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

Data  2 KI  121 IC50  8 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 129 hits for monomerid = 92862   

TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Pfizer

LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Pfizer

LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Zuanzhu Pharma

US Patent
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
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Pfizer

LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails US Patent
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Pfizer

LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Zuanzhu Pharma

US Patent
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
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Northeastern University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Northeastern University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Northeastern University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Northeastern University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50: <10nMAssay Description:Inhibition of PI3KdeltaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Zuanzhu Pharma

US Patent
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50: <10nMAssay Description:Inhibition of PI3KalphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Northeastern University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50: <10nMAssay Description:Inhibition of PI3KbetaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Northeastern University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50: <10nMAssay Description:Inhibition of PI3KgammaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Pfizer

LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50: <10nMAssay Description:Inhibition of mTORMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Pfizer

LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Zuanzhu Pharma

US Patent
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
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Zuanzhu Pharma

US Patent
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
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Northeastern University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Northeastern University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Northeastern University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Pfizer

LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetFKBP12A/mTOR(Homo sapiens (Human))
Xi'An Jiaotong University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetSerine-protein kinase ATM(Homo sapiens (Human))
Duke University School Of Medicine

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  7nMAssay Description:Inhibition of ATM (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Pfizer

LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta(Homo sapiens (Human))
Curtin University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 3-kinase catalytic subunit type 3(Homo sapiens (Human))
Curtin University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Zuanzhu Pharma

US Patent
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
TargetPhosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha(Homo sapiens (Human))
Curtin University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Pfizer

LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Northeastern University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Northeastern University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Northeastern University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
Affinity DataIC50:  1.00E+3nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Northeastern University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Northeastern University

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Pfizer

LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Pfizer

LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM92862(US9284315, BEZ-235 | mTOR Inhibitor, BEZ235)
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
In DepthDetails ArticlePubMed
Displayed 1 to 50 (of 129 total ) | Next | Last >>