Target Validation Information
Target ID T67102
Target Name Cathepsin D
Target Type
Clinical Trial
Drug Potency against Target GRL-7234 Drug Info Ki = 41 nM [528786]
GRASSYSTATIN A Drug Info IC50 = 1000 nM [530345]
CI-992 Drug Info IC50 = 1250 nM [527925]
KNI-10006 Drug Info Ki = 2 nM [530280]
References
Ref 528786J Med Chem. 2007 May 17;50(10):2399-407. Epub 2007 Apr 14.Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands.
Ref 530345J Med Chem. 2009 Sep 24;52(18):5732-47.Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
Ref 527925J Med Chem. 1992 Jul 10;35(14):2562-72.Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors.
Ref 530280Bioorg Med Chem. 2009 Aug 15;17(16):5933-49. Epub 2009 Jul 3.alpha-Substituted norstatines as the transition-state mimic in inhibitors of multiple digestive vacuole malaria aspartic proteases.

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