Compound name
SAR405
Protein family
Protein Kinase
Target name
PIK3C3
Affinity biochemical (nM)
1.2
Affinity on-target cellular (nM)
27
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001786a
SMILES
C[C@@H]1COCCN1c1cc(=O)n2c(n1)N(Cc1cncc(Cl)c1)[C@H](C(F)(F)F)CC2
InChIKey
SPDQRCUBFSRAFI-DOMZBBRYSA-N
NCBI gene ID
5289
UniProt ID
Q8NEB9
Synonyms
Vps34
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
(phosphorylation of a PtdIns substrate by human recombinant Vps34 enzyme)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/25326666/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Vps34 cellular assay (using HeLa cells stably transfected with GFP-FYVE)
Affinity on-target cellular source knowledge
https://www.nature.com/articles/nchembio.1681
Affinity on-target cellular relation
=
Selectivity platform
KiNativTM Profiling (ActivX Biosciences using Jurkat cell lysates)
Selectivity platform number of targets
203
Selectivity remarks
Screened at 1 µM, (MS experiment, 298 protein and lipid kinase peptides, corresponding to 203 unique protein and lipid kinase), closest targets as % of inhibition: PIK3C3 (>96%), PIK3CB (67.7%), PIK3CD (62.5%), SMG(52%)
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/25326666/
Selectivity Number of Off-targets
0