Page last updated: 2024-11-13

gsk2269557

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Description

Nemiralisib: PI3K delta - selective inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID49784002
CHEMBL ID2216859
SCHEMBL ID109919
MeSH IDM000613043

Synonyms (39)

Synonym
CHEMBL2216859 ,
gsk-2269557 free base
gsk2269557a
gsk-2269557a
nemiralisib
S7937
SCHEMBL109919
2-(6-(1h-indol-4-yl)-1h-indazol-4-yl)-5-((4-isopropylpiperazin-1-yl)methyl)oxazole
MCIDWGZGWVSZMK-UHFFFAOYSA-N
6-(1h-indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1h-indazole
vvx ,
bdbm50004529
gtpl9425
compound 2 [pmid: 26301626]
2-[6-(1h-indol-4-yl)-1h-indazol-4-yl]-5-[(4-propan-2-ylpiperazin-1-yl)methyl]-1,3-oxazole
1h-indazole, 6-(1h-indol-4-yl)-4-[5-[[4-(1-methylethyl)-1-piperazinyl]methyl]-2-oxazolyl]-
1254036-71-9
OEP8JJ3OZR ,
6-(1h-indol-4-yl)-4-(5-((4-(1-methylethyl)-1-piperazinyl)methyl)-2-oxazolyl)-1h-indazole
nemiralisib [inn]
1h-indazole, 6-(1h-indol-4-yl)-4-(5-((4-(1-methylethyl)-1-piperazinyl)methyl)-2-oxazolyl)-
nemiralisib [usan]
nemiralisib [who-dd]
6-(1h-indol-4-yl)-4-(5-((4-(1-methylethyl)-1-piperazinyl)methyl)-1,3-oxazol-2-yl)-1h-indazole
gsk2269557 (free base)
CS-5683
HY-19535A
AKOS027422840
unii-oep8jj3ozr
pi3kdelta inhibitor gs2269557
Q27467143
FT-0716060
nemiralisib (usan/inn)
D11267
EX-A5754
CCG-269127
gsk2269557 free base
MS-27918
AC-35584

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Adverse events (AEs) were monitored throughout."( Safety, pharmacokinetics and dose-response characteristics of GSK2269557, an inhaled PI3Kδ inhibitor under development for the treatment of COPD.
Begg, M; Cahn, A; Dunsire, L; Fuhr, R; Galinanes-Garcia, L; Hamblin, JN; Hessel, EM; Kirsten, AM; Leemereise, CN; Montembault, M; Sriskantharajah, S; Watz, H; Wilson, R, 2017
)
0.7
" No serious adverse events were reported."( Evaluation of the Safety, Tolerability, and Pharmacokinetics of GSK2269557 (Nemiralisib) Administered Via Dry Powder Inhaler to Healthy Japanese Subjects.
Cahn, A; Igarashi, H; Ino, H; Numachi, Y; Ogura, H; Terao, T; Wilson, R, 2019
)
0.75

Pharmacokinetics

ExcerptReferenceRelevance
" In part B of the study (primary aim pharmacodynamic dose-response, N = 36 patients), GSK2269557 100, 200, 500, 700, 1000, 2000 μg or placebo was given for 14 days."( Safety, pharmacokinetics and dose-response characteristics of GSK2269557, an inhaled PI3Kδ inhibitor under development for the treatment of COPD.
Begg, M; Cahn, A; Dunsire, L; Fuhr, R; Galinanes-Garcia, L; Hamblin, JN; Hessel, EM; Kirsten, AM; Leemereise, CN; Montembault, M; Sriskantharajah, S; Watz, H; Wilson, R, 2017
)
0.92
"Physiologically based pharmacokinetic (PBPK) modelling has evolved to accommodate different routes of drug administration and enables prediction of drug concentrations in tissues as well as plasma."( Physiologically Based Pharmacokinetic Modelling of Inhaled Nemiralisib: Mechanistic Components for Pulmonary Absorption, Systemic Distribution, and Oral Absorption.
Amour, A; Edwards, CD; Graves, RH; Harrell, AW; Hessel, EM; Miller, NA; O'Brien, B; Patel, A; Robb, O; Taylor, E, 2022
)
0.72

Compound-Compound Interactions

ExcerptReferenceRelevance
" An integrated in silico, in vitro, and clinical approach including a clinical drug interaction study as well as a bespoke physiologically based pharmacokinetic (PBPK) model was used to assess the drug-drug interaction (DDI) risk."( Drug Interactions for Low-Dose Inhaled Nemiralisib: A Case Study Integrating Modeling, In Vitro, and Clinical Investigations.
Cahn, AP; Georgiou, A; Harrell, AW; Hessel, EM; Marotti, M; Patel, A; Riddell, K; Taskar, KS; Taylor, M; Tracey, H; Wilson, R, 2020
)
0.56

Dosage Studied

ExcerptRelevanceReference
" This study evaluated the safety, pharmacokinetics (PK) and dose-response characteristics of inhaled GSK2269557, a PI3Kδ inhibitor, in moderate-to-severe COPD patients with stable disease."( Safety, pharmacokinetics and dose-response characteristics of GSK2269557, an inhaled PI3Kδ inhibitor under development for the treatment of COPD.
Begg, M; Cahn, A; Dunsire, L; Fuhr, R; Galinanes-Garcia, L; Hamblin, JN; Hessel, EM; Kirsten, AM; Leemereise, CN; Montembault, M; Sriskantharajah, S; Watz, H; Wilson, R, 2017
)
0.91
" While nemiralisib had an acceptable safety profile, there was no convincing evidence of target engagement in the lung following inhaled dosing and no downstream effects observed in either the lung or blood compartments."( An open label trial of nemiralisib, an inhaled PI3 kinase delta inhibitor for the treatment of Activated PI3 kinase Delta Syndrome.
Amour, A; Beerahee, M; Begg, M; Cahn, A; Chandra, A; Clark, J; Condliffe, A; Fernando, D; Franco, SS; Hall, EB; Jarvis, E; Karkera, Y; Nejentsev, S; Okkenhaug, K; Sander, C; Singh, D; Southworth, T; Tang, T; Want, A, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)IC50 (µMol)0.10000.00010.33717.3000AID719910
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)Ki0.00010.00000.00810.0310AID1586658
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)IC50 (µMol)5.01190.00000.734010.0000AID1586655
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)IC50 (µMol)1.58490.00020.595310.0000AID1586656
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)IC50 (µMol)6.30960.00030.660710.0000AID1586657
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (118)

Processvia Protein(s)Taxonomy
phosphorylationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
natural killer cell differentiationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
positive regulation of cytokine productionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
positive regulation of endothelial cell proliferationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
adaptive immune responsePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
mast cell chemotaxisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
respiratory burst involved in defense responsePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
protein phosphorylationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
inflammatory responsePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
immune responsePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
signal transductionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
positive regulation of endothelial cell migrationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
positive regulation of gene expressionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
T cell chemotaxisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
natural killer cell activationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
B cell differentiationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
T cell differentiationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
positive regulation of cell migrationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
neutrophil chemotaxisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
positive regulation of neutrophil apoptotic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
natural killer cell chemotaxisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
B cell chemotaxisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
vascular endothelial growth factor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
T cell activationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
B cell activationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
mast cell degranulationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
innate immune responsePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
positive regulation of angiogenesisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
T cell receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
B cell receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
mast cell differentiationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
neutrophil extravasationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
positive regulation of epithelial tube formationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
cell migrationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
phosphatidylinositol-3-phosphate biosynthetic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
phosphatidylinositol-mediated signalingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
phosphorylationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
angiogenesisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
liver developmentPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
regulation of protein phosphorylationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
vasculature developmentPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
glucose metabolic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phagocytosisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
epidermal growth factor receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
insulin receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of lamellipodium assemblyPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of gene expressionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to muscle inactivityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of macroautophagyPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
actin cytoskeleton organizationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
platelet activationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of actin filament depolymerizationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
T cell costimulationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of TOR signalingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cellular response to insulin stimulusPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to muscle stretchPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
vascular endothelial growth factor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
regulation of multicellular organism growthPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to L-leucinePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
anoikisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
regulation of cellular respirationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of neuron apoptotic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
endothelial cell migrationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol phosphate biosynthetic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
insulin-like growth factor receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of smooth muscle cell proliferationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
T cell receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
relaxation of cardiac musclePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cardiac muscle contractionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
adipose tissue developmentPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cellular response to glucose stimulusPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cellular response to hydrostatic pressurePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to dexamethasonePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cardiac muscle cell contractionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
energy homeostasisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
regulation of actin filament organizationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
autosome genomic imprintingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to butyratePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of protein localization to membranePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of fibroblast apoptotic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of anoikisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol-3-phosphate biosynthetic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol-mediated signalingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cell migrationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
regulation of cell-matrix adhesionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
positive regulation of gene expressionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
phosphorylationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
positive regulation of nitric oxide biosynthetic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
endothelial cell proliferationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
response to ischemiaPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
sphingosine-1-phosphate receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
intracellular calcium ion homeostasisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
endocytosisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
autophagyPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
chemotaxisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
homophilic cell adhesion via plasma membrane adhesion moleculesPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
signal transductionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
G protein-coupled receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
positive regulation of autophagyPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
positive regulation of endothelial cell migrationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
cell migrationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
platelet activationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
positive regulation of neutrophil apoptotic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
positive regulation of Rac protein signal transductionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
embryonic cleavagePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
negative regulation of MAPK cascadePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
phosphatidylinositol phosphate biosynthetic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
angiogenesis involved in wound healingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
platelet aggregationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
negative regulation of vascular endothelial growth factor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
negative regulation of hypoxia-induced intrinsic apoptotic signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
negative regulation of sprouting angiogenesisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
regulation of clathrin-dependent endocytosisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
phosphatidylinositol-3-phosphate biosynthetic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
phosphatidylinositol-mediated signalingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
phosphorylationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
angiogenesisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
positive regulation of cytokine productionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
adaptive immune responsePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
dendritic cell chemotaxisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
positive regulation of acute inflammatory responsePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
respiratory burst involved in defense responsePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
endocytosisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
inflammatory responsePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
immune responsePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
G protein-coupled receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
positive regulation of endothelial cell migrationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
T cell chemotaxisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
negative regulation of triglyceride catabolic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
neutrophil chemotaxisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
secretory granule localizationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
regulation of cell adhesion mediated by integrinPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
positive regulation of Rac protein signal transductionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
natural killer cell chemotaxisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
T cell proliferationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
T cell activationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
mast cell degranulationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
positive regulation of MAP kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
innate immune responsePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
regulation of angiogenesisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
negative regulation of cardiac muscle contractionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
platelet aggregationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
cellular response to cAMPPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
neutrophil extravasationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
hepatocyte apoptotic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
regulation of calcium ion transmembrane transportPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
negative regulation of fibroblast apoptotic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
cell migrationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
phosphatidylinositol-mediated signalingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
phosphatidylinositol-3-phosphate biosynthetic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
protein bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
ATP bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
1-phosphatidylinositol-3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
1-phosphatidylinositol-4,5-bisphosphate 3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
1-phosphatidylinositol-4-phosphate 3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
protein serine/threonine kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
protein bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
ATP bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
1-phosphatidylinositol-3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
protein kinase activator activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
insulin receptor substrate bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
1-phosphatidylinositol-4,5-bisphosphate 3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
protein serine kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
1-phosphatidylinositol-4-phosphate 3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
protein bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
ATP bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
1-phosphatidylinositol-3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
insulin receptor substrate bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
1-phosphatidylinositol-4,5-bisphosphate 3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
protein serine kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
1-phosphatidylinositol-4-phosphate 3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
protein kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
protein serine/threonine kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
protein bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
ATP bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
1-phosphatidylinositol-3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
1-phosphatidylinositol-4-phosphate 3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
identical protein bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
ephrin receptor bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
1-phosphatidylinositol-4,5-bisphosphate 3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
protein serine kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (15)

Processvia Protein(s)Taxonomy
cytosolPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
plasma membranePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
phosphatidylinositol 3-kinase complex, class IAPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
phosphatidylinositol 3-kinase complexPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
cytoplasmPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
plasma membranePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)
cytosolPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol 3-kinase complex, class IAPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
intercalated discPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
lamellipodiumPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
perinuclear region of cytoplasmPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol 3-kinase complexPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol 3-kinase complex, class IBPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
plasma membranePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cytoplasmPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
nucleusPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
nucleoplasmPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
nucleolusPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
cytosolPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
phosphatidylinositol 3-kinase complex, class IAPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
midbodyPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
intracellular membrane-bounded organellePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
plasma membranePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
cytoplasmPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
phosphatidylinositol 3-kinase complexPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)
cytoplasmPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
cytosolPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
plasma membranePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
phosphatidylinositol 3-kinase complex, class IAPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
membranePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
phosphatidylinositol 3-kinase complex, class IBPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
plasma membranePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
cytoplasmPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (15)

Assay IDTitleYearJournalArticle
AID1586658Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by HTRF method2018Journal 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.
AID1594893Clearance in rat2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective.
AID1586656Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by HTRF method2018Journal 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.
AID1586657Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by HTRF method2018Journal 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.
AID719923Selectivity ratio of IC50 for PI3Kgamma to IC50 for PI3Kdelta2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases.
AID1586655Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by HTRF method2018Journal 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.
AID719924Selectivity ratio of IC50 for PI3Kalpha to IC50 for PI3Kdelta2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases.
AID719910Inhibition of PI3Kdelta2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases.
AID719925Selectivity ratio of IC50 for PI3Kbeta to IC50 for PI3Kdelta2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases.
AID1594894Oral bioavailability in rat2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective.
AID1345786Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma (Phosphatidylinositol kinases)2015Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18
Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease.
AID1345749Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha (Phosphatidylinositol kinases)2015Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18
Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease.
AID1345748Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta (Phosphatidylinositol kinases)2015Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18
Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease.
AID1346751Human Kv11.1 (Voltage-gated potassium channels)2015Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18
Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease.
AID1345778Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta (Phosphatidylinositol kinases)2015Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18
Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (13)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's9 (69.23)24.3611
2020's4 (30.77)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.74

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.

MetricThis Compound (vs All)
Research Demand Index16.74 (24.57)
Research Supply Index3.04 (2.92)
Research Growth Index4.60 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.74)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (53.85%)5.53%
Reviews1 (7.69%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (38.46%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]