Target Validation Information
Target ID T22839
Target Name Elastase 1
Target Type
Successful
Drug Potency against Target Acetyl-Pro-Ala-Pro-Ala-trifluoro methane Drug Info Ki = 240 nM [532036]
MOLASSAMIDE Drug Info IC50 = 32 nM [530586]
Acetyl-Ala-Ala-Pro-Ala-trifluromethane Drug Info Ki = 150 nM [532036]
GRASSYSTATIN A Drug Info IC50 = 10000 nM [530345]
References
Ref 532036J Med Chem. 1990 Jan;33(1):394-407.Synthesis of peptidyl fluoromethyl ketones and peptidyl alpha-keto esters as inhibitors of porcine pancreatic elastase, human neutrophil elastase, and rat and humanneutrophil cathepsin G.
Ref 530586J Nat Prod. 2010 Mar 26;73(3):459-62.Molassamide, a depsipeptide serine protease inhibitor from the marine cyanobacterium Dichothrix utahensis.
Ref 532036J Med Chem. 1990 Jan;33(1):394-407.Synthesis of peptidyl fluoromethyl ketones and peptidyl alpha-keto esters as inhibitors of porcine pancreatic elastase, human neutrophil elastase, and rat and humanneutrophil cathepsin G.
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.

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