Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM50204693
Substrate
n/a
Meas. Tech.
ChEMBL_442099 (CHEMBL891237)
IC50
13±n/a nM
Citation
 Tong, YClaiborne, AStewart, KDPark, CKovar, PChen, ZCredo, RBGu, WZGwaltney, SLJudge, RAZhang, HRosenberg, SHSham, HLSowin, TJLin, NH Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors. Bioorg Med Chem 15:2759-67 (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:
BDBM50204693
Synonyms:
3-(4'-hydroxy-biphenyl-4-yl)-1,4-dihydro-indeno[1,2-c]pyrazole-6-carboxylic acid (pyridin-4-ylmethyl)-amide | CHEMBL242753
Type:
Small organic molecule
Emp. Form.:
C29H22N4O2
Mol. Mass.:
458.5106
SMILES:
Oc1ccc(cc1)-c1ccc(cc1)-c1n[nH]c-2c1Cc1cc(ccc-21)C(=O)NCc1ccncc1
Structure:
Search PDB for entries with ligand similarity: