Target Validation Information
TTD ID T86385
Target Name Cathepsin G (CTSG)
Type of Target
Clinical trial
Drug Potency against Target Aloxistatin Drug Info IC50 = 1100 nM [2]
Delanzomib Drug Info IC50 = 2110 nM [3]
JNJ-10311795 Drug Info Ki = 38 nM [1]
Action against Disease Model Dermolastin Drug Info N-glycosylation and biological activity of recombinant h uMan alpha1-antitrypsin expressed in a novel h uMan neuronal cell line. [4]
References
REF 1 Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase. J Med Chem. 2007 Apr 19;50(8):1727-30.
REF 2 Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing. J Biol Chem. 2007 Jul 20;282(29):20836-46.
REF 3 Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer. J Med Chem. 2008 Feb 28;51(4):1068-72.
REF 4 N-glycosylation and biological activity of recombinant human alpha1-antitrypsin expressed in a novel human neuronal cell line. Biotechnol Bioeng. 2011 Sep;108(9):2118-28.

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