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.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.