Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T28713 | ||||
Target Name | Serine/threonine-protein kinase Chk2 | ||||
Target Type | Discontinued |
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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 527477 | J Med Chem. 2005 Mar 24;48(6):1873-85.Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. | ||||
Ref 527477 | J Med Chem. 2005 Mar 24;48(6):1873-85.Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. | ||||
Ref 552758 | Targeted cancer therapies based on the inhibition of DNA strand break repair. Oncogene. 2007 Dec 10;26(56):7816-24. | ||||
Ref 527140 | Bioorg Med Chem Lett. 2004 Aug 16;14(16):4319-21.Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine. | ||||
Ref 552758 | Targeted cancer therapies based on the inhibition of DNA strand break repair. Oncogene. 2007 Dec 10;26(56):7816-24. | ||||
Ref 537564 | Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. |
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