Reaction Details Report a problem with these data
Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM33215
Substrate
biotinylated CDC25C peptide
Meas. Tech.
CHK Kinase Inhibition Assay
pH
7.5±n/a
Temperature
296.15±n/a K
IC50
890±n/a nM
Citation
Matthews, TP; Klair, S; Burns, S; Boxall, K; Cherry, M; Fisher, M; Westwood, IM; Walton, MI; McHardy, T; Cheung, KM; Van Montfort, R; Williams, D; Aherne, GW; Garrett, MD; Reader, J; Collins, 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:
BDBM33215
Synonyms:
pyrazolopyridine, (Rac)-14 | racemic
Type:
Small organic molecule
Emp. Form.:
C17H19N5O
Mol. Mass.:
309.3657
SMILES:
NCC1CN(CCO1)c1c(cnc2[nH]ncc12)-c1ccccc1
Substrate
Name:
biotinylated CDC25C peptide
Synonyms:
n/a
Type:
biotinylated peptide
Mol. Mass.:
3148.69
Organism:
n/a
Description:
n/a
Residue:
27
Sequence:
ITINKKKVSRSGLYRSPSMPENLNRPR