Target Validation Information
Target ID T30372
Target Name Cruzipain
Target Type
Successful
Drug Potency against Target K-777 Drug Info IC50 = 4 nM [530398]
5-Chloro-1-(4-chloro-benzyl)-1H-indole-2,3-dione Drug Info IC50 = 6000 nM [526832]
VITAMIN K2 Drug Info IC50 = 18000 nM [530877]
1-(3-Methoxy-benzyl)-5-methyl-1H-indole-2,3-dione Drug Info IC50 = 2000 nM [526832]
MANIDIPINE Drug Info IC50 = 6000 nM [530877]
TRICLABENDAZOLE Drug Info IC50 = 15000 nM [530877]
(3Z)-1H-indole-2,3-dione 3-thiosemicarbazone Drug Info IC50 = 8000 nM [526832]
GNF-PF-4478 Drug Info Ki = 2000 nM [530968]
3'-bromopropiophenonethiosemicarbazone Drug Info IC50 = 40 nM [531227]
2-methoxy-1-naphthaldehyde thiosemicarbazone Drug Info IC50 = 560 nM [526354]
5-(4-bromophenyl)-2-furaldehyde thiosemicarbazone Drug Info IC50 = 280 nM [526354]
1-(3,4-dihydronaphthalen-1-yl)ethanone Drug Info IC50 = 1360 nM [528258]
1-(bis(3-bromophenyl)methylene)thiosemicarbazide Drug Info IC50 = 24 nM [528258]
N1,N4-bis(5-chloro-2-methylphenyl)succinamide Drug Info IC50 = 12000 nM [530512]
3-chloro-N-(4-(phenyldiazenyl)phenyl)benzamide Drug Info IC50 = 12000 nM [530512]
3-amino-5-(furan-2-yl)biphenyl-2,4-dicarbonitrile Drug Info IC50 = 12000 nM [530512]
2-(trifluoromethyl)benzaldehyde thiosemicarbazone Drug Info IC50 = 1300 nM [526354]
3-(trifluoromethyl)benzaldehyde thiosemicarbazone Drug Info IC50 = 480 nM [526354]
5-(3,4-dichlorophenyl)-1H-pyrazol-3-ol Drug Info IC50 = 12000 nM [530512]
L-755507 Drug Info IC50 = 12000 nM [530512]
3,5-dichlorobenzaldehyde thiosemicarbazone Drug Info IC50 = 560 nM [526354]
1-(1-(3-nitrophenyl)propylidene)thiosemicarbazide Drug Info IC50 = 860 nM [528258]
3,4-dichlorobenzaldehyde thiosemicarbazone Drug Info IC50 = 460 nM [526354]
3',4'-dichloroacetophenonethiosemicarbazone Drug Info IC50 = 100 nM [531227]
References
Ref 530398Bioorg Med Chem Lett. 2009 Nov 1;19(21):6218-21. Epub 2009 Sep 3.Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases.
Ref 526832Bioorg Med Chem Lett. 2003 Oct 20;13(20):3527-30.Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain.
Ref 530877J Med Chem. 2010 May 27;53(10):4259-65.Colloid formation by drugs in simulated intestinal fluid.
Ref 526832Bioorg Med Chem Lett. 2003 Oct 20;13(20):3527-30.Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain.
Ref 530877J Med Chem. 2010 May 27;53(10):4259-65.Colloid formation by drugs in simulated intestinal fluid.
Ref 530877J Med Chem. 2010 May 27;53(10):4259-65.Colloid formation by drugs in simulated intestinal fluid.
Ref 526832Bioorg Med Chem Lett. 2003 Oct 20;13(20):3527-30.Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain.
Ref 530968J Med Chem. 2010 Jul 8;53(13):4891-905.Complementarity between a docking and a high-throughput screen in discovering new cruzain inhibitors.
Ref 531227Bioorg Med Chem. 2010 Nov 15;18(22):7826-35. Epub 2010 Sep 29.Studies toward the structural optimization of novel thiazolylhydrazone-based potent antitrypanosomal agents.
Ref 526354J Med Chem. 2002 Jun 20;45(13):2695-707.Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruzain.
Ref 526354J Med Chem. 2002 Jun 20;45(13):2695-707.Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruzain.
Ref 528258Bioorg Med Chem Lett. 2006 Aug 15;16(16):4405-9. Epub 2006 Jun 15.Design, synthesis, and biochemical evaluation of novel cruzain inhibitors with potential application in the treatment of Chagas' disease.
Ref 528258Bioorg Med Chem Lett. 2006 Aug 15;16(16):4405-9. Epub 2006 Jun 15.Design, synthesis, and biochemical evaluation of novel cruzain inhibitors with potential application in the treatment of Chagas' disease.
Ref 530512J Med Chem. 2010 Jan 14;53(1):37-51.Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease.
Ref 530512J Med Chem. 2010 Jan 14;53(1):37-51.Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease.
Ref 530512J Med Chem. 2010 Jan 14;53(1):37-51.Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease.
Ref 526354J Med Chem. 2002 Jun 20;45(13):2695-707.Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruzain.
Ref 526354J Med Chem. 2002 Jun 20;45(13):2695-707.Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruzain.
Ref 530512J Med Chem. 2010 Jan 14;53(1):37-51.Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease.
Ref 530512J Med Chem. 2010 Jan 14;53(1):37-51.Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease.
Ref 526354J Med Chem. 2002 Jun 20;45(13):2695-707.Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruzain.
Ref 528258Bioorg Med Chem Lett. 2006 Aug 15;16(16):4405-9. Epub 2006 Jun 15.Design, synthesis, and biochemical evaluation of novel cruzain inhibitors with potential application in the treatment of Chagas' disease.
Ref 526354J Med Chem. 2002 Jun 20;45(13):2695-707.Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruzain.
Ref 531227Bioorg Med Chem. 2010 Nov 15;18(22):7826-35. Epub 2010 Sep 29.Studies toward the structural optimization of novel thiazolylhydrazone-based potent antitrypanosomal agents.

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