Compound name
Enzastaurin
Protein family
Protein Kinase
Target name
PRKCB
Affinity biochemical (nM)
6
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000154b
SMILES
Cn1cc(C2=C(c3cn(C4CCN(Cc5ccccn5)CC4)c4ccccc34)C(=O)NC2=O)c2ccccc21
InChIKey
AXRCEOKUDYDWLF-UHFFFAOYSA-N
NCBI gene ID
5579
UniProt ID
P05771
Synonyms
PKCbeta
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Filter-binding assays
Affinity Biochemical Source Knowledge
https://doi.org/10.1158/0008-5472.CAN-05-0071
Affinity biochemical relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
456
Selectivity remarks
Screened at 1 µM, follow-up Kds for closest targets: Kd(GSK3B) = 8.3 nM, Kd(PRKCD) = 25 nM, Kd(RSK4) = 25 nM, Kd(PRKCQ) = 36 nM, Kd(FLT3(D835Y)) = 40 nM, Kd(PRKCH) = 46 nM, Kd(FLT3(D835H)) = 49 nM, Kd(FLT3(ITD)) = 72 nM, Kd(MAPK15) = 76 nM, Kd(RSK2Kd) = 87 nM, 18 other targets with Kd 0.1-1 µM;
Selectivity Source Knowledge
https://www.guidetopharmacology.org/GRAC/LigandScreenDisplayForward?ligandId=5693&screenId=2
Selectivity Number of Off-targets
10