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Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM17140
Substrate
Synthetic Chk1 Peptide Substrate
Meas. Tech.
Chk1 Enzymatic Assay
pH
7.4±n/a
Temperature
310.15±n/a K
Ki
15±4 nM
Comments
The apparent Km for ATP in the Chk1 assay was about 120 uM.
Citation
 Zhao, B; Bower, MJ; McDevitt, PJ; Zhao, H; Davis, ST; Johanson, KO; Green, SM; Concha, NO; Zhou, BB Structural basis for Chk1 inhibition by UCN-01. J Biol Chem 277:46609-15 (2002) [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:
BDBM17140
Synonyms:
(15R,18R)-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]octacosa-1,6,8(13),9,11,20(25),21,23,26-nonaene-3,5-dione | SB 218078 | SB-218078 | SB218078
Type:
Small organic molecule
Emp. Form.:
C24H15N3O3
Mol. Mass.:
393.3942
SMILES:
O=C1NC(=O)c2c1c1c3ccccc3n3[C@H]4CC[C@@H](O4)n4c5ccccc5c2c4c13 |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Synthetic Chk1 Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2323.67
Organism:
n/a
Description:
A synthetic peptide with a sequence flanking Ser-216 of human Cdc25C.
Residue:
20
Sequence:
KVSRSGLYRSPSMPENLNRK