BDBM92862 US9284315, BEZ-235::mTOR Inhibitor, BEZ235
SMILES Cn1c2cnc3ccc(cc3c2n(-c2ccc(cc2)C(C)(C)C#N)c1=O)-c1cnc2ccccc2c1
InChI Key InChIKey=JOGKUKXHTYWRGZ-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 140 hits for monomerid = 92862
Affinity DataKi: 1.70nM ΔG°: -12.0kcal/mole IC50: 3.90nMT: 2°CAssay Description:The LanthaScreen TR-FRET mTOR assay was performed using Costar low-binding 284-well plates at room temperature according to the instructions of the m...More data for this Ligand-Target Pair
Affinity DataKi: 2.5nM IC50: 9.60nMAssay Description:The mTOR activity was determined by measuring the amount of [gamma-33 P] phosphae from ATP incorporated in the substrate protein.More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Zuanzhu Pharma
US Patent
Zuanzhu Pharma
US Patent
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
Affinity DataIC50: 3.23nMpH: 7.5 T: 2°CAssay Description:1. Preparation of test reagents {circle around (1)} 1x kinase buffer (50 mM HEPES, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 3 mM MnCl, 0.01% Tween-20, 2 mM DT...More data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description:Inhibition of human recombinant mTOR assessed as inhibition of 4EBP1 phosphorylation after 30 mins by TR-FRET analysisMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Zuanzhu Pharma
US Patent
Zuanzhu Pharma
US Patent
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
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Northeastern University
Curated by ChEMBL
Northeastern University
Curated by ChEMBL
Affinity DataIC50: 316nMAssay Description:Inhibition of human PI3K-beta assessed as inhibition of Ptdlns(3,4,5)P3 phosphorylation after 1 hr by TR-FRET analysisMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Northeastern University
Curated by ChEMBL
Northeastern University
Curated by ChEMBL
Affinity DataIC50: 100nMAssay Description:Inhibition of human PI3K-gamma assessed as inhibition of Ptdlns(3,4,5)P3 phosphorylation after 1 hr by TR-FRET analysisMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Northeastern University
Curated by ChEMBL
Northeastern University
Curated by ChEMBL
Affinity DataIC50: 13nMAssay Description:Inhibition of human PI3K-delta assessed as inhibition of Ptdlns(3,4,5)P3 phosphorylation after 1 hr by TR-FRET analysisMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Northeastern University
Curated by ChEMBL
Northeastern University
Curated by ChEMBL
Affinity DataIC50: <10nMAssay Description:Inhibition of PI3KdeltaMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Zuanzhu Pharma
US Patent
Zuanzhu Pharma
US Patent
Affinity DataIC50: <10nMAssay Description:Inhibition of PI3KalphaMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Northeastern University
Curated by ChEMBL
Northeastern University
Curated by ChEMBL
Affinity DataIC50: <10nMAssay Description:Inhibition of PI3KbetaMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Northeastern University
Curated by ChEMBL
Northeastern University
Curated by ChEMBL
Affinity DataIC50: <10nMAssay Description:Inhibition of PI3KgammaMore data for this Ligand-Target Pair
Affinity DataIC50: 12nMAssay Description:Inhibition of mTOR (unknown origin) using GFP-4E-BP1 as substrate after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Zuanzhu Pharma
US Patent
Zuanzhu Pharma
US Patent
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
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Zuanzhu Pharma
US Patent
Zuanzhu Pharma
US Patent
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
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Northeastern University
Curated by ChEMBL
Northeastern University
Curated by ChEMBL
Affinity DataIC50: 399nMAssay Description:Inhibition of PI3Kbeta (unknown origin) assessed as reduction of ATP level after 40 mins by luciferase based luminescence assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Northeastern University
Curated by ChEMBL
Northeastern University
Curated by ChEMBL
Affinity DataIC50: 95nMAssay Description:Inhibition of PI3Kgamma (unknown origin) assessed as reduction of ATP level after 40 mins by luciferase based luminescence assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Northeastern University
Curated by ChEMBL
Northeastern University
Curated by ChEMBL
Affinity DataIC50: 164nMAssay Description:Inhibition of PI3Kdelta (unknown origin) assessed as reduction of ATP level after 40 mins by luciferase based luminescence assayMore data for this Ligand-Target Pair
Affinity DataIC50: 89nMAssay Description:Inhibition of mTOR (unknown origin) assessed as reduction of ATP level after 40 mins by luciferase based luminescence assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Xi'An Jiaotong University
Curated by ChEMBL
Xi'An Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 49nMAssay Description:Inhibition of p110alpha/p85alpha (unknown origin) incubated for 40 mins by luciferase based ATP depletion assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Xi'An Jiaotong University
Curated by ChEMBL
Xi'An Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 478nMAssay Description:Inhibition of p110beta/p85alpha (unknown origin) incubated for 40 mins by luciferase based ATP depletion assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Xi'An Jiaotong University
Curated by ChEMBL
Xi'An Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 138nMAssay Description:Inhibition of p110delta/p85alpha (unknown origin) incubated for 40 mins by luciferase based ATP depletion assayMore data for this Ligand-Target Pair
Affinity DataIC50: 44nMAssay Description:Inhibition of mTORC1 (unknown origin) incubated for 40 mins by luciferase based ATP depletion assayMore data for this Ligand-Target Pair
TargetSerine-protein kinase ATM(Homo sapiens (Human))
Duke University School Of Medicine
Curated by ChEMBL
Duke University School Of Medicine
Curated by ChEMBL
Affinity DataIC50: 7nMAssay Description:Inhibition of ATM (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of human recombinant mTOR using substrate PI incubated for 1 hr by Adapta kinase assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta(Homo sapiens (Human))
Curtin University
Curated by ChEMBL
Curtin University
Curated by ChEMBL
Affinity DataIC50: 44nMAssay Description:Inhibition of human recombinant PI3KC2beta using substrate PI incubated for 1 hr by Adapta kinase assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase catalytic subunit type 3(Homo sapiens (Human))
Curtin University
Curated by ChEMBL
Curtin University
Curated by ChEMBL
Affinity DataIC50: 450nMAssay Description:Inhibition of human recombinant Vps34 using substrate PI incubated for 1 hr by Adapta kinase assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Zuanzhu Pharma
US Patent
Zuanzhu Pharma
US Patent
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
TargetPhosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha(Homo sapiens (Human))
Curtin University
Curated by ChEMBL
Curtin University
Curated by ChEMBL
Affinity DataIC50: 34nMAssay Description:Inhibition of human recombinant PI3KC2alpha using substrate PI incubated for 1 hr by Adapta kinase assayMore data for this Ligand-Target Pair
Affinity DataIC50: 21nMAssay Description:Inhibition of mTOR (unknown origin) expressed in baculovirus after 60 mins by kinase-glo assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Xi'An Jiaotong University
Curated by ChEMBL
Xi'An Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 4nMAssay Description:Inhibition of PI3Kalpha/p85 iSH2 domain (unknown origin) expressed in baculovirus using l-alpha-phosphatidylinositol as substrate after 60 mins by ki...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Northeastern University
Curated by ChEMBL
Northeastern University
Curated by ChEMBL
Affinity DataIC50: 5nMAssay Description:Inhibition of PI3Kdelta (unknown origin) expressed in baculovirus co-expressing p85 using l-alpha-phosphatidylinositol as substrate after 120 mins by...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Northeastern University
Curated by ChEMBL
Northeastern University
Curated by ChEMBL
Affinity DataIC50: 7nMAssay Description:Inhibition of PI3Kgamma (unknown origin) expressed in baculovirus co-expressing p85 using l-alpha-phosphatidylinositol as substrate after 120 mins by...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Northeastern University
Curated by ChEMBL
Northeastern University
Curated by ChEMBL
Affinity DataIC50: 76nMAssay Description:Inhibition of PI3Kbeta (unknown origin) expressed in baculovirus co-expressing p85 using l-alpha-phosphatidylinositol as substrate after 60 mins by k...More data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+3nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Northeastern University
Curated by ChEMBL
Northeastern University
Curated by ChEMBL
Affinity DataIC50: 89nMAssay Description:Inhibition of PI3K p110delta (unknown origin) using PIP2 as substrate after 1 hr by ADP-Glo kinase assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Northeastern University
Curated by ChEMBL
Northeastern University
Curated by ChEMBL
Affinity DataIC50: 26nMAssay Description:Inhibition of recombinant full length His-tagged human PI3K p110gamma expressed in baculovirus expression system using PIP2 as substrate after 1 hr b...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Xi'An Jiaotong University
Curated by ChEMBL
Xi'An Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 35nMAssay Description:Inhibition of PI3K p110alpha/p85alpha (unknown origin) using PIP2 as substrate after 1 hr by luminescent kinase-Glo assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Xi'An Jiaotong University
Curated by ChEMBL
Xi'An Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 16nMAssay Description:Inhibition of recombinant full length human N-terminal His6-tagged PI3K p110beta/p85alpha expressed in baculovirus infected Sf21 cells using PIP2 as ...More data for this Ligand-Target Pair
Affinity DataIC50: 21nMAssay Description:Inhibition of recombinant human N-terminal FLAG-tagged mTOR (1362-end residues) using ULight-4E-BP1 peptide substrate after 1 hr in presence of ATP b...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Xi'An Jiaotong University
Curated by ChEMBL
Xi'An Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 89nMAssay Description:Inhibition of P110alpha/p85alpha (unknown origin) using L-alpha-phosphatidylinositol as substrate after 40 mins by ATP depletion assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Xi'An Jiaotong University
Curated by ChEMBL
Xi'An Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 421nMAssay Description:Inhibition of P110beta/p85alpha (unknown origin) using L-alpha-phosphatidylinositol as substrate after 40 mins by ATP depletion assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform/Phosphoinositide 3-kinase regulatory subunit 5(Homo sapiens (Human))
Xi'An Jiaotong University
Curated by ChEMBL
Xi'An Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 169nMAssay Description:Inhibition of P110gamma/PIK3R5 (unknown origin) using L-alpha-phosphatidylinositol as substrate after 40 mins by ATP depletion assayMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Xi'An Jiaotong University
Curated by ChEMBL
Xi'An Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 204nMAssay Description:Inhibition of P110delta/p85alpha (unknown origin) using L-alpha-phosphatidylinositol as substrate after 40 mins by ATP depletion assayMore data for this Ligand-Target Pair
Affinity DataIC50: 97nMAssay Description:Inhibition of mTOR (unknown origin) using L-alpha-phosphatidylinositol as substrate after 40 mins by ATP depletion assayMore data for this Ligand-Target Pair
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ...More data for this Ligand-Target Pair
Affinity DataIC50: 7.90E+3nMAssay Description:Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to ...More data for this Ligand-Target Pair
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair