Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM33202
Substrate
biotinylated CHKtide
Meas. Tech.
CHK1 AlphaScreen
pH
7.5±n/a
Temperature
296.15±n/a K
Comments
26.4 +/- 6.9 inhibition @ 250 uM.
Citation
 Matthews, TPKlair, SBurns, SBoxall, KCherry, MFisher, MWestwood, IMWalton, MIMcHardy, TCheung, KMVan Montfort, RWilliams, DAherne, GWGarrett, MDReader, JCollins, I Identification of inhibitors of checkpoint kinase 1 through template screening. J Med Chem 52:4810-9 (2009) [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:
BDBM33202
Synonyms:
benzisoxazole, 1
Type:
Small organic molecule
Emp. Form.:
C16H10FN3O
Mol. Mass.:
279.2685
SMILES:
Fc1ccc(cc1)-c1onc2ccc(cc12)-c1cc[nH]n1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated CHKtide
Synonyms:
n/a
Type:
biotinylated peptide
Mol. Mass.:
3148.69
Organism:
n/a
Description:
n/a
Residue:
27
Sequence:
ITINKKKVSRSGLYRSPSMPENLNRPR