Target Validation Information
TTD ID	T28713
Target Name	Serine/threonine-protein kinase Chk2 (RAD53)
Type of Target	Clinical trial
Drug Potency against Target	AZD7762	Drug Info	IC50 < 10 nM	[4]
	XL844	Drug Info	IC50 = 0.2 nM	[4]
	2-(4-Phenoxy-phenyl)-1H-benzoimidazol-5-ylamine	Drug Info	IC50 = 2400 nM	[2]
	5-Nitro-2-(4-phenoxy-phenyl)-1H-benzoimidazole	Drug Info	IC50 = 1500 nM	[2]
	DEBROMOHYMENIALDISINE	Drug Info	IC50 = 183 nM	[1]
Action against Disease Model	AZD7762	Drug Info	Potentiated the response to DNA-damaging agents in double-negative p53 cancer cell lines and rodent xenograft models in a dose-dependent manner.	[3]
References
REF 1	Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4319-21.
REF 2	Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. J Med Chem. 2005 Mar 24;48(6):1873-85.
REF 3	Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
REF 4	Targeted cancer therapies based on the inhibition of DNA strand break repair. Oncogene. 2007 Dec 10;26(56):7816-24.

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