Target Validation Information
TTD ID	T58470
Target Name	Cyclin A2 (CCNA2)
Type of Target	Literature-reported
Drug Potency against Target	2,5-dichloro-N-p-tolylthiophene-3-sulfonamide	Drug Info	IC50 = 800 nM
	3-((3,5-diamino-1H-pyrazol-4-yl)diazenyl)phenol	Drug Info	IC50 = 1500 nM	[7]
	4-(phenyldiazenyl)-1H-pyrazole-3,5-diamine	Drug Info	IC50 = 15000 nM	[7]
	4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol	Drug Info	IC50 = 350 nM	[7]
	6-(Cyclohex-3-enylmethoxy)-9H-purin-2-ylamine	Drug Info	IC50 = 13000 nM	[2]
	6-O-Cyclohexylmethyl Guanine	Drug Info	IC50 = 17000 nM	[6]
	aloisine A	Drug Info	IC50 = 120 nM	[4]
	GW-8510	Drug Info	IC50 = 10 nM	[5]
	MERIOLIN 1	Drug Info	IC50 = 26 nM	[9]
	MERIOLIN 2	Drug Info	IC50 = 18 nM	[9]
	MERIOLIN 3	Drug Info	IC50 = 6 nM	[9]
	MERIOLIN 4	Drug Info	IC50 = 7 nM	[9]
	MERIOLIN 5	Drug Info	IC50 = 5.6 nM	[9]
	MERIOLIN 6	Drug Info	IC50 = 5.6 nM	[9]
	MERIOLIN 7	Drug Info	IC50 = 5300 nM	[9]
	MERIOLIN 8	Drug Info	IC50 = 1200 nM	[9]
	NU-6027	Drug Info	IC50 = 2200 nM	[3]
	PD-0183812	Drug Info	IC50 = 209 nM	[1]
	Purvalanol A	Drug Info	IC50 = 30 nM	[8]
	RESCOVITINE	Drug Info	IC50 = 500 nM	[10]
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	Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives. J Med Chem. 2002 Aug 1;45(16):3381-93.
REF 3	4-Alkoxy-2,6-diaminopyrimidine derivatives: inhibitors of cyclin dependent kinases 1 and 2. Bioorg Med Chem Lett. 2003 Jan 20;13(2):217-22.
REF 4	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 5	Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles. Bioorg Med Chem Lett. 2004 Feb 23;14(4):953-7.
REF 6	N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2. J Med Chem. 2004 Jul 15;47(15):3710-22.
REF 7	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 8	The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
REF 9	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 10	Design, synthesis, and biological evaluation of novel pyrimidine derivatives as CDK2 inhibitors. Eur J Med Chem. 2010 Mar;45(3):1158-66.

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