Compound name
PI-103
Protein family
Protein Kinase
Target name
PIK3CA
Affinity biochemical (nM)
2
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000658a
SMILES
Oc1cccc(c1)c1nc(N2CCOCC2)c2oc3ncccc3c2n1
InChIKey
TUVCWJQQGGETHL-UHFFFAOYSA-N
NCBI gene ID
5290
UniProt ID
P42336
Synonyms
PI3K
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Scintillation proximity radiometric assay (1 µM ATP)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/17575152/
Affinity biochemical relation
=
Selectivity platform
Kinase panel (competition-binding assays)
Selectivity platform number of targets
442
Selectivity remarks
In-vitro potencies of closest targets in the screen: Kd(MTOR) = 12 nM, Kd(HIPK3) = 310 nM, Kd(PIP5K2C) = 620 nM, Kd(RIOK2), Kd(DAPK3) = 840 nM, Kd(YSK4) = 930 nM, full screening data are available as supporting information;
Screened against 69 kinases at 1 µM, closest targets as % of control: SmMLCK (62%), HIPK2 (67%), full screening data available in paper, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2267365/;
Screened against 69 kinases at 1 µM, closest targets as % of control: SmMLCK (62%), HIPK2 (67%), full screening data available in paper, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2267365/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/22037378/
Selectivity Number of Off-targets
6