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Found 21 Enz. Inhib. hit(s) with Target = 'Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform' and Ligand = 'BDBM92862'
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  4nMAssay Description:Inhibition of choline acetyltransferase (ChAT) activityMore data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  4nMAssay Description:Inhibition of C-terminal His-tagged full-length PI3K p110alpha (unknown origin) expressed in baculovirus incubated for 60 mins by Kinase-Glo luminesc...More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  4nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  4nMAssay Description:Inhibition of PI3K alpha (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  4nMAssay Description:Inhibition of PI3Kalpha (unknown origin) expressed in baculovirus expression system using L-alpha-phosphatidylinositol as substrate by luminescence a...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Rattus norvegicus (Rat))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  5.30nMAssay Description:Inhibition of PI3Kalpha in rat Rat1 cells assessed as reduction in phosphorylation of AKT at Ser473 residue incubated for 1 hr by cellular assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  6.20nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2/PS as substrate after 1 hr by luciferase-based luminescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  7nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using substrate PI incubated for 1 hr by Adapta kinase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50: <10nMAssay Description:Inhibition of PI3KalphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  11nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs in presence of ATP by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  16nMAssay Description:Inhibition of recombinant human PI3K-alpha using PIP2:3PS as substrate preincubated for 15 mins followed by ATP addition measured after 1 hr by ADP-G...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  16nMAssay Description:Inhibition of PI3K p110alpha (unknown origin) using PIP2 as substrate by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  17nMAssay Description:Inhibition of recombinant PI3Kalpha (unknown origin) using phosphatidyl inositol as substrate after 30 to 60 mins in presence of ATP by Kinase Glo lu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  20nMAssay Description:Inhibition of human PI3K-alpha assessed as inhibition of Ptdlns(3,4,5)P3 phosphorylation after 1 hr by TR-FRET analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  29nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate incubated for 1 hr in presence of ATP by Kinase Glo luminescence assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  30nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 1 hr by Kinase-Glo luminescent assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  32.5nMpH: 7.5 T: 2°CAssay Description:1. Preparation of test reagents{circle around (1)} 1x kinase buffer (50 mM HEPES, pH 7.5, 3 mM MgCl2, 1 mM EGTA, 100 mM NaCl, 0.03% CHAPS, 2 mM DTT);...More data for this Ligand-Target Pair
In DepthDetails US Patent
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  49nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  54nMAssay Description:Inhibition of PI3Kalpha (unknown origin) assessed as reduction of ATP level after 40 mins by luciferase based luminescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  89nMAssay Description:Inhibition of PI3Kalpha (unknown origin) assessed as reduction in ATP depletion using lipid substrate after 40 mins by Kinase-Glo luminescent assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataEC50:  40nMAssay Description:Inhibition of wild type PI3Kalpha (unknown origin) after 40 mins by kinase-Glo reagent based luminescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed