Target Validation Information
TTD ID	T57700
Target Name	Tyrosine-protein kinase Kit (KIT)
Type of Target	Successful
Drug Potency against Target	Imatinib	Drug Info	Ki = 100 nM
	Sunitinib	Drug Info	Ki = 1~10 nM	[9]
	Motesanib	Drug Info	Ki = 8 nM	[7]
	Nilotinib	Drug Info	Ki = 27 nM	[6]
	OSI-930	Drug Info	IC50 = 8 nM	[8]
	4-(4-aminophenyl)-1H-indazol-3yl-amine	Drug Info	IC50 = 7360 nM	[4]
	5,11-Dimethyl-6H-pyrido[4,3-b]carbazol-9-ol	Drug Info	IC50 = 10 nM	[2]
	9-Bromo-5,11-dimethyl-6H-pyrido[4,3-b]carbazole	Drug Info	IC50 = 200 nM	[2]
	9-Methoxy-5,11-dimethyl-6H-pyrido[4,3-b]carbazole	Drug Info	IC50 = 300 nM	[2]
	Bis-(5-hydroxy-1H-indol-2-yl)-methanone	Drug Info	IC50 = 500 nM	[3]
	PD-0166326	Drug Info	IC50 = 636 nM	[5]
	PD-0173956	Drug Info	IC50 = 290 nM	[5]
	Romiplostim	Drug Info	IC50 = 400 nM	[1]
References
REF 1	New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven a... J Med Chem. 2000 Jun 15;43(12):2310-23.
REF 2	Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases. J Med Chem. 2005 Oct 6;48(20):6194-201.
REF 3	Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase. J Med Chem. 2006 Jun 1;49(11):3101-15.
REF 4	Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted ... J Med Chem. 2007 Apr 5;50(7):1584-97.
REF 5	Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6872-6.
REF 6	Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell. 2005 Feb;7(2):129-41.
REF 7	AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts. Cancer Res. 2006 Sep 1;66(17):8715-21.
REF 8	Molecular design and clinical development of VEGFR kinase inhibitors. Curr Top Med Chem. 2007;7(14):1379-93.
REF 9	BCL-2 family antagonists for cancer therapy. Nat Rev Drug Discov. 2008 Dec;7(12):989-1000.

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