Target Validation Information
TTD ID	T62449
Target Name	Checkpoint kinase-1 (CHK1)
Type of Target	Clinical trial
Drug Potency against Target	AZD7762	Drug Info	IC50 = 5 nM	[11]
	PF-477736	Drug Info	Ki = 0.49 nM	[11]
	UCN-01	Drug Info	IC50 = 11 nM	[11]
	UCN-01	Drug Info	IC50 = 11 nM	[10]
	XL844	Drug Info	Ki = 2.2 nM	[8]
	3-(1H-Indol-2-yl)-1H-quinolin-2-one	Drug Info	IC50 = 1000 nM	[4]
	6-(3-aminopropyl)benzo[h]isoquinolin-1(2H)-one	Drug Info	IC50 = 98 nM	[6]
	9-chlorobenzo[h]isoquinolin-1(2H)-one	Drug Info	IC50 = 580 nM	[6]
	9-hydroxypyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione	Drug Info	IC50 = 470 nM	[3]
	A-432411	Drug Info	IC50 = 7 nM	[7]
	BIS-IMIDE A	Drug Info	IC50 = 20 nM	[5]
	DEBROMOHYMENIALDISINE	Drug Info	IC50 = 725 nM	[1]
	GRANULATIMIDE	Drug Info	IC50 = 80 nM	[5]
	Isogranulatimide	Drug Info	IC50 = 440 nM	[5]
	NU-6102	Drug Info	IC50 < 500 nM	[2]
Action against Disease Model	UCN-01	Drug Info	Abrogated DNA damage-induced G2 arrest, leading to mitotic entry and subsequent cell death.	[9]
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	Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1353-7.
REF 3	4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modific... J Med Chem. 2006 Aug 10;49(16):4896-911.
REF 4	Development of 6-substituted indolylquinolinones as potent Chek1 kinase inhibitors. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5907-12.
REF 5	Synthesis, in vitro antiproliferative activities, and Chk1 inhibitory properties of pyrrolo[3,4-a]carbazole-1,3-diones, pyrrolo[3,4-c]carbazole-1,3... Eur J Med Chem. 2008 Feb;43(2):282-92.
REF 6	Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6280-5.
REF 7	Synthesis of selenophene derivatives as novel CHK1 inhibitors. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5065-8.
REF 8	The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8.
REF 9	Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
REF 10	The radiosensitizing agent 7-hydroxystaurosporine (UCN-01) inhibits the DNA damage checkpoint kinase hChk1. Cancer Res. 2000 Apr 15;60(8):2108-12.
REF 11	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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