Target Validation Information
TTD ID	T87675
Target Name	Aurora kinase A (AURKA)
Type of Target	Clinical trial
Drug Potency against Target	AT9283	Drug Info	IC50 = 3 nM	[12]
	AZD-1152-HQPA	Drug Info	Ki = 0.36 nM	[10]
	CYC116	Drug Info	IC50 = 19 nM	[12]
	ENMD-2076	Drug Info	IC50 = 5 nM	[12]
	MLN8054	Drug Info	IC50 = 4 nM	[6]
	MLN8237	Drug Info	IC50 = 1 nM	[12]
	PF-03814735	Drug Info	IC50 = 5 nM	[11]
	PHA-739358	Drug Info	Ki = 13 nM	[9]
	R763	Drug Info	Ki = 4 nM	[7]
	Rosiglitazone + metformin	Drug Info	IC50 = 850 nM	[8]
	SNS-314	Drug Info	IC50 = 3.4 nM	[12]
	VX-680	Drug Info	Ki = 0.6 nM	[10]
	4-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine	Drug Info	IC50 = 584 nM	[5]
	6-bromoindirubin-3-oxime	Drug Info	IC50 = 600 nM	[4]
	7-fluoroindirubin-3-oxime	Drug Info	IC50 = 2000 nM	[4]
	AZD-1152-HQPA	Drug Info	Ki = 1400 nM	[3]
	Indirubin-3'-monoxime	Drug Info	IC50 = 4000 nM	[4]
	Indirubin-3-acetoxime	Drug Info	IC50 = 2300 nM	[4]
	Indirubin-3-methoxime	Drug Info	IC50 = 4300 nM	[4]
	PHA-739358	Drug Info	IC50 = 27 nM	[1]
	ZM-447439	Drug Info	IC50 = 110 nM	[2]
Action against Disease Model	MLN8237	Drug Info	Active against neuroblastoma xenografts in vivo (more than standard chemotherapy) and ALL xenografts. Induced cytotoxicity and cell cycle arrest in G2-M phase in multiple myeloma cellular models (at 0.25 mM).	[6]
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	Accurate prediction of the relative potencies of members of a series of kinase inhibitors using molecular docking and MM-GBSA scoring. J Med Chem. 2006 Aug 10;49(16):4805-8.
REF 3	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 4	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 5	Discovery of a new series of Aurora inhibitors through truncation of GSK1070916. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2552-5.
REF 6	Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
REF 7	Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14.
REF 8	Proteomic characterization of the angiogenesis inhibitor SU6668 reveals multiple impacts on cellular kinase signaling. Cancer Res. 2005 Aug 1;65(15):6919-26.
REF 9	PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3158-68.
REF 10	Aurora-B kinase inhibitors for cancer chemotherapy. Mini Rev Med Chem. 2008 Dec;8(14):1514-25.
REF 11	Aurora kinase inhibitors in preclinical and clinical testing. Expert Opin Investig Drugs. 2009 Apr;18(4):379-98.
REF 12	End of the line for cannabinoid receptor 1 as an anti-obesity target An opinion. Nat Rev Drug Discov. 2009 Jul;8(7):594.

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