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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