Target Validation Information
Target ID T50547
Target Name Plasmepsin 1
Target Type
Discontinued
Drug Potency against Target L-mannitol derivative Drug Info Ki = 478 nM [527739]
PS-777621 Drug Info Ki = 727 nM [528560]
SC-5003 Drug Info IC50 = 500 nM [525693]
KNI-10006 Drug Info IC50 = 280 nM [530280]
References
Ref 527739J Med Chem. 2005 Sep 22;48(19):6090-106.Synthesis of malarial plasmepsin inhibitors and prediction of binding modes by molecular dynamics simulations.
Ref 528560J Med Chem. 2006 Dec 14;49(25):7440-9.High antiplasmodial activity of novel plasmepsins I and II inhibitors.
Ref 525693J Med Chem. 2000 Feb 10;43(3):305-41.Protease inhibitors: current status and future prospects.
Ref 530280Bioorg Med Chem. 2009 Aug 15;17(16):5933-49. Epub 2009 Jul 3.alpha-Substituted norstatines as the transition-state mimic in inhibitors of multiple digestive vacuole malaria aspartic proteases.

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