Target Validation Information
TTD ID T67102
Target Name Cathepsin D (CTSD)
Type of Target
Clinical trial
Drug Potency against Target CI-992 Drug Info IC50 = 1250 nM [1]
Grassystatin a Drug Info IC50 = 1000 nM [4]
GRL-7234 Drug Info Ki = 41 nM [2]
KNI-10006 Drug Info Ki = 2 nM [3]
References
REF 1 Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors. J Med Chem. 1992 Jul 10;35(14):2562-72.
REF 2 Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands. J Med Chem. 2007 May 17;50(10):2399-407.
REF 3 alpha-Substituted norstatines as the transition-state mimic in inhibitors of multiple digestive vacuole malaria aspartic proteases. Bioorg Med Chem. 2009 Aug 15;17(16):5933-49.
REF 4 Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. J Med Chem. 2009 Sep 24;52(18):5732-47.

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