Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00010

Target Information
NameSerine/threonine-protein kinase Chk2    
Type of targetDiscontinued target    
SynonymsCHEK2    
CHK2    
Cds1    
RAD53    
DiseaseSolid tumors
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[1]
Drug(s)XL844Suspended in Phase IAdvanced solid tumours or lymphoma[1]
EC NumberEC 2.7.11.1
PathwayCell cycle
p53 signaling pathway
UniProt IDO96017
PDB Structure1GXC; 2CN5; 2CN8; 2W0J; 2W7X; 2WTC; 2WTD; 2WTI; 2WTJ; 2XBJ; 2XK9; 2XM8; 2XM9; 2YCF; 2YCQ; 2YCR; 2YCS; 2YIQ; 2YIR; 2YIT; 3I6U; 3I6W; 3VA4; 4A9R; 4A9S; 4A9T; 4A9U.    
SequenceMSRESDVEAQQSHGSSACSQPHGSVTQSQGSSSQSQGISSSSTSTMPNSSQSSHSSSGTL SSLETVSTQELYSIPEDQEPEDQEPEEPTPAPWARLWALQDGFANLECVNDNYWFGRDKS CEYCFDEPLLKRTDKYRTYSKKHFRIFREVGPKNSYIAYIEDHSGNGTFVNTELVGKGKR RPLNNNSEIALSLSRNKVFVFFDLTVDDQSVYPKALRDEYIMSKTLGSGACGEVKLAFER KTCKKVAIKIISKRKFAIGSAREADPALNVETEIEILKKLNHPCIIKIKNFFDAEDYYIV LELMEGGELFDKVVGNKRLKEATCKLYFYQMLLAVQYLHENGIIHRDLKPENVLLSSQEE DCLIKITDFGHSKILGETSLMRTLCGTPTYLAPEVLVSVGTAGYNRAVDCWSLGVILFIC LSGYPPFSEHRTQVSLKDQITSGKYNFIPEVWAEVSEKALDLVKKLLVVDPKARFTTEEA LRHPWLQDEDMKRKFQDLLSEENESTALPQVLAQPSTSRKRPREGEAEGAETTKRPAVCA AVL
Target ValidationClick to Find Target Validation Information.    
Inhibitor2- (4-Phenoxy-phenyl)-1H-benzoimidazol-5-ylamine[2]
5-Nitro-2- (4-phenoxy-phenyl)-1H-benzoimidazole[2]
DEBROMOHYMENIALDISINE[3]
XL844[1]
MultitargetXL844[1]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Pharmacological abrogation of S-phase checkpoint enhances the anti-tumor activity of gemcitabine in vivo. Cell Cycle. 2007 Jan 1;6(1):104-10. Epub 2007 Jan 7. To Reference
Ref 2J Med Chem. 2005 Mar 24;48(6):1873-85.Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. To Reference
Ref 3Bioorg Med Chem Lett. 2004 Aug 16;14(16):4319-21.Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine. To Reference



 

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