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  141 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 167 hits for monomerid = 92862   

LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 0.00400nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 0.00500nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 0.00700nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 0.0760nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 0.450nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 0.800nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 1.40nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 1.40nMAssay Description:Inhibition of recombinant human N-terminal FLAG-tagged mTOR (1362 to end residues) using Ulight-4E-BP1 as substrate incubated for 30 mins by fluoresc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/22/2021
Entry Details Article
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
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 Depth
Date in BDB:
2/26/2013
Entry Details Article
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 1.90nMAssay Description:Displacement of Alexa Fluor labelled Tracer-314 from human N-terminal GST-tagged mTOR incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 2nMAssay Description:Inhibition of mTOR (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
TargetHistone deacetylase 6(Human)
Harbin Medical University

Curated by ChEMBL
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 2nMAssay Description:Inhibition of HDAC6 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/19/2022
Entry Details Article
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
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 Depth
Date in BDB:
7/14/2018
Entry Details Article
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 2nMAssay Description:Inhibition of DNA-PK (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
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 Depth
Date in BDB:
2/26/2013
Entry Details Article
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
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 Depth
Date in BDB:
2/21/2017
Entry Details
US Patent

LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
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 Depth
Date in BDB:
8/12/2018
Entry Details Article
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
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 Depth
Date in BDB:
4/19/2024
Entry Details
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 4nMAssay Description:Inhibition of full-length His-tagged PI3Kalpha (unknown origin) using L-alpha-phosphatidylinositolMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 4nMAssay Description:Inhibition of PI3K alpha (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 4nMAssay Description:Inhibition of C-terminal His-tagged full length P13Kalpha (unknown origin) using l-alpha-phosphatidylinositol as substrate incubated for 120 mins in ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
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 Depth
Date in BDB:
6/21/2023
Entry Details
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 4nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 4.30nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 5nMAssay Description:Inhibition of C-terminal His-tagged full length P13Kgamma (unknown origin) using l-alpha-phosphatidylinositol as substrate incubated for 120 mins in ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 5nMAssay Description:Inhibition of PI3Kgamma (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 5nMAssay Description:Inhibition of PI3Kgamma (unknown origin) expressed in baculovirus expression system using L-alpha-phosphatidylinositol as substrate by luminescence a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
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 Depth
Date in BDB:
8/12/2018
Entry Details Article
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 5nMAssay Description:Inhibition of full-length His-tagged PI3Kgamma (unknown origin) using L-alpha-phosphatidylinositolMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 5nMAssay Description:Inhibition of C-terminal His-tagged full-length PI3K p110delta (unknown origin) expressed in baculovirus incubated for 120 mins by Kinase-Glo lumines...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/19/2024
Entry Details
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
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 Depth
Date in BDB:
2/10/2015
Entry Details Article
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 5nMAssay Description:Inhibition of human PI3Kalpha using PIP2 as substrate after 1 hrMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Rat)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
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 Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 6nMAssay Description:Inhibition of human PI3Kgamma using PIP2 as substrate after 1 hrMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 6nMAssay Description:Inhibition of full-length His-tagged mTOR (unknown origin) using L-alpha-phosphatidylinositolMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 6nMAssay Description:Inhibition of mTOR (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 6nMAssay Description:Inhibition of human mTOR after 60 mins in presence of [gamma-33P]-ATP by microplate scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 6nMAssay Description:Inhibition of PI3Kbeta (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
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 Depth
Date in BDB:
10/8/2016
Entry Details Article
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
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 Depth
Date in BDB:
7/14/2018
Entry Details Article
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 7nMAssay Description:Inhibition of PI3Kdelta (unknown origin) expressed in baculovirus expression system using L-alpha-phosphatidylinositol as substrate by luminescence a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 7nMAssay Description:Inhibition of C-terminal His-tagged full length P13Kdelta (unknown origin) using l-alpha-phosphatidylinositol as substrate incubated for 120 mins in ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
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 Depth
Date in BDB:
8/12/2018
Entry Details Article
PubMed
TargetSerine-protein kinase ATM(Human)
Duke University School of Medicine

Curated by ChEMBL
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 7nMAssay Description:Inhibition of ATM (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2017
Entry Details Article
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 7nMAssay Description:Inhibition of full-length His-tagged PI3Kdelta (unknown origin) (unknown origin) using L-alpha-phosphatidylinositolMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
TargetSerine-protein kinase ATM(Human)
Duke University School of Medicine

Curated by ChEMBL
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 7nMAssay Description:Inhibition of flag tagged- ATM (unknown origin) expressed in Escherichia coli BL21 incubated for 20 mins in presence of ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
LigandPNGBDBM92862(mTOR Inhibitor, BEZ235 | US9284315, BEZ-235)
Affinity DataIC50: 7nMAssay Description:Inhibition of C-terminal His-tagged full-length PI3K p110gamma (unknown origin) expressed in baculovirus incubated for 60 mins by Kinase-Glo luminesc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/19/2024
Entry Details
PubMed
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