Target Validation Information
TTD ID	T30372
Target Name	Trypanosoma Cruzipain (Trypano CYSP)
Type of Target	Successful
Drug Potency against Target	(3Z)-1H-indole-2,3-dione 3-thiosemicarbazone	Drug Info	IC50 = 8000 nM	[2]
	1-(1-(3-nitrophenyl)propylidene)thiosemicarbazide	Drug Info	IC50 = 860 nM	[3]
	1-(3,4-dihydronaphthalen-1-yl)ethanone	Drug Info	IC50 = 1360 nM	[3]
	1-(3-Methoxy-benzyl)-5-methyl-1H-indole-2,3-dione	Drug Info	IC50 = 2000 nM	[2]
	1-(bis(3-bromophenyl)methylene)thiosemicarbazide	Drug Info	IC50 = 24 nM	[3]
	2-(trifluoromethyl)benzaldehyde thiosemicarbazone	Drug Info	IC50 = 1300 nM	[1]
	2-methoxy-1-naphthaldehyde thiosemicarbazone	Drug Info	IC50 = 560 nM	[1]
	3',4'-dichloroacetophenonethiosemicarbazone	Drug Info	IC50 = 100 nM	[8]
	3'-bromopropiophenonethiosemicarbazone	Drug Info	IC50 = 40 nM	[8]
	3,4-dichlorobenzaldehyde thiosemicarbazone	Drug Info	IC50 = 460 nM	[1]
	3,5-dichlorobenzaldehyde thiosemicarbazone	Drug Info	IC50 = 560 nM	[1]
	3-(trifluoromethyl)benzaldehyde thiosemicarbazone	Drug Info	IC50 = 480 nM	[1]
	3-amino-5-(furan-2-yl)biphenyl-2,4-dicarbonitrile	Drug Info	IC50 = 12000 nM	[5]
	3-chloro-N-(4-(phenyldiazenyl)phenyl)benzamide	Drug Info	IC50 = 12000 nM	[5]
	5-(3,4-dichlorophenyl)-1H-pyrazol-3-ol	Drug Info	IC50 = 12000 nM	[5]
	5-(4-bromophenyl)-2-furaldehyde thiosemicarbazone	Drug Info	IC50 = 280 nM	[1]
	5-Chloro-1-(4-chloro-benzyl)-1H-indole-2,3-dione	Drug Info	IC50 = 6000 nM	[2]
	GNF-PF-4478	Drug Info	Ki = 2000 nM	[7]
	K-777	Drug Info	IC50 = 4 nM	[4]
	L-755507	Drug Info	IC50 = 12000 nM	[5]
	MANIDIPINE	Drug Info	IC50 = 6000 nM	[6]
	N1,N4-bis(5-chloro-2-methylphenyl)succinamide	Drug Info	IC50 = 12000 nM	[5]
	TRICLABENDAZOLE	Drug Info	IC50 = 15000 nM	[6]
	VITAMIN K2	Drug Info	IC50 = 18000 nM	[6]
References
REF 1	Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruz... J Med Chem. 2002 Jun 20;45(13):2695-707.
REF 2	Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain. Bioorg Med Chem Lett. 2003 Oct 20;13(20):3527-30.
REF 3	Design, synthesis, and biochemical evaluation of novel cruzain inhibitors with potential application in the treatment of Chagas' disease. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4405-9.
REF 4	Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6218-21.
REF 5	Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease. J Med Chem. 2010 Jan 14;53(1):37-51.
REF 6	Colloid formation by drugs in simulated intestinal fluid. J Med Chem. 2010 May 27;53(10):4259-65.
REF 7	Complementarity between a docking and a high-throughput screen in discovering new cruzain inhibitors. J Med Chem. 2010 Jul 8;53(13):4891-905.
REF 8	Studies toward the structural optimization of novel thiazolylhydrazone-based potent antitrypanosomal agents. Bioorg Med Chem. 2010 Nov 15;18(22):7826-35.

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