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Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM17054
Substrate
Synthetic Chk1 Peptide Substrate
Meas. Tech.
Chk1 Enzymatic Assay
pH
7.4±n/a
Temperature
310.15±n/a K
Ki
5.6±2.0 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:
Human
Description:
gi_166295192
Residue:
476
Sequence:
MAVPFVEDWDLVQTLGEGAYGEVQLAVNRVTEEAVAVKIVDMKRAVDCPENIKKEICINKMLNHENVVKFYGHRREGNIQYLFLEYCSGGELFDRIEPDIGMPEPDAQRFFHQLMAGVVYLHGIGITHRDIKPENLLLDERDNLKISDFGLATVFRYNNRERLLNKMCGTLPYVAPELLKRREFHAEPVDVWSCGIVLTAMLAGELPWDQPSDSCQEYSDWKEKKTYLNPWKKIDSAPLALLHKILVENPSARITIPDIKKDRWYNKPLKKGAKRPRVTSGGVSESPSGFSKHIQSNLDFSPVNSASSEENVKYSSSQPEPRTGLSLWDTSPSYIDKLVQGISFSQPTCPDHMLLNSQLLGTPGSSQNPWQRLVKRMTRFFTKLDADKSYQCLKETCEKLGYQWKKSCMNQVTISTTDRRNNKLIFKVNLLEMDDKILVDFRLSKGDGLEFKRHFLKIKGKLIDIVSSQKIWLPAT
  
Inhibitor
Name:
BDBM17054
Synonyms:
(2S,3R,4R,6R,18R)-18-hydroxy-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one | (5S,6R,7R,9R,16R)-16-hydroxy-6-methoxy-5-methyl-7-(methylamino)-6,7,8,9,15,16-hexahydro-5H,14H-5,9-epoxy-4b,9a,15-triazadibenzo[b,h]cyclonona[1,2,3,4-jkl]cyclopenta[e]-as-indacen-14-one | 7-Hydroxystaurosporine | UCN-01
Type:
Small organic molecule
Emp. Form.:
C28H26N4O4
Mol. Mass.:
482.5304
SMILES:
[H][C@]12C[C@@H](NC)[C@@H](OC)[C@](C)(O1)n1c3ccccc3c3c4[C@@H](O)NC(=O)c4c4c5ccccc5n2c4c13 |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