Target Validation Information
TTD ID	T77764
Target Name	Aurora B messenger RNA (AURKB mRNA)
Type of Target	Clinical trial
Drug Potency against Target	4-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine	Drug Info	IC50 = 782 nM	[7]
	6-bromoindirubin-3-oxime	Drug Info	IC50 = 900 nM	[3]
	7-bromoindirubin-3-oxime	Drug Info	IC50 = 4600 nM	[3]
	7-chloroindirubin-3-oxime	Drug Info	IC50 = 8000 nM	[3]
	7-fluoroindirubin-3-acetoxime	Drug Info	IC50 = 8000 nM	[3]
	7-fluoroindirubin-3-oxime	Drug Info	IC50 = 7000 nM	[3]
	7-iodoindirubin-3-oxime	Drug Info	IC50 = 10000 nM	[3]
	AZD-1152-HQPA	Drug Info	IC50 = 17 nM	[6]
	CGP-57380	Drug Info	IC50 = 2500 nM	[4]
	HESPERADIN	Drug Info	IC50 = 250 nM	[2]
	Indirubin-3'-monoxime	Drug Info	IC50 = 2300 nM	[3]
	Indirubin-3-acetoxime	Drug Info	IC50 = 2100 nM	[3]
	Indirubin-3-methoxime	Drug Info	IC50 = 3000 nM	[3]
	PHA-739358	Drug Info	IC50 = 135 nM	[1]
	quinazoline deriv. 1	Drug Info	IC50 = 1250 nM	[5]
	SU 6656	Drug Info	IC50 = 19 nM	[4]
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 of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors. J Med Chem. 2006 Feb 9;49(3):955-70.
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	A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8.
REF 6	Discovery and development of aurora kinase inhibitors as anticancer agents. J Med Chem. 2009 May 14;52(9):2629-51.
REF 7	Discovery of a new series of Aurora inhibitors through truncation of GSK1070916. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2552-5.

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