Target Validation Information
Target ID T58470
Target Name Cyclin-A2
Target Type
Discontinued
Drug Potency against Target GW-8510 Drug Info IC50 = 10 nM [526991]
NU-2058 Drug Info IC50 = 17000 nM [527129]
6-(Cyclohex-3-enylmethoxy)-9H-purin-2-ylamine Drug Info IC50 = 13000 nM [526389]
MERIOLIN 8 Drug Info IC50 = 1200 nM [529275]
4-(7-Butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)-phenol Drug Info IC50 = 120 nM [526504]
PD-0183812 Drug Info IC50 = 209 nM [525924]
2,5-dichloro-N-p-tolylthiophene-3-sulfonamide Drug Info IC50 = 800 nM
NU-6027 Drug Info IC50 = 2200 nM [526489]
MERIOLIN 7 Drug Info IC50 = 5300 nM [529275]
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol Drug Info IC50 = 350 nM [528490]
4-(phenyldiazenyl)-1H-pyrazole-3,5-diamine Drug Info IC50 = 15000 nM [528490]
PURVALANOLA Drug Info IC50 = 30 nM [529039]
RESCOVITINE Drug Info IC50 = 500 nM [530612]
MERIOLIN 5 Drug Info IC50 = 5.6 nM [529275]
MERIOLIN 4 Drug Info IC50 = 7 nM [529275]
MERIOLIN 2 Drug Info IC50 = 18 nM [529275]
MERIOLIN 3 Drug Info IC50 = 6 nM [529275]
MERIOLIN 1 Drug Info IC50 = 26 nM [529275]
3-((3,5-diamino-1H-pyrazol-4-yl)diazenyl)phenol Drug Info IC50 = 1500 nM [528490]
MERIOLIN 6 Drug Info IC50 = 5.6 nM [529275]
References
Ref 526991Bioorg Med Chem Lett. 2004 Feb 23;14(4):953-7.Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles.
Ref 527129J Med Chem. 2004 Jul 15;47(15):3710-22.N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2.
Ref 526389J Med Chem. 2002 Aug 1;45(16):3381-93.Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives.
Ref 529275J Med Chem. 2008 Feb 28;51(4):737-51. Epub 2008 Jan 31.Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolincomplex.
Ref 526504J Med Chem. 2003 Jan 16;46(2):222-36.Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects.
Ref 525924J Med Chem. 2000 Nov 30;43(24):4606-16.Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases.
Ref 526489Bioorg Med Chem Lett. 2003 Jan 20;13(2):217-22.4-Alkoxy-2,6-diaminopyrimidine derivatives: inhibitors of cyclin dependent kinases 1 and 2.
Ref 529275J Med Chem. 2008 Feb 28;51(4):737-51. Epub 2008 Jan 31.Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolincomplex.
Ref 528490J Med Chem. 2006 Nov 2;49(22):6500-9.4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
Ref 528490J Med Chem. 2006 Nov 2;49(22):6500-9.4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
Ref 529039Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update.
Ref 530612Eur J Med Chem. 2010 Mar;45(3):1158-66. Epub 2009 Dec 21.Design, synthesis, and biological evaluation of novel pyrimidine derivatives as CDK2 inhibitors.
Ref 529275J Med Chem. 2008 Feb 28;51(4):737-51. Epub 2008 Jan 31.Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolincomplex.
Ref 529275J Med Chem. 2008 Feb 28;51(4):737-51. Epub 2008 Jan 31.Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolincomplex.
Ref 529275J Med Chem. 2008 Feb 28;51(4):737-51. Epub 2008 Jan 31.Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolincomplex.
Ref 529275J Med Chem. 2008 Feb 28;51(4):737-51. Epub 2008 Jan 31.Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolincomplex.
Ref 529275J Med Chem. 2008 Feb 28;51(4):737-51. Epub 2008 Jan 31.Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolincomplex.
Ref 528490J Med Chem. 2006 Nov 2;49(22):6500-9.4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
Ref 529275J Med Chem. 2008 Feb 28;51(4):737-51. Epub 2008 Jan 31.Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolincomplex.

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