Target Validation Information
TTD ID	TTDS00348
Target Name	Proto-oncogene tyrosine-protein kinase receptor ret
Type of Target	Successful target
Drug Potency against Target	Sorafenib		IC50 = 20 nM	[1]
	Sorafenib		IC50 = 22 nM	[2]
	Sorafenib		IC50 = 28 nM	[3]
	Sorafenib		IC50 = 6 nM	[4]
	Sorafenib		IC50 = 6 nM	[5]
	Sorafenib		Ki = 15 nM	[6]
	Sorafenib		Ki = 5.9 nM	[7]
	Vandetanib		IC50 = 100 nM	[2]
	SU-5614		IC50 = 1000 nM	[8]
	SU-4984		IC50 = 1100 nM	[8]
	SU-11248		IC50 = 1300 nM	[8]
	SU-9516		IC50 = 1600 nM	[8]
	SEMAXINIB		IC50 = 170 nM	[8]
	(E)-3-(4-hydroxybenzylidene)indolin-2-one		IC50 = 2300 nM	[8]
	(Z)-3-((1H-pyrrol-2-yl)methylene)indolin-2-one		IC50 = 460 nM	[8]
	(Z)-5-Amino-3-(4-methoxybenzylidene)indolin-2-one		IC50 = 5300 nM	[8]
	SU-6656		IC50 = 770 nM	[8]
	TG-100435		Ki = 407 nM	[9]
Ref 1	Nat Biotechnol. 2005 Mar;23(3):329-36. Epub 2005 Feb 13.A small molecule-kinase interaction map for clinical kinase inhibitors. To Reference
Ref 2	Nat Biotechnol. 2008 Jan;26(1):127-32.A quantitative analysis of kinase inhibitor selectivity. To Reference
Ref 3	Expert Opin Investig Drugs. 2008 Jul;17(7):1013-28.Therapeutic potential of novel selective-spectrum kinase inhibitors in oncology. To Reference
Ref 4	Curr Top Med Chem. 2006;6(11):1071-89.Recent advances in the research and development of RAF kinase inhibitors. To Reference
Ref 5	Curr Top Med Chem. 2007;7(14):1364-78.Recent advances of MEK inhibitors and their clinical progress. To Reference
Ref 6	Curr Opin Pharmacol. 2008 Aug;8(4):419-26. Epub 2008 Aug 3.Therapeutic strategies for inhibiting oncogenic BRAF signaling. To Reference
Ref 7	J Biol Chem. 2007 Oct 5;282(40):29230-40. Epub 2007 Jul 30.Sorafenib functions to potently suppress RET tyrosine kinase activity by direct enzymatic inhibition and promoting RET lysosomal degradation independent of proteasomal targeting. To Reference
Ref 8	Bioorg Med Chem. 2010 Feb 15;18(4):1482-96. Epub 2010 Jan 11.Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. To Reference
Ref 9	Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. Epub 2006 Nov 7.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 kinase inhibitor with anti-tumor activity in preclinical assays. To Reference

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Dr. Chen Yuzong
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Professor in Department of Pharmacy
National University of Singapore, Singapore

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