Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T50547 | ||||
Target Name | Plasmodium Plasmepsin 1 (Malaria PLA1) | ||||
Type of Target |
Literature-reported |
||||
Drug Potency against Target | KNI-10006 | Drug Info | IC50 = 280 nM | [4] | |
L-mannitol derivative | Drug Info | Ki = 478 nM | [2] | ||
PS-777621 | Drug Info | Ki = 727 nM | [3] | ||
SC-5003 | Drug Info | IC50 = 500 nM | [1] | ||
References | |||||
REF 1 | Protease inhibitors: current status and future prospects. J Med Chem. 2000 Feb 10;43(3):305-41. | ||||
REF 2 | Synthesis of malarial plasmepsin inhibitors and prediction of binding modes by molecular dynamics simulations. J Med Chem. 2005 Sep 22;48(19):6090-106. | ||||
REF 3 | High antiplasmodial activity of novel plasmepsins I and II inhibitors. J Med Chem. 2006 Dec 14;49(25):7440-9. | ||||
REF 4 | alpha-Substituted norstatines as the transition-state mimic in inhibitors of multiple digestive vacuole malaria aspartic proteases. Bioorg Med Chem. 2009 Aug 15;17(16):5933-49. | ||||
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