Target Validation Information
TTD ID	T97592
Target Name	Aurora kinase C (AURKC)
Type of Target	Clinical trial
Drug Potency against Target	AZD-1152-HQPA	Drug Info	IC50 = 4.6 nM	[5]
	CYC116	Drug Info	IC50 = 69 nM	[5]
	GSK1070916	Drug Info	IC50 = 1.5 nM	[5]
	MK-5108	Drug Info	IC50 = 12 nM	[7]
	PHA-739358	Drug Info	IC50 = 61 nM	[5]
	R763	Drug Info	IC50 = 6.8 nM	[6]
	SNS-314	Drug Info	IC50 = 3.4 nM	[5]
	VX-680	Drug Info	IC50 = 4.6 nM	[5]
	6-bromoindirubin-3-oxime	Drug Info	IC50 = 200 nM	[3]
	7-bromoindirubin-3-acetoxime	Drug Info	IC50 = 4500 nM	[3]
	7-bromoindirubin-3-oxime	Drug Info	IC50 = 700 nM	[3]
	7-chloroindirubin-3-oxime	Drug Info	IC50 = 900 nM	[3]
	7-fluoroindirubin-3-acetoxime	Drug Info	IC50 = 1000 nM	[3]
	7-fluoroindirubin-3-oxime	Drug Info	IC50 = 1000 nM	[3]
	7-iodoindirubin-3-oxime	Drug Info	IC50 = 600 nM	[3]
	AZD-1152-HQPA	Drug Info	Ki = 17 nM	[2]
	Indirubin-3'-monoxime	Drug Info	IC50 = 300 nM	[3]
	Indirubin-3-acetoxime	Drug Info	IC50 = 700 nM	[3]
	Indirubin-3-methoxime	Drug Info	IC50 = 400 nM	[3]
	PHA-739358	Drug Info	IC50 = 120 nM	[1]
	SU 6656	Drug Info	IC50 = 17 nM	[4]
Action against Disease Model	AZD-1152-HQPA	Drug Info	Induced growth arrest, polyploidy and promoted apoptosis in various h uMan t uMour xenografts and AML cell lines. Sensitized t uMour cells to radiotherapy in vitro and in vivo.	[5]
References
REF 1	Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition. J Med Chem. 2005 Apr 21;48(8):3080-4.
REF 2	Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase. J Med Chem. 2007 May 3;50(9):2213-24.
REF 3	An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted in... J Med Chem. 2007 Aug 23;50(17):4027-37.
REF 4	The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
REF 5	Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
REF 6	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 7	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.

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