Target Validation Information
TTD ID	T10052
Target Name	G1/S-specific cyclin-E1 (CCNE1)
Type of Target	Literature-reported
Drug Potency against Target	(2'Z,3'E)-5-Fluoro-5'-methoxy-indirubin-3'-oxime	Drug Info	IC50 = 4120 nM	[4]
	(2'Z,3'E)-5-Nitro-5'-methoxy-indirubin-3'-oxime	Drug Info	IC50 = 2950 nM	[4]
	2-((3,5-diamino-1H-pyrazol-4-yl)diazenyl)phenol	Drug Info	IC50 = 2500 nM	[3]
	3-((3,5-diamino-1H-pyrazol-4-yl)diazenyl)phenol	Drug Info	IC50 = 6000 nM	[3]
	4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol	Drug Info	IC50 = 3500 nM	[3]
	5-nitroindirubin-3'-oxime	Drug Info	IC50 = 7.35 nM	[4]
	aloisine A	Drug Info	IC50 = 400 nM	[2]
	PD-0183812	Drug Info	IC50 = 165 nM	[1]
References
REF 1	Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. J Med Chem. 2000 Nov 30;43(24):4606-16.
REF 2	Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects. J Med Chem. 2003 Jan 16;46(2):222-36.
REF 3	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 4	5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity. J Med Chem. 2010 May 13;53(9):3696-706.

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