Target Validation Information
TTD ID	T46781
Target Name	Aurora kinase B (AURKB)
Type of Target	Clinical trial
Drug Potency against Target	AT9283	Drug Info	IC50 = 3 nM	[2]
	AZD-1152-HQPA	Drug Info	IC50 = 3.7 nM	[2]
	CYC116	Drug Info	IC50 = 19 nM	[2]
	GSK1070916	Drug Info	IC50 = 0.38 nM	[2]
	MK-5108	Drug Info	IC50 = 14 nM	[5]
	PF-03814735	Drug Info	Ki = 0.8 nM	[6]
	PHA-739358	Drug Info	IC50 = 79 nM	[2]
	R763	Drug Info	IC50 = 4.8 nM	[3]
	Rosiglitazone + metformin	Drug Info	IC50 = 8 nM	[4]
	SNS-314	Drug Info	IC50 = 31 nM	[2]
	VX-680	Drug Info	Ki = 18 nM	[1]
Action against Disease Model	PHA-739358	Drug Info	PHA-739358 inhibits Aurora kinases in a biochemical assay with IC50 79 nmol/L for Aurora A, B, and C, respectively.	[2]
References
REF 1	VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nat Med. 2004 Mar;10(3):262-7.
REF 2	Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
REF 3	Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypic screen. J Cancer Res Clin Oncol. 2010 Jan;136(1):99-113.
REF 4	Molecular design and clinical development of VEGFR kinase inhibitors. Curr Top Med Chem. 2007;7(14):1379-93.
REF 5	MK-5108, a highly selective Aurora-A kinase inhibitor, shows antitumor activity alone and in combination with docetaxel. Mol Cancer Ther. 2010 Jan;9(1):157-66.
REF 6	PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. Mol Cancer Ther. 2010 Apr;9(4):883-94.

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