Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM50192369
Substrate
n/a
Meas. Tech.
ChEMBL_379936 (CHEMBL864856)
IC50
74±n/a nM
Citation
 Palmer, BDThompson, AMBooth, RJDobrusin, EMKraker, AJLee, HHLunney, EAMitchell, LHOrtwine, DFSmaill, JBSwan, LMDenny, WA 4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modification and phenyl ring substitution. J Med Chem 49:4896-911 (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:
BDBM50192369
Synonyms:
3,9-dihydroxy-4-phenyl-2,3-dihydropyrrolo[3,4-c]carbazol-1(6H)-one | 3,9-dihydroxy-4-phenyl-3,6-dihydropyrrolo[3,4-c]carbazol-1(2H)-one | CHEMBL378766
Type:
Small organic molecule
Emp. Form.:
C20H14N2O3
Mol. Mass.:
330.3368
SMILES:
OC1NC(=O)c2c1c(cc1[nH]c3ccc(O)cc3c21)-c1ccccc1
Structure:
Search PDB for entries with ligand similarity: