Target Validation Information
Target ID T49898
Target Name Cell division control protein 2 homolog
Target Type
Clinical Trial
Drug Potency against Target P276-00 Drug Info IC50 = 20 nM [1]
3,4-bis(indol-3-yl)maleimide derivative Drug Info IC50 = 4500 nM [2]
KENPAULLONE Drug Info IC50 = 400 nM [3]
PF-228 Drug Info IC50 = 486 nM [4]
AG-024322 Drug Info IC50 = 1~3 nM [5]
(2,6-Diamino-pyridin-3-yl)-phenyl-methanone Drug Info IC50 = 1100 nM [6]
CGP-60474 Drug Info IC50 = 17 nM [7]
AZAKENPAULLONE Drug Info IC50 = 2000 nM [8]
PHA-767491 Drug Info IC50 = 170 nM [9]
SCH 727965 Drug Info Ki = 3 nM [10]
Thieno analogue of kenpaullone Drug Info IC50 = 600 nM [8]
ZK 304709 Drug Info Ki = 50 nM [11]
JNJ-7706621 Drug Info IC50 = 6 nM [12]
R-roscovitine Drug Info IC50 = 330 nM [5]
2-(p-toluidino)-4-phenylpyrimidine-5-carbonitrile Drug Info IC50 = 3500 nM [13]
Flavopiridol Drug Info IC50 = 30~400 nM [5]
RO-316233 Drug Info IC50 = 18000 nM [2]
R547 Drug Info IC50 = 1~3 nM [5]
GF-109203 Drug Info IC50 = 19000 nM [2]
Action against Disease Model AG-024322 Arrested multiple stages of the cell cycle and induced apoptosis in various h uMan t uMour cell lines (IC50 = 30-200 nM). Displayed dose-dependent antit uMour activity in mice bearing h uMan t uMour xenografts. [5] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Deficiency in CDK1 results in embryonic lethality in the first cell divisions [1]
References
REF 1End of the line for cannabinoid receptor 1 as an anti-obesity target? An opinion. Nat Rev Drug Discov. 2009 Jul;8(7):594. doi: 10.1038/nrd2775-c1.
REF 2Bioorg Med Chem Lett. 1998 May 5;8(9):1019-22.Design of new inhibitors for cdc2 kinase based on a multiple pseudosubstrate structure.
REF 3Eur J Med Chem. 2010 Sep;45(9):4316-30. Epub 2010 Jun 30.Discovery of novel CDK1 inhibitors by combining pharmacophore modeling, QSAR analysis and in silico screening followed by in vitro bioassay.
REF 4J Biol Chem. 2007 May 18;282(20):14845-52. Epub 2007 Mar 28.Cellular characterization of a novel focal adhesion kinase inhibitor.
REF 5Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
REF 6Bioorg Med Chem Lett. 2005 May 2;15(9):2221-4.3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.
REF 7J Med Chem. 2005 Mar 24;48(6):1886-900.Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors.
REF 8Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6.1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.
REF 9J Med Chem. 2007 May 31;50(11):2647-54. Epub 2007 May 5.Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).
REF 10Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor. Mol Cancer Ther. 2010 Aug;9(8):2344-53. doi: 10.1158/1535-7163.MCT-10-0324. Epub 2010 Jul 27.
REF 11Molecular and pharmacodynamic characteristics of the novel multi-target tumor growth inhibitor ZK 304709. Biomed Pharmacother. 2006 Jul;60(6):269-72. Epub 2006 Jun 23.
REF 12Bioorg Med Chem Lett. 2006 Jul 15;16(14):3639-41. Epub 2006 May 6.Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621.
REF 13Bioorg Med Chem Lett. 2007 Jun 15;17(12):3266-70. Epub 2007 Apr 10.4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation.

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