Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T58470 | ||||
Target Name | Cyclin-A2 | ||||
Target Type | Discontinued |
||||
Drug Potency against Target | GW-8510 | Drug Info | IC50 = 10 nM | [1] | |
NU-2058 | Drug Info | IC50 = 17000 nM | [2] | ||
6-(Cyclohex-3-enylmethoxy)-9H-purin-2-ylamine | Drug Info | IC50 = 13000 nM | [3] | ||
MERIOLIN 8 | Drug Info | IC50 = 1200 nM | [4] | ||
4-(7-Butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)-phenol | Drug Info | IC50 = 120 nM | [5] | ||
PD-0183812 | Drug Info | IC50 = 209 nM | [6] | ||
2,5-dichloro-N-p-tolylthiophene-3-sulfonamide | Drug Info | IC50 = 800 nM | |||
NU-6027 | Drug Info | IC50 = 2200 nM | [7] | ||
MERIOLIN 7 | Drug Info | IC50 = 5300 nM | [4] | ||
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol | Drug Info | IC50 = 350 nM | [8] | ||
4-(phenyldiazenyl)-1H-pyrazole-3,5-diamine | Drug Info | IC50 = 15000 nM | [8] | ||
PURVALANOLA | Drug Info | IC50 = 30 nM | [9] | ||
RESCOVITINE | Drug Info | IC50 = 500 nM | [10] | ||
MERIOLIN 5 | Drug Info | IC50 = 5.6 nM | [4] | ||
MERIOLIN 4 | Drug Info | IC50 = 7 nM | [4] | ||
MERIOLIN 2 | Drug Info | IC50 = 18 nM | [4] | ||
MERIOLIN 3 | Drug Info | IC50 = 6 nM | [4] | ||
MERIOLIN 1 | Drug Info | IC50 = 26 nM | [4] | ||
3-((3,5-diamino-1H-pyrazol-4-yl)diazenyl)phenol | Drug Info | IC50 = 1500 nM | [8] | ||
MERIOLIN 6 | Drug Info | IC50 = 5.6 nM | [4] | ||
References | |||||
REF 1 | Bioorg 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 2 | J Med Chem. 2004 Jul 15;47(15):3710-22.N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2. | ||||
REF 3 | J 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 4 | J 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 5 | J 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 6 | J Med Chem. 2000 Nov 30;43(24):4606-16.Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. | ||||
REF 7 | Bioorg 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 8 | J 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 9 | Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update. | ||||
REF 10 | Eur 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. | ||||
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