Target Validation Information
TTD ID T14558
Target Name Tryptase alpha/beta-1 (Tryptase)
Type of Target
Successful
Drug Potency against Target APC-366 Drug Info IC50 = 100 nM
BMS-262084 Drug Info IC50 = 4 nM [1]
Grassystatin a Drug Info IC50 = 10000 nM [2]
Action against Disease Model Pentamidine Drug Info To identify potential anti-Pne uMocystis agents, we synthesized bisbenzamidine derivatives in which the parent compound pentamidine was modified by a 1,4-piperazinediyl, alkanediamide, or 1,3-phenylenediamide moiety as the central linker. Several of the compounds were more active against P. carinii and less toxic than pentamidine in cytotoxicity assays. IC50 against Pne uMocystis carinii: 300 ng/mL [3]
References
REF 1 Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3229-33.
REF 2 Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. J Med Chem. 2009 Sep 24;52(18):5732-47.
REF 3 In vitro selection and in vivo efficacy of piperazine- and alkanediamide-linked bisbenzamidines against Pneumocystis pneumonia in mice. Antimicrob Agents Chemother. 2006 Jul;50(7):2337-43.

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