Compound name
BAY1125976
Protein family
Protein Kinase
Target name
AKT1
Affinity biochemical (nM)
5.2
Affinity on-target cellular (nM)
0.9
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000637a
SMILES
C1CC(C1)(C2=CC=C(C=C2)C3=C(N4C(=N3)C=CC(=N4)C(=O)N)C5=CC=CC=C5)N
InChIKey
JBGYKRAZYDNCNV-UHFFFAOYSA-N
NCBI gene ID
207
UniProt ID
P31749
Synonyms
RAC, PKB, PRKBA, AKT, RAC-alpha
Mode of action
Allosteric Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
TR-FRET-based in vitro kinase assays (10 µM ATP)
Affinity Biochemical Source Knowledge
https://doi.org/10.1002/ijc.30457
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
TR-FRET assay (inhibition of AKT1-T308 phosphorylation in KPL-4 cells)
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
468
Selectivity remarks
Screened at 10 µM, follow-up Kds and IC50s of closest targets: Kd(FLT1,D835Y) = 210 nM, Kd(CKL1) = 310 nM, Kd(MKNK2) = 330 nM, IC50(AKT3) = 427 nM.
Selectivity Source Knowledge
https://doi.org/10.1002/ijc.30457
Selectivity Number of Off-targets
4