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Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM50195216
Substrate
n/a
Meas. Tech.
ChEMBL_424834 (CHEMBL908461)
EC50
120±n/a nM
Citation
 Huang, S; Garbaccio, RM; Fraley, ME; Steen, J; Kreatsoulas, C; Hartman, G; Stirdivant, S; Drakas, B; Rickert, K; Walsh, E; Hamilton, K; Buser, CA; Hardwick, J; Mao, X; Abrams, M; Beck, S; Tao, W; Lobell, R; Sepp-Lorenzino, L; Yan, Y; Ikuta, M; Murphy, JZ; Sardana, V; Munshi, S; Kuo, L; Reilly, M; Mahan, E Development of 6-substituted indolylquinolinones as potent Chek1 kinase inhibitors. Bioorg Med Chem Lett 16:5907-12 (2006) [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:
BDBM50195216
Synonyms:
3-(5-((4-fluoropiperidin-1-yl)methyl)-1H-indol-2-yl)-6-(1H-pyrazol-4-yl)quinolin-2(1H)-one | CHEMBL220956
Type:
Small organic molecule
Emp. Form.:
C26H24FN5O
Mol. Mass.:
441.5001
SMILES:
FC1CCN(Cc2ccc3[nH]c(cc3c2)-c2cc3cc(ccc3[nH]c2=O)-c2cn[nH]c2)CC1
Structure:
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