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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