Compound name
Leniolisib
Protein family
Protein Kinase
Target name
PIK3CD
Affinity biochemical (nM)
11
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000877a
SMILES
COC1=NC=C(N2CC(C(N[C@H]3CCN(C(CC)=O)C3)=NC=N4)=C4CC2)C=C1C(F)(F)F
InChIKey
MWKYMZXCGYXLPL-ZDUSSCGKSA-N
NCBI gene ID
5293
UniProt ID
O00329
Synonyms
p110D
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Adapta™ TR-FRET assay
Affinity Biochemical Source Knowledge
https://pubs.acs.org/doi/10.1021/acsmedchemlett.7b00293
Affinity biochemical relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
442
Selectivity remarks
Screened at 10 µM, closest targets as % of contr.: RPS6KA5 (76%); Screened against 50 related targets (GPCRs, ion channels, transporters): in-vitro potency of closest targets IC50(hPDE4D) = 4.7 µM, IC50(5HT2B) = 7.7 µM; No activity when tested against CYP isoforms (CYP3A3, CYP2D9, CYP2D6,CYP2C9)
Selectivity Source Knowledge
https://pubs.acs.org/doi/10.1021/acsmedchemlett.7b00293