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TargetSerine/threonine-protein kinase Chk1
LigandBDBM50212492
Substrate/Competitorn/a
Meas. Tech.ChEMBL_447306 (CHEMBL896339)
IC50 5.2±n/a nM
Citation Tong, YClaiborne, APyzytulinska, MTao, ZFStewart, KDKovar, PChen, ZCredo, RBGuan, RMerta, PJZhang, HBouska, JEveritt, EAMurry, BPHickman, DStratton, TJWu, JRosenberg, SHSham, HLSowin, TJLin, NH 1,4-Dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: extended exploration on phenyl ring substitutions and preliminary ADME/PK studies. Bioorg Med Chem Lett17:3618-23 (2007) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Serine/threonine-protein kinase Chk1
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:
MAVPFVEDWDLVQTLGEGAYGEVQLAVNRVTEEAVAVKIVDMKRAVDCPENIKKEICINK
MLNHENVVKFYGHRREGNIQYLFLEYCSGGELFDRIEPDIGMPEPDAQRFFHQLMAGVVY
LHGIGITHRDIKPENLLLDERDNLKISDFGLATVFRYNNRERLLNKMCGTLPYVAPELLK
RREFHAEPVDVWSCGIVLTAMLAGELPWDQPSDSCQEYSDWKEKKTYLNPWKKIDSAPLA
LLHKILVENPSARITIPDIKKDRWYNKPLKKGAKRPRVTSGGVSESPSGFSKHIQSNLDF
SPVNSASSEENVKYSSSQPEPRTGLSLWDTSPSYIDKLVQGISFSQPTCPDHMLLNSQLL
GTPGSSQNPWQRLVKRMTRFFTKLDADKSYQCLKETCEKLGYQWKKSCMNQVTISTTDRR
NNKLIFKVNLLEMDDKILVDFRLSKGDGLEFKRHFLKIKGKLIDIVSSQKIWLPAT
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50212492
n/a
NameBDBM50212492
Synonyms:4'-{7-[(2-dimethylamino-ethylamino)-methyl]-1,4-dihydro-indeno[1,2-c]pyrazol-3-yl}-biphenyl-4-ol | CHEMBL234867
TypeSmall organic molecule
Emp. Form.C27H28N4O
Mol. Mass.424.5374
SMILESCN(C)CCNCc1ccc2Cc3c(n[nH]c3-c2c1)-c1ccc(cc1)-c1ccc(O)cc1
Structure
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