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Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM50220886
Substrate
n/a
Meas. Tech.
ChEMBL_457438 (CHEMBL941010)
IC50
1.1±n/a nM
Citation
 Brnardic, EJ; Garbaccio, RM; Fraley, ME; Tasber, ES; Steen, JT; Arrington, KL; Dudkin, VY; Hartman, GD; Stirdivant, SM; Drakas, BA; Rickert, K; Walsh, ES; Hamilton, K; Buser, CA; Hardwick, J; Tao, W; Beck, SC; Mao, X; Lobell, RB; Sepp-Lorenzino, L; Yan, Y; Ikuta, M; Munshi, SK; Kuo, LC; Kreatsoulas, C Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors. Bioorg Med Chem Lett 17:5989-94 (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:
BDBM50220886
Synonyms:
5-(3-aminopropyl)-7,8-dicyclohexyl-3-methyl-2H-pyrazolo[4,3-c]quinolin-4(5H)-one | CHEMBL250481
Type:
Small organic molecule
Emp. Form.:
C26H36N4O
Mol. Mass.:
420.5902
SMILES:
Cc1[nH]nc2c1c(=O)n(CCCN)c1cc(C3CCCCC3)c(cc21)C1CCCCC1
Structure:
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