Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM50220777
Substrate
n/a
Meas. Tech.
ChEMBL_457402 (CHEMBL941921)
IC50
5.9±n/a nM
Citation
 Tong, YPrzytulinska, MTao, ZFBouska, JStewart, KDPark, CLi, GClaiborne, AKovar, PChen, ZMerta, PJBui, MHOlson, AOsterling, DZhang, HSham, HLRosenberg, SHSowin, TJLin, NH Cyanopyridyl containing 1,4-dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: improving oral biovailability. Bioorg Med Chem Lett 17:5665-70 (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:
BDBM50220777
Synonyms:
5-(7-(2-morpholinoethoxy)-1,4-dihydroindeno[1,2-c]pyrazol-3-yl)picolinonitrile | CHEMBL249282
Type:
Small organic molecule
Emp. Form.:
C22H21N5O2
Mol. Mass.:
387.4344
SMILES:
N#Cc1ccc(cn1)-c1n[nH]c-2c1Cc1ccc(OCCN3CCOCC3)cc-21
Structure:
Search PDB for entries with ligand similarity: