Target Validation Information
TTD ID	T60631
Target Name	Proto-oncogene c-Ret (RET)
Type of Target	Successful
Drug Potency against Target	Sorafenib	Drug Info	Ki = 5.9 nM	[3]
	Vandetanib	Drug Info	IC50 = 100 nM	[4]
	(E)-3-(4-hydroxybenzylidene)indolin-2-one	Drug Info	IC50 = 2300 nM	[2]
	(Z)-3-((1H-pyrrol-2-yl)methylene)indolin-2-one	Drug Info	IC50 = 460 nM	[2]
	(Z)-5-Amino-3-(4-methoxybenzylidene)indolin-2-one	Drug Info	IC50 = 5300 nM	[2]
	Romiplostim	Drug Info	IC50 = 170 nM	[2]
	Sunitinib	Drug Info	IC50 = 1300 nM	[2]
	TG-100435	Drug Info	Ki = 407 nM	[1]
References
REF 1	Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinas... Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8.
REF 2	Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. Bioorg Med Chem. 2010 Feb 15;18(4):1482-96.
REF 3	Sorafenib functions to potently suppress RET tyrosine kinase activity by direct enzymatic inhibition and promoting RET lysosomal degradation indepe... J Biol Chem. 2007 Oct 5;282(40):29230-40.
REF 4	A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32.

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