Page last updated: 2024-11-13
gsk2292767
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
GSK2292767: inhibits phosphoinositide 3-kinase delta; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
ID Source | ID |
---|---|
PubMed CID | 49783923 |
CHEMBL ID | 4434674 |
SCHEMBL ID | 173490 |
MeSH ID | M000613045 |
Synonyms (29)
Synonym |
---|
S7938 |
SCHEMBL173490 |
n-[5-[4-(5-{[(2r,6s)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1h-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methanesulfonamide |
AC-32649 |
EX-A994 |
1254036-66-2 |
gsk2292767 |
n-{5-[4-(5-{[(2r,6s)-2,6-dimethylmorpholin-4-yl]methyl}-1,3-oxazol-2-yl)-1h-indazol-6-yl]-2-methoxypyridin-3-yl}methanesulfonamide |
CS-0003832 |
HY-15280 |
pi3kdelta inhibitor gs2292767 |
n-(5-(4-(5-(((2r,6s)-2,6-dimethylmorpholino)methyl)oxazol-2-yl)-1h-indazol-6-yl)-2-methoxypyridin-3-yl)methanesulfonamide |
mfcd22572737 |
c24h28n6o5s |
AKOS032945160 |
BCP24323 |
Q27464135 |
gsk-2292767 |
4M4E8NZ73C , |
methanesulfonamide, n-(5-(4-(5-(((2r,6s)-2,6-dimethyl-4-morpholinyl)methyl)-2-oxazolyl)-1h-indazol-6-yl)-2-methoxy-3-pyridinyl)-, rel- |
methanesulfonamide, n-[5-[4-[5-[[(2r,6s)-2,6-dimethyl-4-morpholinyl]methyl]-2-oxazolyl]-1h-indazol-6-yl]-2-methoxy-3-pyridinyl]-, rel- |
CCG-269791 |
n-[5-[4-[5-[[(2s,6r)-2,6-dimethylmorpholin-4-yl]methyl]-1,3-oxazol-2-yl]-1h-indazol-6-yl]-2-methoxypyridin-3-yl]methanesulfonamide |
gtpl10633 |
compound 2 [pmid: 30532965] |
compound 3 [pmid: 26301626] |
CHEMBL4434674 , |
bdbm50521218 |
unii-4m4e8nz73c |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (5)
Inhibition Measurements
Biological Processes (128)
Molecular Functions (19)
Ceullar Components (16)
Bioassays (38)
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1636696 | Clearance in human liver microsomes at 0.5 uM measured up to 30 mins by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1594891 | Inhibition of PI3K in human lung parenchyma cells assessed as reduction in IL2 secretion | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective. |
AID1894037 | Inhibition of human PI3K beta | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases. |
AID1636703 | Kinetic solubility in phosphate buffered saline at pH 7.4 after 1 hr by chemiluminescent nitrogen detection method | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1594890 | Inhibition of PI3K in human lung parenchyma cells assessed as reduction in IFNgamma secretion | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective. |
AID1636689 | Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins in presence of biotin-labeled PIP3 by HTRF assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1594892 | Antiinflammatory activity in Brown Norway rat acute OVA model of Th2 driven lung inflammation assessed as protection against eosinophil recruitment | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective. |
AID1586657 | Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by HTRF method | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase δ through a Deconstruction and Regrowth Approach. |
AID1636692 | Selectivity ratio of IC50 for PI3Kgamma (unknown origin) to IC50 for PI3Kdelta (unknown origin) | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1636702 | Binding affinity to human serum albumin by HPLC analysis | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1636688 | Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins in presence of biotin-labeled PIP3 by HTRF assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1636691 | Selectivity ratio of IC50 for PI3Kbeta (unknown origin) to IC50 for PI3Kdelta (unknown origin) | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1636687 | Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins in presence of biotin-labeled PIP3 by HTRF assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1636694 | Clearance in rat liver microsomes at 0.5 uM measured up to 30 mins by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1594886 | Inhibition of PI3Kbeta (unknown origin) | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective. |
AID1586656 | Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by HTRF method | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase δ through a Deconstruction and Regrowth Approach. |
AID1594889 | Inhibition of PI3K in human PBMC assessed as reduction in IFNgamma secretion | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective. |
AID1586655 | Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by HTRF method | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase δ through a Deconstruction and Regrowth Approach. |
AID1594881 | Inhibition of PI3Kalpha (unknown origin) | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective. |
AID1589131 | Selectivity index, ratio of IC50 for PI3KD (unknown origin) to IC50 for PI3KG (unknown origin) | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Design of selective PI3Kδ inhibitors using an iterative scaffold-hopping workflow. |
AID1594882 | Inhibition of PI3Kdelta (unknown origin) | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective. |
AID1636699 | Clearance in Sprague-Dawley rat at 1 mg/kg, iv measured up to 7 hrs by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1894036 | Inhibition of human PI3K alpha | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases. |
AID1594887 | Inhibition of PI3Kgamma (unknown origin) | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective. |
AID1636693 | Inhibition of PI3Kdelta in human PBMC assessed as reduction in cytostim-induced IFNgamma production after 20 hrs by electrochemiluminescence assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1636705 | Apparent passive permeability in MDCK2-MDR1 cells at 3 mM in presence of P-gp inhibitor | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1586658 | Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by HTRF method | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase δ through a Deconstruction and Regrowth Approach. |
AID1894035 | Inhibition of recombinant human full length P13Kdelta expressed in Sf9 cells assessed as reduction in ATP-dependent phosphorylation by chromatography method | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases. |
AID1636704 | Cmax in Sprague-Dawley rat at 3 mg/kg, po measured up to 7 hrs by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1636697 | AUC(infinity) in Sprague-Dawley rat at 3 mg/kg, po measured up to 7 hrs by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1636695 | Clearance in mouse liver microsomes at 0.5 uM measured up to 30 mins by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1636698 | Half life in Sprague-Dawley rat at 1 mg/kg, iv by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1636690 | Selectivity ratio of IC50 for PI3Kalpha (unknown origin) to IC50 for PI3Kdelta (unknown origin) | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1636707 | Lipophilicity, log D of compound at pH 7.4 by chromatographic method | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1894038 | Inhibition of human PI3Kgamma | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases. |
AID1636700 | Oral bioavailability in Sprague-Dawley rat at 3 mg/kg measured up to 7 hrs by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
AID1589128 | Inhibition of PI3KD (unknown origin) by HTRF assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Design of selective PI3Kδ inhibitors using an iterative scaffold-hopping workflow. |
AID1636701 | Volume of distribution at steady state in Sprague-Dawley rat at 3 mg/kg, po or 1 mg/kg, iv measured up to 7 hrs by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Research
Studies (7)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 6 (85.71) | 24.3611 |
2020's | 1 (14.29) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Market Indicators
Research Demand Index: 17.55
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (17.55) All Compounds (24.57) |
Study Types
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 1 (14.29%) | 5.53% |
Reviews | 1 (14.29%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 5 (71.43%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |