Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM14717
Substrate
Cdc25C peptide substrate
Meas. Tech.
Chk1 Enzymatic Assay
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
7±n/a nM
Citation
 Li, GHasvold, LATao, ZFWang, GTGwaltney, SLPatel, JKovar, PCredo, RBChen, ZZhang, HPark, CSham, HLSowin, TRosenberg, SHLin, NH Synthesis and biological evaluation of 1-(2,4,5-trisubstituted phenyl)-3-(5-cyanopyrazin-2-yl)ureas as potent Chk1 kinase inhibitors. Bioorg Med Chem Lett 16:2293-8 (2006) [PubMed]  Article 
Target
Name:
Serine/threonine-protein kinase Chk1
Synonyms:
CHEK1 | CHK1 | CHK1 checkpoint homolog | CHK1_HUMAN | Checkpoint kinase-1 (CHK1)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
54443.02
Organism:
Homo sapiens (Human)
Description:
gi_166295192
Residue:
476
Sequence:
MAVPFVEDWDLVQTLGEGAYGEVQLAVNRVTEEAVAVKIVDMKRAVDCPENIKKEICINKMLNHENVVKFYGHRREGNIQYLFLEYCSGGELFDRIEPDIGMPEPDAQRFFHQLMAGVVYLHGIGITHRDIKPENLLLDERDNLKISDFGLATVFRYNNRERLLNKMCGTLPYVAPELLKRREFHAEPVDVWSCGIVLTAMLAGELPWDQPSDSCQEYSDWKEKKTYLNPWKKIDSAPLALLHKILVENPSARITIPDIKKDRWYNKPLKKGAKRPRVTSGGVSESPSGFSKHIQSNLDFSPVNSASSEENVKYSSSQPEPRTGLSLWDTSPSYIDKLVQGISFSQPTCPDHMLLNSQLLGTPGSSQNPWQRLVKRMTRFFTKLDADKSYQCLKETCEKLGYQWKKSCMNQVTISTTDRRNNKLIFKVNLLEMDDKILVDFRLSKGDGLEFKRHFLKIKGKLIDIVSSQKIWLPAT
  
Inhibitor
Name:
BDBM14717
Synonyms:
1-(5-chloro 2,4-dimethoxyphenyl)-3-(5-cyanopyrazin-2-yl)urea | 3-(5-chloro-2,4-dimethoxyphenyl)-1-(5-cyanopyrazin-2-yl)urea | Urea Compound 2
Type:
Small Organic Molecule
Emp. Form.:
C14H12ClN5O3
Mol. Mass.:
333.73
SMILES:
COc1cc(OC)c(NC(=O)Nc2cnc(cn2)C#N)cc1Cl
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Cdc25C peptide substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2519.88
Organism:
n/a
Description:
Cdc25c peptide substrate contained a sequence of amino acid residues 204-225 of human phosphatase Cdc25C.
Residue:
22
Sequence:
AKVSRSGLYRSPSMPENLNRPR