Target Validation Information
Target ID T28713
Target Name Serine/threonine-protein kinase Chk2
Target Type
Discontinued
Drug Potency against Target 5-Nitro-2-(4-phenoxy-phenyl)-1H-benzoimidazole Drug Info IC50 = 1500 nM [527477]
2-(4-Phenoxy-phenyl)-1H-benzoimidazol-5-ylamine Drug Info IC50 = 2400 nM [527477]
XL844 Drug Info IC50 = 0.2 nM [552758]
DEBROMOHYMENIALDISINE Drug Info IC50 = 183 nM [527140]
AZD7762 Drug Info IC50 < 10 nM [552758]
Action against Disease Model AZD7762 Potentiated the response to DNA-damaging agents in double-negative p53 cancer cell lines and rodent xenograft models in a dose-dependent manner. [537564] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Since the CHK2 null mice showed a remarkable radioresistance, which bear significant similarity to clinical behavior of NSCLC, down-regulation of CHK2 kinase expression by CHK2 gene silencing and methylation in non-small cell lung cancer suggest a critical role of CHK2 kinase in DNA damage induced apoptosis and a novel mechanism of the resistance of NSCLC to DNA damage basedtherapy. [527477]
References
Ref 527477J Med Chem. 2005 Mar 24;48(6):1873-85.Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles.
Ref 527477J Med Chem. 2005 Mar 24;48(6):1873-85.Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles.
Ref 552758Targeted cancer therapies based on the inhibition of DNA strand break repair. Oncogene. 2007 Dec 10;26(56):7816-24.
Ref 527140Bioorg Med Chem Lett. 2004 Aug 16;14(16):4319-21.Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine.
Ref 552758Targeted cancer therapies based on the inhibition of DNA strand break repair. Oncogene. 2007 Dec 10;26(56):7816-24.
Ref 537564Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.

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