Compound name
AZD 6482
Protein family
Protein Kinase
Target name
PIK3CB
Affinity biochemical (nM)
10
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000621a
SMILES
CC1=CN2C(=O)C=C(N=C2C(=C1)[C@@H](C)NC3=CC=CC=C3C(=O)O)N4CCOCC4
InChIKey
IRTDIKMSKMREGO-OAHLLOKOSA-N
NCBI gene ID
5291
UniProt ID
P42338
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Alphascreen assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/22906130/
Affinity biochemical relation
=
Selectivity platform
Kinase panel (DSF assay)
Selectivity platform number of targets
100
Selectivity remarks
Screened at 20 µM, closest targets with dTm >1K: dTm(MARK3) = 1.76 K, dTm(MST4) = 1.33 K, dTm(GSK3B) = 1.33 K; Screened against 88 targets in functional assays (AstraZeneca): >200-fold with exception of PIK3 isoforms, PIK3CA (86-fold) and PIK3CG (108-fold), as well as DNA-PK (42-fold), IC50(PIK3CA) = 0.87 µM (AlphaScreen), IC50(PIK3CG) = 1.09 µM (AlphaScreen), IC50(DNA-PK) = 0.42 µM (ELISA), https://pubmed.ncbi.nlm.nih.gov/22906130/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/22906130/