BDBM25045 3-(4-morpholin-4-ylpyrido[2,3]furo[2,4-b]pyrimidin-2-yl)phenol::3-(4-morpholin-4-ylpyrido[3 ,2 :4,5]furo[3,2-d]pyrimidin-2-yl)phenol::3-(4-morpholinopyrido[2,3]furo[2,4-b]pyrimidin-2-yl)phenol::3-[4-(4-morpholinyl)-2-pyrido[2,3]furo[2,4-b]pyrimidinyl]phenol::3-[6-(morpholin-4-yl)-8-oxa-3,5,10-triazatricyclo[7.4.0.0^{2,7}]trideca-1(9),2,4,6,10,12-hexaen-4-yl]phenol::CHEMBL538346::PI-103::US9637488, PI-103::cid_9884685::mTOR Inhibitor, PI103::pyridofuropyrimidine derivative, 2

SMILES Oc1cccc(c1)-c1nc(N2CCOCC2)c2oc3ncccc3c2n1

InChI Key InChIKey=TUVCWJQQGGETHL-UHFFFAOYSA-N

Data  2 KI  125 IC50  770 Kd

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 895 hits for monomerid = 25045   

LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataKd:  1.30nMAssay Description:Binding constant for PIK3CA(C420R) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataKd:  1.40nMAssay Description:Binding constant for PIK3CA(E542K) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataKd:  1.5nMAssay Description:Binding constant for PIK3CA kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataKd:  1.5nMAssay Description:Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2011
Entry Details
PCBioAssay
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataKd:  1.5nMAssay Description:Binding constant for PIK3CA(E545K) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataKd:  1.5nMAssay Description:Binding constant for PIK3CA kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/25/2012
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataKd:  1.5nMAssay Description:Binding constant for PIK3CA(E545A) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataKd:  1.5nMAssay Description:Binding constant for PIK3CA kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/25/2012
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataKd:  1.5nMAssay Description:Binding constant for PIK3CA(Q546K) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataKd:  1.70nMAssay Description:Binding constant for PIK3CB kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 1.76nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2020
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 2nMAssay Description:Inhibition of human PI3K p110alpha/p85alpha using PIP2 as substrate incubated for 10 mins followed by ATP addition and measured after 30 mins in pres...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2022
Entry Details Article
PubMed
TargetDNA-dependent protein kinase catalytic subunit(Human)
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 2nMAssay Description:Inhibition of human DNA-PK by non-radiometric ADP-Glo assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/19/2016
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 2nMAssay Description:Inhibition of P13Kalpha (unknown origin) in the presence of ATP by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 2nMAssay Description:Competitive inhibition of human PI3K p110alpha/p85alpha using PIP2 as substrate preincubated for 10 mins followed by ATP addition measured after 30 m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/17/2019
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 2.5nMAssay Description:Exemplary compounds of the invention were tested their inhibitory activity or potency against PI3Kδ in 10-dose IC50 mode with 3-fold serial dilu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/29/2019
Entry Details
Go to US Patent

LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataKd:  2.90nMAssay Description:Binding constant for PIK3CA(I800L) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataKd:  3nMAssay Description:Binding constant for PIK3CA(M1043I) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 3nMpH: 7.4 T: 2°CAssay Description:The test compounds and enzyme were mixed in buffer, and the substrate and [gamma-33P] ATP/ATP were added to the mixture to initiate the reaction. Aft...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/26/2008
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 3nMAssay Description:Inhibition of p110betaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/10/2012
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 3nMAssay Description:Inhibition of P13Kdelta (unknown origin) in the presence of ATP by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 3nMAssay Description:Inhibition of P13Kbeta (unknown origin) in the presence of ATP by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 3nMAssay Description:Inhibition of PI3K delta (unknown origin) using PIP2 as substrate after 1 hr by kinase-Glo luminescent assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2017
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 3nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 3nMAssay Description:Inhibition of human PI3Kdelta assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 3nMAssay Description:Inhibition of human recombinant PI3K delta by scintillation proximity radiometric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2017
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 3.20nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2022
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataKd:  3.20nMAssay Description:Binding constant for PIK3CA(H1047L) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataKd:  3.40nMAssay Description:Binding constant for PIK3CA(H1047Y) kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 3.60nMAssay Description:Inhibition of p110alpha by SPA assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/10/2012
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 3.60nMpH: 7.4 T: 2°CAssay Description:The test compounds and enzyme were mixed in buffer, and the substrate and [gamma-33P] ATP/ATP were added to the mixture to initiate the reaction. Aft...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/26/2008
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 3.80nMAssay Description:Inhibition of human PI3Kalpha incubated for 1 hr by ADP-Glo kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 3.82nMAssay Description:Inhibition of PI3Kbeta (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2020
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 3.90nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate in presence of ATP measured after 1 hr by ADP-Glo assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 4nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 4nMAssay Description:Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate in presence of ATP measured after 60 mins by ADP-Glo assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/24/2022
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 4nMAssay Description:Inhibition of human PI3Kalpha assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 4nMAssay Description:Inhibition of PI3Kdelta (unknown origin) in presence of [33P]-ATP incubated for 2 hrs by hotspot kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 4.40nMAssay Description:Inhibition of recombinant human full-length N-terminal His-tagged p110alpha/p85alpha expressed in baculovirus expression system using PIP2 as substra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 4.40nMAssay Description:Inhibition of PI3KalphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 4.5nMAssay Description:Inhibition of PI3Kalpha by HTRF assay in presence of ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 5nMAssay Description:Inhibition of PI3Kbeta (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetSerine/threonine-protein kinase mTOR(Human)
West China Hospital of Sichuan University

Curated by ChEMBL
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 5.30nMAssay 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
TargetSerine/threonine-protein kinase mTOR(Human)
West China Hospital of Sichuan University

Curated by ChEMBL
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 5.30nMAssay Description:Inhibition of mTOR kinase (unknown origin) assessed as suppression of ULight-4E-BP1 substrate phosphorylation incubated for 1 hr by lance ultra assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/14/2017
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 5.80nMAssay Description:Inhibition of human recombinant PI3K alpha by scintillation proximity radiometric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2017
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 5.80nMAssay Description:Inhibition of PI3K alpha (unknown origin) using PIP2 as substrate after 1 hr by kinase-Glo luminescent assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2017
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 6nMAssay Description:Inhibition of human PI3Kalpha using ATP as substrate at 25 uM incubated for 60 mins by ADP-glo based luminescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/20/2022
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 6.10nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate after 1 hr in presence of ATP by kinase-glo luminescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/4/2018
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 6.5nMAssay Description:Inhibition of PI3Kdelta (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2022
Entry Details Article
PubMed
LigandPNGBDBM25045(CHEMBL538346 | mTOR Inhibitor, PI103 | PI-103 | 3-...)
Affinity DataIC50: 6.80nMAssay Description:Inhibition of PI3Kbeta (unknown origin) in presence of [33P]-ATP incubated for 2 hrs by hotspot kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
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