Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM14654
Substrate
Cdc25C peptide substrate
Meas. Tech.
Chk1 Enzymatic Assay
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
29±n/a nM
Citation
 Lin, NHXia, PKovar, PPark, CChen, ZZhang, HRosenberg, SHSham, HL Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors. Bioorg Med Chem Lett 16:421-6 (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:
BDBM14654
Synonyms:
(3Z)-6-(4-hydroxyphenyl)-3-(1H-pyrrol-3-ylmethylidene)-2,3-dihydro-1H-indol-2-one | indolinone analog 18
Type:
Small organic molecule
Emp. Form.:
C19H14N2O2
Mol. Mass.:
302.3267
SMILES:
Oc1ccc(cc1)-c1ccc2\C(=C\c3cc[nH]c3)C(=O)Nc2c1
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