| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T14558 | ||||
| Target Name | Tryptase | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | BMS-262084 | Drug Info | IC50 = 4 nM | [526439] | |
| APC-366 | Drug Info | IC50 = 100 nM | |||
| GRASSYSTATIN A | Drug Info | IC50 = 10000 nM | [530345] | ||
| Action against Disease Model | Pentamidine | 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 | [552612] | Drug Info | |
| References | |||||
| Ref 526439 | Bioorg Med Chem Lett. 2002 Nov 4;12(21):3229-33.Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors. | ||||
| Ref 552612 | 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. | ||||
| Ref 530345 | J 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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