, N.; Mallari, J.P.; Hansell, E.J.; Mackey, Z.; Doyle, P.; Zhou, Y.M.; Gut, J.; Rosenthal, P.J.; McKerrow, J.H.; Guy, R.K.
    Discovery of potent thiosemicarbazone inhibitors of rhodesain and cruzain (2005), Bioorg. Med. Chem. Lett., 15, 121-123.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.51 (1E)-1-(3,4-dichlorophenyl)-2-phenylethan-1-one thiosemicarbazone IC50: 80 nM Trypanosoma cruzi
3.4.22.51 (1E)-1-(3,4-dichlorophenyl)-3-phenylpropan-1-one thiosemicarbazone IC50: 40 nM Trypanosoma cruzi
3.4.22.51 (1E)-1-(3,4-dichlorophenyl)pentan-1-one thiosemicarbazone IC50: 19 nM Trypanosoma cruzi
3.4.22.51 (1E)-1-(3,4-dichlorophenyl)propan-1-one thiosemicarbazone IC50: 30 nM Trypanosoma cruzi
3.4.22.51 (1E)-1-(3-bromophenyl)propan-1-one thiosemicarbazone IC50: 310 nM Trypanosoma cruzi
3.4.22.51 (1E,2E)-1-(3,4-dichlorophenyl)-3-phenylprop-2-en-1-one thiosemicarbazone IC50: 30 nM Trypanosoma cruzi
3.4.22.51 (1Z)-1-(3,4-dichlorophenyl)-2-phenoxyethan-1-one thiosemicarbazone IC50: 30 nM Trypanosoma cruzi
3.4.22.51 (E)-(3,4-dichlorophenyl)(2-phenylcyclopropyl)methanone thiosemicarbazone IC50: 30 nM Trypanosoma cruzi
3.4.22.51 (E)-(3,4-dichlorophenyl)(4-methylphenyl)methanone thiosemicarbazone IC50: 40 nM Trypanosoma cruzi
3.4.22.51 (E)-cyclohexyl(3,4-dichlorophenyl)methanone thiosemicarbazone IC50: 3000 nM Trypanosoma cruzi

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.51 Trypanosoma cruzi
-
-
-

Synonyms

EC Number Synonyms Comment Organism
3.4.22.51 cruzain
-
 Trypanosoma cruzi

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.22.51 0.000019
-
 IC50: 19 nM Trypanosoma cruzi (1E)-1-(3,4-dichlorophenyl)pentan-1-one thiosemicarbazone
3.4.22.51 0.00003
-
 IC50: 30 nM Trypanosoma cruzi (1E)-1-(3,4-dichlorophenyl)propan-1-one thiosemicarbazone
3.4.22.51 0.00003
-
 IC50: 30 nM Trypanosoma cruzi (1E,2E)-1-(3,4-dichlorophenyl)-3-phenylprop-2-en-1-one thiosemicarbazone
3.4.22.51 0.00003
-
 IC50: 30 nM Trypanosoma cruzi (E)-(3,4-dichlorophenyl)(2-phenylcyclopropyl)methanone thiosemicarbazone
3.4.22.51 0.00003
-
 IC50: 30 nM Trypanosoma cruzi (1Z)-1-(3,4-dichlorophenyl)-2-phenoxyethan-1-one thiosemicarbazone
3.4.22.51 0.00004
-
 IC50: 40 nM Trypanosoma cruzi (E)-(3,4-dichlorophenyl)(4-methylphenyl)methanone thiosemicarbazone
3.4.22.51 0.00004
-
 IC50: 40 nM Trypanosoma cruzi (1E)-1-(3,4-dichlorophenyl)-3-phenylpropan-1-one thiosemicarbazone
3.4.22.51 0.00008
-
 IC50: 80 nM Trypanosoma cruzi (1E)-1-(3,4-dichlorophenyl)-2-phenylethan-1-one thiosemicarbazone
3.4.22.51 0.00031
-
 IC50: 310 nM Trypanosoma cruzi (1E)-1-(3-bromophenyl)propan-1-one thiosemicarbazone
3.4.22.51 0.003
-
 IC50: 3000 nM Trypanosoma cruzi (E)-cyclohexyl(3,4-dichlorophenyl)methanone thiosemicarbazone