Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM50220901
Substrate
n/a
Meas. Tech.
ChEMBL_457438 (CHEMBL941010)
IC50
130±n/a nM
Citation
 Brnardic, EJGarbaccio, RMFraley, METasber, ESSteen, JTArrington, KLDudkin, VYHartman, GDStirdivant, SMDrakas, BARickert, KWalsh, ESHamilton, KBuser, CAHardwick, JTao, WBeck, SCMao, XLobell, RBSepp-Lorenzino, LYan, YIkuta, MMunshi, SKKuo, LCKreatsoulas, 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:
BDBM50220901
Synonyms:
3-methyl-2,5,7,8,9,10-hexahydro-1,2,5-triaza-cyclopenta[a]anthracen-4-one | CHEMBL251211
Type:
Small organic molecule
Emp. Form.:
C15H15N3O
Mol. Mass.:
253.2991
SMILES:
Cc1[nH]nc2c1c(=O)[nH]c1cc3CCCCc3cc21
Structure:
Search PDB for entries with ligand similarity: