Target Validation Information
TTD ID	T49898
Target Name	Cyclin-dependent kinase 1 (CDK1)
Type of Target	Clinical trial
Drug Potency against Target	Flavopiridol	Drug Info	IC50 = 30~400 nM	[10]
	P276-00	Drug Info	IC50 = 20 nM	[12]
	R-roscovitine	Drug Info	IC50 = 330 nM	[10]
	R547	Drug Info	IC50 = 1~3 nM	[10]
	SCH 727965	Drug Info	Ki = 3 nM	[13]
	ZK 304709	Drug Info	Ki = 50 nM	[11]
	AG-024322	Drug Info	IC50 = 1~3 nM	[10]
	(2,6-Diamino-pyridin-3-yl)-phenyl-methanone	Drug Info	IC50 = 1100 nM	[3]
	2-(p-toluidino)-4-phenylpyrimidine-5-carbonitrile	Drug Info	IC50 = 3500 nM	[7]
	3,4-bis(indol-3-yl)maleimide derivative	Drug Info	IC50 = 4500 nM	[9]
	AZAKENPAULLONE	Drug Info	IC50 = 2000 nM	[1]
	Bisindolylmaleimide-I	Drug Info	IC50 = 19000 nM	[9]
	CGP-60474	Drug Info	IC50 = 17 nM	[2]
	JNJ-7706621	Drug Info	IC50 = 6 nM	[4]
	KENPAULLONE	Drug Info	IC50 = 400 nM	[8]
	PF-228	Drug Info	IC50 = 486 nM	[5]
	PHA-767491	Drug Info	IC50 = 170 nM	[6]
	RO-316233	Drug Info	IC50 = 18000 nM	[9]
	Thieno analogue of kenpaullone	Drug Info	IC50 = 600 nM	[1]
Action against Disease Model	AG-024322	Drug Info	Arrested multiple stages of the cell cycle and induced apoptosis in various h uMan t uMour cell lines (IC50 = 30-200 nM). Displayed dose-dependent antit uMour activity in mice bearing h uMan t uMour xenografts.	[10]
References
REF 1	1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6.
REF 2	Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors. J Med Chem. 2005 Mar 24;48(6):1886-900.
REF 3	3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation. Bioorg Med Chem Lett. 2005 May 2;15(9):2221-4.
REF 4	Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3639-41.
REF 5	Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem. 2007 May 18;282(20):14845-52.
REF 6	Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J Med Chem. 2007 May 31;50(11):2647-54.
REF 7	4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3266-70.
REF 8	Discovery of novel CDK1 inhibitors by combining pharmacophore modeling, QSAR analysis and in silico screening followed by in vitro bioassay. Eur J Med Chem. 2010 Sep;45(9):4316-30.
REF 9	Design of new inhibitors for cdc2 kinase based on a multiple pseudosubstrate structure. Bioorg Med Chem Lett. 1998 May 5;8(9):1019-22.
REF 10	Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
REF 11	Molecular and pharmacodynamic characteristics of the novel multi-target tumor growth inhibitor ZK 304709. Biomed Pharmacother. 2006 Jul;60(6):269-72.
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.
REF 13	Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor. Mol Cancer Ther. 2010 Aug;9(8):2344-53.

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