Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM33210
Substrate
biotinylated CHKtide
Meas. Tech.
CHK1 AlphaScreen
pH
7.5±n/a
Temperature
296.15±n/a K
Comments
75.7 +/- 1.0 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:
BDBM33210
Synonyms:
4-(7H-purin-6-yl)morpholine | purine, 9
Type:
Small organic molecule
Emp. Form.:
C9H11N5O
Mol. Mass.:
205.2165
SMILES:
C1CN(CCO1)c1ncnc2nc[nH]c12
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