Target Validation Information
TTD ID	T46465
Target Name	Plasmodium Plasmepsin 2 (Malaria PLA2)
Type of Target	Patented-recorded
Drug Potency against Target	KNI-10006	Drug Info	Ki = 0.5 nM	[5]
	KNI-10033	Drug Info	Ki = 3 nM	[2]
	KNI-10061	Drug Info	Ki = 15 nM	[2]
	KNI-10062	Drug Info	Ki = 9 nM	[2]
	KNI-10074	Drug Info	Ki = 39 nM	[3]
	KNI-10079	Drug Info	Ki = 145 nM	[3]
	KNI-10080	Drug Info	Ki = 42 nM	[3]
	KNI-10081	Drug Info	Ki = 55 nM	[3]
	KNI-10087	Drug Info	Ki = 29 nM	[3]
	KNI-10088	Drug Info	Ki = 28 nM	[3]
	KNI-10092	Drug Info	Ki = 153 nM	[3]
	KNI-10093	Drug Info	Ki = 4 nM	[3]
	KNI-10094	Drug Info	Ki = 479 nM	[3]
	KNI-10095	Drug Info	Ki = 55 nM	[3]
	KNI-10106	Drug Info	Ki = 126 nM	[3]
	KNI-10113	Drug Info	Ki = 132 nM	[3]
	KNI-10124	Drug Info	Ki = 9 nM	[3]
	KNI-10125	Drug Info	Ki = 10 nM	[3]
	KNI-10152	Drug Info	Ki = 23 nM	[3]
	KNI-10155	Drug Info	Ki = 5 nM	[3]
	KNI-10216	Drug Info	Ki = 10 nM	[3]
	KNI-10217	Drug Info	Ki = 10 nM	[3]
	KNI-10232	Drug Info	Ki = 0.2 nM	[2]
	KNI-10255	Drug Info	Ki = 38 nM	[3]
	KNI-10256	Drug Info	Ki = 25 nM	[3]
	KNI-10260	Drug Info	Ki = 782 nM	[3]
	KNI-10265	Drug Info	Ki = 14 nM	[3]
	KNI-10266	Drug Info	Ki = 19 nM	[3]
	KNI-10282	Drug Info	Ki = 21 nM	[3]
	KNI-10283	Drug Info	Ki = 25 nM	[3]
	KNI-10313	Drug Info	Ki = 5 nM	[2]
	KNI-10314	Drug Info	Ki = 9 nM	[2]
	KNI-10315	Drug Info	Ki = 4 nM	[2]
	KNI-10316	Drug Info	Ki = 17 nM	[2]
	KNI-10332	Drug Info	Ki = 18 nM	[2]
	KNI-10341	Drug Info	Ki = 16 nM	[2]
	KNI-10342	Drug Info	Ki = 4 nM	[2]
	KNI-10368	Drug Info	Ki = 12 nM	[2]
	KNI-10369	Drug Info	Ki = 112 nM	[3]
	KNI-10372	Drug Info	Ki = 4 nM	[2]
	KNI-10526	Drug Info	Ki = 21 nM	[3]
	KNI-10527	Drug Info	Ki = 6 nM	[3]
	KNI-10529	Drug Info	Ki = 7 nM	[3]
	KNI-10538	Drug Info	Ki = 10 nM	[5]
	KNI-10539	Drug Info	Ki = 30 nM	[3]
	KNI-10541	Drug Info	Ki = 26 nM	[3]
	KNI-10737	Drug Info	Ki = 6.5 nM	[5]
	KNI-10740	Drug Info	Ki = 1.2 nM	[5]
	KNI-10741	Drug Info	Ki = 0.68 nM	[5]
	KNI-10742	Drug Info	Ki = 0.1 nM	[5]
	KNI-10743	Drug Info	Ki = 0.1 nM	[5]
	KNI-10758	Drug Info	Ki = 4.2 nM	[5]
	KNI-10759	Drug Info	Ki = 10 nM	[5]
	KNI-10760	Drug Info	Ki = 5.1 nM	[5]
	KNI-10761	Drug Info	Ki = 17 nM	[5]
	KNI-10762	Drug Info	Ki = 8.5 nM	[5]
	KNI-10763	Drug Info	Ki = 9.1 nM	[5]
	KNI-1293	Drug Info	Ki = 23 nM	[3]
	KNI-227	Drug Info	Ki = 36 nM	[2]
	KNI-272	Drug Info	Ki = 1000 nM	[2]
	KNI-764	Drug Info	IC50 = 30 nM	[4]
	PS-154636-1	Drug Info	Ki = 590 nM	[6]
	PS-222036	Drug Info	Ki = 440 nM	[6]
	PS-444035	Drug Info	Ki = 220 nM	[6]
PS-662477	Drug Info	Ki = 220 nM	[6]
PS-725074	Drug Info	Ki = 500 nM	[6]
PS-777621	Drug Info	Ki = 58.9 nM	[1]
References
REF 1	High antiplasmodial activity of novel plasmepsins I and II inhibitors. J Med Chem. 2006 Dec 14;49(25):7440-9.
REF 2	Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52.
REF 3	Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. Bioorg Med Chem. 2008 Dec 1;16(23):10049-60.
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.
REF 5	Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4836-9.
REF 6	Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library. Bioorg Med Chem Lett. 1998 Sep 8;8(17):2315-20.

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