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TargetSerine/threonine-protein kinase Chk1
LigandBDBM12134
Substrate/CompetitorBiotinylated Peptide Substrate
Meas. Tech.Homogeneous Time-resolved Fluorescence (HTRF) Assay
pH7.5±n/a
Temperature295.15±n/a K
IC50 0.25±n/a nM
Citation Fraley MESteen JTBrnardic EJArrington KLSpencer KLHanney BAKim YHartman GDStirdivant SMDrakas BARickert KWalsh ESHamilton KBuser CAHardwick JTao WBeck SCMao XLobell RBSepp-Lorenzino LYan YIkuta MMunshi SKKuo LCKreatsoulas C 3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6. Bioorg Med Chem Lett 16:6049-53 (2006) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
Serine/threonine-protein kinase Chk1
Name:Serine/threonine-protein kinase Chk1/2
Synonyms:CHK1 checkpoint homolog | Checkpoint kinase-1 (CHK1) | Serine/threonine-protein kinase 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:
BDBM12134
Biotinylated Peptide Substrate
Name:Biotinylated Peptide Substrate
Synonyms:n/a
Type:Peptide
Mol. Mass.:1734.89
Organism:n/a
Description:n/a
Residue:17
Sequence:
biotin-GGRARTSSFAEPG