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Literature summary for 3.4.22.51 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

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

Organism

Organism UniProt Comment Textmining
Trypanosoma cruzi
-
-
-

Synonyms

Synonyms Comment Organism
cruzain
-
Trypanosoma cruzi

IC50 Value

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