Compound name
PF-477736
Protein family
Protein Kinase
Target name
CHEK1
Affinity biochemical (nM)
0.49
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000665a
SMILES
O=C([C@H](N)C1CCCCC1)NC2=CC3=C4C(NC(C5=CN(C)N=C5)=C4C=NNC3=O)=C2
InChIKey
NDEXUOWTGYUVGA-LJQANCHMSA-N
NCBI gene ID
1111
UniProt ID
O14757
Synonyms
CHK1
Mode of action
Inhibitor
Affinity biochemical definition
Ki
Affinity biochemical assay type
Biochemical activity-based assay (0.15 mM ATP)
Affinity Biochemical Source Knowledge
https://doi.org/ 10.1158/1535-7163.MCT-07-2391
Affinity biochemical relation
=
Selectivity platform
Kinase panel, literature
Selectivity platform number of targets
100
Selectivity remarks
Screened at 1 µM or 10 µM (iknase panel literature or Upstate/Millipore); Closest targets: Ki(VEGFR2) = 8 nM, IC50(YES) = 14 nM, IC50(FMS) = 10 nM, IC50(AURKA) = 23nM, IC50(FGFR3) = 23 nM, IC50(FLT3) = 25 nM, IC50(RET) = 39 nM;
Selectivity Source Knowledge
https://doi.org/ 10.1158/1535-7163.MCT-07-2391
Selectivity Number of Off-targets
7