Target Validation Information
TTD ID	T44458
Target Name	Cyclin-dependent kinase 9 (CDK9)
Type of Target	Clinical trial
Drug Potency against Target	AT7519	Drug Info	IC50 < 10 nM	[3]
	Flavopiridol	Drug Info	IC50 = 3 nM	[3]
	P276-00	Drug Info	IC50 = 20 nM	[3]
	R-roscovitine	Drug Info	IC50 = 230 nM	[3]
	SCH 727965	Drug Info	Ki = 4 nM	[5]
	SNS-032	Drug Info	IC50 = 1 nM	[4]
	ZK 304709	Drug Info	IC50 = 4 nM	[4]
	3-((3,5-diamino-1H-pyrazol-4-yl)diazenyl)phenol	Drug Info	IC50 = 1500 nM	[1]
	4-(phenyldiazenyl)-1H-pyrazole-3,5-diamine	Drug Info	IC50 = 15000 nM	[1]
	4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol	Drug Info	IC50 = 350 nM	[1]
	MERIOLIN 1	Drug Info	IC50 = 26 nM	[2]
	MERIOLIN 2	Drug Info	IC50 = 18 nM	[2]
	MERIOLIN 3	Drug Info	IC50 = 6 nM	[2]
	MERIOLIN 4	Drug Info	IC50 = 7 nM	[2]
	MERIOLIN 5	Drug Info	IC50 = 5.6 nM	[2]
	MERIOLIN 6	Drug Info	IC50 = 5.6 nM	[2]
	MERIOLIN 7	Drug Info	IC50 = 5300 nM	[2]
	MERIOLIN 8	Drug Info	IC50 = 1200 nM	[2]
Action against Disease Model	SCH 727965	Drug Info	Induced apoptosis in t uMour cell lines and growth inhibition or regression in xenograft models.	[3]
References
REF 1	4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006 Nov 2;49(22):6500-9.
REF 2	Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin com... J Med Chem. 2008 Feb 28;51(4):737-51.
REF 3	Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
REF 4	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 5	Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor. Mol Cancer Ther. 2010 Aug;9(8):2344-53.

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