Compound name
Taselisib
Protein family
Protein Kinase
Target name
PIK3CB
Affinity biochemical (nM)
9.1
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000685a
SMILES
CC1=NN(C(C)C)C(C2=CN(CCO3)C(C4=C3C=C(C5=CN(C(C)(C)C(N)=O)N=C5)C=C4)=N2)=N1
InChIKey
BEUQXVWXFDOSAQ-UHFFFAOYSA-N
NCBI gene ID
5291
UniProt ID
P42338
Mode of action
Inhibitor
Affinity biochemical definition
Ki
Affinity biochemical assay type
Enzymatic fluorescence polarization assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/jm4003632
Affinity biochemical relation
=
Selectivity platform
SelectScreen panel (Invitrogen)
Selectivity platform number of targets
235
Selectivity remarks
Screened at 1 µM, closest targets as % of cont.: PIK3C2B (80.4%), PIK3CA (98.6%), PIK3CD (97.9%), PIK3CG (90.6%), PIK3C3 (69.9%); IC50 follow-up of closest targets: IC50(PIK3C2B) = 292 nM, IC50(PIK3C3) = 374 nM, >1000-fold selective
Selectivity Source Knowledge
https://doi.org/10.1021/jm4003632
Selectivity Number of Off-targets
0