Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM50223448
Substrate
n/a
Meas. Tech.
ChEMBL_458175 (CHEMBL924433)
IC50
110±n/a nM
Citation
 Garbaccio, RMHuang, STasber, ESFraley, MEYan, YMunshi, SIkuta, MKuo, LKreatsoulas, CStirdivant, SDrakas, BRickert, KWalsh, ESHamilton, KABuser, CAHardwick, JMao, XBeck, SCAbrams, MTTao, WLobell, RSepp-Lorenzino, LHartman, GD Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase. Bioorg Med Chem Lett 17:6280-5 (2007) [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:
BDBM50223448
Synonyms:
9-fluoro-2-pyridin-3-yl-3,6-dihydro-1,3,6-triaza-cyclopenta[l]phenanthren-7-one | CHEMBL248584
Type:
Small organic molecule
Emp. Form.:
C19H11FN4O
Mol. Mass.:
330.3152
SMILES:
Fc1ccc2c3[nH]c(nc3c3cc[nH]c(=O)c3c2c1)-c1cccnc1
Structure:
Search PDB for entries with ligand similarity: