BDBM50145416 GSK2126458::Omipalisib

SMILES COc1ncc(cc1NS(=O)(=O)c1ccc(F)cc1F)-c1ccc2nccc(-c3ccnnc3)c2c1

InChI Key InChIKey=CGBJSGAELGCMKE-UHFFFAOYSA-N

Data  9 KI  29 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 73 hits for monomerid = 50145416   

LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.00100nMAssay Description:Inhibition of p110 alpha (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.00100nMAssay Description:Inhibition of p110 delta (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.00100nMAssay Description:Inhibition of p110 beta (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.00100nMAssay Description:Inhibition of p110 gamma (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.00800nMAssay Description:Binding affinity to p110 alpha E545K mutant (unknown origin) assessed as inhibition constant in presence of ATP by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.00800nMAssay Description:Binding affinity to p110 alpha E542K mutant (unknown origin) assessed as inhibition constant in presence of ATP by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.00900nMAssay Description:Binding affinity to p110 alpha H1047R mutant (unknown origin) assessed as inhibition constant in presence of ATP by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.0190nMAssay Description:Inhibition of PI3K alpha (unknown origin) by PIP3 production detection based fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.0190nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.0190nMAssay Description:Binding affinity to p110 alpha (unknown origin) assessed as inhibition constant in presence of ATP by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.0190nMAssay 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
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.0200nMAssay Description:Inhibition of P13Kalpha (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.0200nMAssay Description:Inhibition of P13Kbeta (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.0200nMAssay Description:Inhibition of P13Kdelta (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.0240nMAssay Description:Binding affinity to p110 delta (unknown origin) assessed as inhibition constant in presence of ATP by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.0240nMAssay Description:Inhibition of PI3Kgamma (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataEC50:  0.0400nMAssay Description:Inhibition of PI3K alpha (unknown origin) by PIP3 production detection based fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.0400nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr in p...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.0400nMAssay Description:Inhibition of PI3Kalpha (unknown origin) by kinase profiling assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.0600nMAssay Description:Inhibition of human p110alpha/p85alpha using PIP2 as substrate in presence of ATP measured by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/20/2022
Entry Details Article
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.0600nMAssay Description:Binding affinity to p110 gamma (unknown origin) assessed as inhibition constant in presence of ATP by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.0600nMAssay Description:Inhibition of PI3Kdelta (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.0600nMAssay Description:Inhibition of PI3K gamma (unknown origin) by PIP3 production detection based fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.0700nMAssay Description:Inhibition of human p110delta/p85alpha using PIP2 as substrate in presence of ATP measured by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/20/2022
Entry Details Article
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.130nMAssay Description:Inhibition of PI3K beta (unknown origin) by PIP3 production detection based fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.130nMAssay Description:Binding affinity to p110 beta (unknown origin) assessed as inhibition constant in presence of ATP by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.130nMAssay Description:Inhibition of PI3Kbeta (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.130nMAssay Description:Inhibition of human PI3Kbeta assessed as reduction in PIP3 product complex formationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetTarget of rapamycin complex subunit LST8(Human)
Sichuan University

Curated by ChEMBL
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.180nMAssay Description:Binding affinity to mTORC1 (unknown origin) assessed as apparent inhibition constant in presence of ATP by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetSerine/threonine-protein kinase mTOR(Human)
Temple University

Curated by ChEMBL
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.180nMAssay Description:Competitive inhibition of human mTOR using 4EBP1 as substrate in presence of [33gammaP]-ATP after 120 mins by filter binding methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/17/2019
Entry Details Article
PubMed
TargetTarget of rapamycin complex subunit LST8(Human)
Sichuan University

Curated by ChEMBL
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.180nMAssay Description:Binding affinity to mTORC1 (unknown origin) assessed as apparent inhibition constant in presence of ATP by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetTarget of rapamycin complex subunit LST8(Human)
Sichuan University

Curated by ChEMBL
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.180nMAssay Description:Inhibition of mTORC1 (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
TargetTarget of rapamycin complex 2 subunit MAPKAP1(Human)
Bioland Laboratory (Guangzhou Regenerative Medicine and Health - Guangdong Laboratory)

Curated by ChEMBL
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.180nMAssay Description:Inhibition of mTORC2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.190nMAssay Description:Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate measured after 1 hr by ADP-glo assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetDNA-dependent protein kinase catalytic subunit(Human)
GlaxoSmithKline

Curated by ChEMBL
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.280nMAssay Description:Inhibition of DNA-PK (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetSerine/threonine-protein kinase mTOR(Human)
Temple University

Curated by ChEMBL
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.300nMAssay 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
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of recombinant human PI3Kalpha using PIP2 as substrate incubated for 1 hr by kinase-glo luminescent assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetTarget of rapamycin complex 2 subunit MAPKAP1(Human)
Bioland Laboratory (Guangzhou Regenerative Medicine and Health - Guangdong Laboratory)

Curated by ChEMBL
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.300nMAssay Description:Binding affinity to mTORC2 (unknown origin) assessed as apparent inhibition constant in presence of ATP by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetTarget of rapamycin complex 2 subunit MAPKAP1(Human)
Bioland Laboratory (Guangzhou Regenerative Medicine and Health - Guangdong Laboratory)

Curated by ChEMBL
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.300nMAssay Description:Inhibition of mTORC2 (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
TargetTarget of rapamycin complex 2 subunit MAPKAP1(Human)
Bioland Laboratory (Guangzhou Regenerative Medicine and Health - Guangdong Laboratory)

Curated by ChEMBL
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.300nMAssay Description:Binding affinity to mTORC2 (unknown origin) assessed as apparent inhibition constant in presence of ATP by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetSerine/threonine-protein kinase mTOR(Human)
Temple University

Curated by ChEMBL
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.310nMAssay Description:Inhibition of mTOR (unknown origin) using ULight-4E-BP1 peptide as substrate after 1 hr in presence of ATP by lance ultra assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/4/2018
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase mTOR(Human)
Temple University

Curated by ChEMBL
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.340nMAssay Description:Inhibition of recombinant human N-terminal FLAG-tagged mTOR (1362 to end amino acids) using ULight-4E-BP1 as substrate incubated for 1 hr by LANCE Ul...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.340nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using lipid as substrate incubated for 15 mins followed by substrate addition and measured after 60 mins ADP...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.440nMAssay Description:Inhibition of recombinant human full-length His-tagged PI3Kgamma expressed in baculovirus expression system using PIP2 as substrate measured after 1 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.510nMAssay Description:Inhibition of human p110gamma using PIP2 as substrate in presence of ATP measured by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/20/2022
Entry Details Article
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataKi:  0.530nMAssay Description:Inhibition of human p110beta/p85alpha using PIP2 as substrate in presence of ATP measured by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/20/2022
Entry Details Article
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.550nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 30 mins by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of PI3K-gamma (unknown origin) after 40 mins by ADP-Glo luminescent kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/14/2017
Entry Details Article
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.610nMAssay Description:Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate after 1 hr in presence of ATP by ADP-glo based luminescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/4/2018
Entry Details Article
PubMed
LigandPNGBDBM50145416(GSK2126458 | Omipalisib)
Affinity DataIC50: 0.630nMAssay 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
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