Target Validation Information
TTD ID	T35940
Target Name	ERK activator kinase 1 (MEK1)
Type of Target	Clinical trial
Drug Potency against Target	4,5-Dibromo-1H-pyrrole-2-carboxylic acid amide	Drug Info	IC50 = 2500 nM	[1]
	5-phenylamino-4-cyano-3-hydroxy-isothiazole	Drug Info	IC50 = 7000 nM	[2]
	ALDISIN	Drug Info	IC50 = 2500 nM	[1]
	DEBROMOHYMENIALDISINE	Drug Info	IC50 = 2500 nM	[1]
	OROIDIN	Drug Info	IC50 = 2500 nM	[1]
	REVERSINE	Drug Info	IC50 = 8 nM	[3]
References
REF 1	Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1). J Med Chem. 2002 Jan 17;45(2):529-32.
REF 2	Discovery of 3-hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles as potent MEK1 inhibitors. Bioorg Med Chem Lett. 2006 Aug 1;16(15):3975-80.
REF 3	Reversine increases the plasticity of lineage-committed mammalian cells. Proc Natl Acad Sci U S A. 2007 Jun 19;104(25):10482-7.

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