Compound name
CAL-101
Protein family
Protein Kinase
Target name
PIK3CG
Affinity biochemical (nM)
89
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000876a
SMILES
FC1=CC=CC(N=C([C@@H](NC2=C(N=CN3)C3=NC=N2)CC)N4C5=CC=CC=C5)=C1C4=O
InChIKey
IFSDAJWBUCMOAH-HNNXBMFYSA-N
NCBI gene ID
5294
UniProt ID
P48736
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Competition binding assay (Ambit)
Affinity Biochemical Source Knowledge
https://ashpublications.org/blood/article/117/2/591/28152/CAL-101-a-p110-selective-phosphatidylinositol-3
Affinity biochemical relation
=
Selectivity platform
Ambit KINOMEscan
Selectivity platform number of targets
402
Selectivity remarks
Screened at 10 µM, IC50(PIK3CD) = 2.5 nM, IC50(PIK3CG) = 89 nM, 40-300-fold selective to other PI3K class I enzymes: IC50(PIK3CG) = 565 nM, IC50(PIK3CA) = 820 nM; 400- to 4000-fold selective against related kinases C2β, hVPS34, DNA-PK, and mTOR
Selectivity Source Knowledge
https://ashpublications.org/blood/article/117/2/591/28152/CAL-101-a-p110-selective-phosphatidylinositol-3
Selectivity Number of Off-targets
0