Target Validation Information
TTD ID	T04820
Target Name	Plasmodium CDK Pfmrk (Malaria Pfmrk)
Type of Target	Patented-recorded
Drug Potency against Target	(E)-1-(4-Nitro-phenyl)-3-pyridin-2-yl-propenone	Drug Info	IC50 = 18000 nM	[1]
	2,5-dichloro-N-p-tolylthiophene-3-sulfonamide	Drug Info	IC50 = 600 nM
	2,5-dichloro-N-phenylthiophene-3-sulfonamide	Drug Info	IC50 = 14900 nM
	2-chloro-N-(o-tolylcarbamoyl)benzamide	Drug Info	IC50 = 200 nM
	3-[3-(2-Hydroxy-ethoxy)-phenyl]-1H-quinolin-2-one	Drug Info	IC50 = 18000 nM	[1]
	5-chloro-4-nitrothiophene-2-sulfonamide	Drug Info	IC50 = 17400 nM
	5-Nitro-1H-indole-2,3-dione	Drug Info	IC50 = 5900 nM	[1]
	APIGENIN	Drug Info	IC50 = 7000 nM	[1]
	KENPAULLONE	Drug Info	IC50 = 15000 nM	[1]
	N'-(2-fluorobenzoyl)-2-naphthohydrazide	Drug Info	IC50 = 400 nM
	N-(2-aminoethyl)isoquinoline-5-sulfonamide	Drug Info	IC50 = 700 nM	[2]
	WR-080539	Drug Info	IC50 = 17000 nM	[3]
	WR-089120	Drug Info	IC50 = 10000 nM	[3]
	WR-190706	Drug Info	IC50 = 12000 nM	[3]
	WR-203581	Drug Info	IC50 = 18000 nM	[3]
	WR-289009	Drug Info	IC50 = 8200 nM	[3]
	WR-289010	Drug Info	IC50 = 9000 nM	[3]
	WR-289012	Drug Info	IC50 = 19000 nM	[3]
	WR-289016	Drug Info	IC50 = 1300 nM	[3]
References
REF 1	A three-dimensional in silico pharmacophore model for inhibition of Plasmodium falciparum cyclin-dependent kinases and discovery of different class... J Med Chem. 2004 Oct 21;47(22):5418-26.
REF 2	Evaluation of broad spectrum protein kinase inhibitors to probe the architecture of the malarial cyclin dependent protein kinase Pfmrk. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4961-6.
REF 3	Selective inhibition of Pfmrk, a Plasmodium falciparum CDK, by antimalarial 1,3-diaryl-2-propenones. Bioorg Med Chem Lett. 2009 Apr 1;19(7):1982-5.

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