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Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM50223465
Substrate
n/a
Meas. Tech.
ChEMBL_458175 (CHEMBL924433)
IC50
420±n/a nM
Citation
 Garbaccio, RM; Huang, S; Tasber, ES; Fraley, ME; Yan, Y; Munshi, S; Ikuta, M; Kuo, L; Kreatsoulas, C; Stirdivant, S; Drakas, B; Rickert, K; Walsh, ES; Hamilton, KA; Buser, CA; Hardwick, J; Mao, X; Beck, SC; Abrams, MT; Tao, W; Lobell, R; Sepp-Lorenzino, L; Hartman, 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:
BDBM50223465
Synonyms:
3-(9-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinolin-6-yl)propanenitrile | CHEMBL249401
Type:
Small organic molecule
Emp. Form.:
C16H11BrN2O
Mol. Mass.:
327.175
SMILES:
Brc1ccc2c(CCC#N)cc3cc[nH]c(=O)c3c2c1
Structure:
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