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phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 2156

Nomenclature: phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma

Abbreviated Name: PI3Kγ

Family: Phosphatidylinositol-4,5-bisphosphate 3-kinase family, Phosphatidylinositol kinases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1102 7q22.3 PIK3CG phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma
Mouse - 1102 12 A3 Pik3cg phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma
Rat - 1102 6 q16 Pik3cg phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit gamma
Previous and Unofficial Names Click here for help
p120-PI3K | PI3Kgamma | p110γ/PIK3CG | phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit gamma | phosphatidylinositol-4
Database Links Click here for help
Alphafold P48736 (Hs), Q9JHG7 (Mm)
BRENDA 2.7.1.153
CATH/Gene3D 1.10.1070.11, 2.60.40.150
ChEMBL Target CHEMBL3267 (Hs), CHEMBL2189158 (Mm)
Ensembl Gene ENSG00000105851 (Hs), ENSMUSG00000020573 (Mm), ENSRNOG00000009385 (Rn)
Entrez Gene 5294 (Hs), 30955 (Mm), 298947 (Rn)
Human Protein Atlas ENSG00000105851 (Hs)
KEGG Enzyme 2.7.1.153
KEGG Gene hsa:5294 (Hs), mmu:30955 (Mm), rno:298947 (Rn)
OMIM 601232 (Hs)
Pharos P48736 (Hs)
RefSeq Nucleotide NM_002649 (Hs), NM_001146200 (Mm), XM_003750140 (Rn)
RefSeq Protein NP_002640 (Hs), NP_001139672 (Mm), XP_003750188 (Rn)
SynPHARM 83128 (in complex with AMG319)
80759 (in complex with apitolisib)
81104 (in complex with AZD6482)
80292 (in complex with CH5132799)
82826 (in complex with compound 82 [PMID: 21332118])
83277 (in complex with omipalisib)
80524 (in complex with PI 3-Kg inhibitor)
80528 (in complex with PI 3-Kg inhibitor II)
81100 (in complex with pictilisib)
84482 (in complex with pictilisib)
UniProtKB P48736 (Hs), Q9JHG7 (Mm)
Wikipedia PIK3CG (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  STRUCTURE DETERMINANTS OF PHOSPHOINOSITIDE 3-KINASE INHIBITION BY WORTMANNIN, LY294002, QUERCETIN, MYRICETIN AND STAUROSPORINE
PDB Id:  1E8Y
Resolution:  2.0Å
Species:  Human
References:  66
Image of receptor 3D structure from RCSB PDB
Description:  X-ray structure of phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma (PI3Kγ) in complex with the dual PI3K/mTOR inhibitor PF-04691502.
PDB Id:  3ML9
Ligand:  PF-04691502
Resolution:  2.55Å
Species:  Human
References:  13
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human PI3K-gamma in complex with (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine AMG319 inhibitor.
PDB Id:  4WWN
Ligand:  AMG319
Resolution:  2.7Å
Species:  Human
References:  16
Enzyme Reaction Click here for help
EC Number: 2.7.1.153

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
eganelisib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 9.5 pKd 20
⤷ pKd 9.5 (Kd 2.9x10-10 M) [20]
AZ2 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.6 pKd 26
⤷ pKd 8.6 (Kd 2.24x10-9 M) [26]
Description: Binding affinity determined by SPR using a two-step binding model.
neolymphostin A Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.5 pKd 12
⤷ pKd 8.5 (Kd 3.5x10-9 M) [12]
Description: Determined using an active-site dependent competition binding assay.
wortmannin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pKd 12
⤷ pKd 7.8 (Kd 1.5x10-8 M) [12]
CZC 24832 Small molecule or natural product Primary target of this compound Hs Inhibition 7.7 pKd 7
⤷ pKd 7.7 [7]
bimiralisib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.6 pKd
⤷ pKd 7.6 (Kd 2.5x10-8 M)
taselisib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.8 – 9.0 pKi 8,50
⤷ pKi 9.0 (Ki 9.7x10-10 M) [50]
pKi 8.8 (Ki 1.43x10-9 M) [8]
compound 22 [PMID: 24754609] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.7 pKi 15
⤷ pKi 8.7 (Ki 2x10-9 M) [15]
inavolisib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.7 pKi 8
⤷ pKi 7.7 (Ki 1.82x10-8 M) [8]
omipalisib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.6 pKi 38
⤷ pKi 7.6 (Ki 2.4x10-8 M) [38]
pictilisib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.4 pKi 8
⤷ pKi 7.4 (Ki 4.18x10-8 M) [8]
berzosertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.7 pKi 22
⤷ pKi 6.7 (Ki 2.2x10-7 M) [22]
AZ2 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 9.5 pIC50 26
⤷ pIC50 9.5 (IC50 3.5x10-10 M) [26]
Description: Biochemical assay using purified protein expressed from a construct containing C-terminal 6-His-tagged human p110&gamma (S144-A1102).
AZD3458 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 9.1 pIC50 54
⤷ pIC50 9.1 (IC50 7.9x10-10 M) [54]
Description: In a biochemical enzyme activity assay.
AZD8154 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 9.1 pIC50 55
⤷ pIC50 9.1 (IC50 9x10-10 M) [55]
compound 15a [PMID: 32069401] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.9 pIC50 74
⤷ pIC50 8.9 (IC50 1.2x10-9 M) [74]
compound 5d [PMID: 31335136] Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.8 pIC50 42
⤷ pIC50 8.8 (IC50 1.6x10-9 M) [42]
compound 82 [PMID: 21332118] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.3 pIC50 17
⤷ pIC50 8.3 (IC50 4.7x10-9 M) [17]
dactolisib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.3 pIC50 46
⤷ pIC50 8.3 (IC50 5x10-9 M) [46]
copanlisib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.2 pIC50 44
⤷ pIC50 8.2 (IC50 6.4x10-9 M) [44]
PI 3-Kg inhibitor Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.1 pIC50 10
⤷ pIC50 8.1 (IC50 8x10-9 M) [10]
NVP-CLR457 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.1 pIC50 21
⤷ pIC50 8.1 (IC50 8.3x10-9 M) [21]
apitolisib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pIC50 62
⤷ pIC50 7.8 (IC50 1.4x10-8 M) [62]
PI-103 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pIC50 58
⤷ pIC50 7.8 (IC50 1.5x10-8 M) [58]
bosmolisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pIC50 73
⤷ pIC50 7.8 (IC50 1.5x10-8 M) [73]
pilaralisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 pIC50 69
⤷ pIC50 7.6 (IC50 2.3x10-8 M) [69]
samotolisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 pIC50 5
⤷ pIC50 7.6 (IC50 2.38x10-8 M) [5]
tenalisib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.6 pIC50 65
⤷ pIC50 7.6 (IC50 2.385x10-8 M) [65]
Description: In a high throughput biochemical assay.
VS-5584 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.6 pIC50 30
⤷ pIC50 7.6 (IC50 2.5x10-8 M) [30]
RV1729 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.6 pIC50 37
⤷ pIC50 7.6 (IC50 2.5x10-8 M) [37]
Description: In a biochemical enzyme activity assay.
CZC 24832 Small molecule or natural product Primary target of this compound Hs Inhibition 7.6 pIC50 7
⤷ pIC50 7.6 (IC50 2.7x10-8 M) [7]
duvelisib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.6 pIC50 67
⤷ pIC50 7.6 (IC50 2.7x10-8 M) [67]
RV6153 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.6 pIC50 63
⤷ pIC50 7.6 (IC50 2.8x10-8 M) [63]
Description: In a biochemical enzyme activity assay.
AS-252424 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.5 pIC50 56
⤷ pIC50 7.5 (IC50 3.3x10-8 M) [56]
izorlisib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.4 pIC50 52
⤷ pIC50 7.4 (IC50 3.6x10-8 M) [52]
BGT-226 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.4 pIC50 47
⤷ pIC50 7.4 (IC50 3.8x10-8 M) [47]
amdizalisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 pIC50 61
⤷ pIC50 7.4 (IC50 3.8x10-8 M) [61]
ZSTK474 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.3 – 7.3 pIC50 69,71
⤷ pIC50 7.3 – 7.3 (IC50 5.3x10-8 – 4.9x10-8 M) [69,71]
AZD7648 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.3 pIC50 27
⤷ pIC50 7.3 (IC50 5.2x10-8 M) [27]
PIK-75 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.1 – 7.4 pIC50 31,39
⤷ pIC50 7.4 (IC50 4x10-8 M) [31]
pIC50 7.1 (IC50 7.6x10-8 M) [39]
compound 11j [PMID: 23021994] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pIC50 28
⤷ pIC50 7.2 (IC50 6x10-8 M) [28]
pictilisib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.1 pIC50 23
⤷ pIC50 7.1 (IC50 7.5x10-8 M) [23]
TG-100-115 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.1 pIC50 53
⤷ pIC50 7.1 (IC50 8.3x10-8 M) [53]
idelalisib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.1 pIC50 40
⤷ pIC50 7.1 (IC50 8.9x10-8 M) [40]
AZD8835 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.1 pIC50 6
⤷ pIC50 7.1 (IC50 9x10-8 M) [6]
puquitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.1 pIC50 70
⤷ pIC50 7.1 (IC50 8.98x10-8 M) [70]
vulolisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.1 pIC50 75
⤷ pIC50 7.1 (IC50 9x10-8 M) [75]
compound 27 [PMID: 35834807] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.9 pIC50 33
⤷ pIC50 6.9 (IC50 1.28x10-7 M) [33]
compound 52 [PMID: 28541707] Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.8 pIC50 45
⤷ pIC50 6.8 (IC50 1.7x10-7 M) [45]
Description: Calculated based on potency being 100-fold lower for PI3Kγ than for PI3Kδ.
panulisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.7 pIC50 35
⤷ pIC50 6.7 (IC50 2.03x10-7 M) [35]
Description: Using a radiometric protein kinase (33PanQinase activity) assay.
sapanisertib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Guide to Malaria Pharmacology Ligand Hs Inhibition 6.7 pIC50 34
⤷ pIC50 6.7 (IC50 2.21x10-7 M) [34]
PI 3-Kg inhibitor II Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.6 pIC50 10
⤷ pIC50 6.6 (IC50 2.5x10-7 M) [10]
alpelisib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.6 pIC50 25
⤷ pIC50 6.6 (IC50 2.5x10-7 M) [25]
DS-7423 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.6 pIC50 36
⤷ pIC50 6.6 (IC50 2.49x10-7 M) [36]
seletalisib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.6 pIC50 3
⤷ pIC50 6.6 (IC50 2.82x10-7 M) [3]
fimepinostat Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.5 pIC50 57
⤷ pIC50 6.5 (IC50 3.11x10-7 M) [57]
compound 41 [PMID: 31855425] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.5 pIC50 32
⤷ pIC50 6.5 (IC50 3.16x10-7 M) [32]
dezapelisib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition <6.3 pIC50 41
⤷ pIC50 <6.3 (IC50 >5x10-7 M) [41]
zandelisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition <6.3 pIC50 9
⤷ pIC50 <6.3 (IC50 >5x10-7 M) [9]
KU-0060648 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.2 pIC50 11
⤷ pIC50 6.2 (IC50 5.9x10-7 M) [11]
AZD8186 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.2 pIC50 29
⤷ pIC50 6.2 (IC50 6.75x10-7 M) [29]
AMG319 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.1 pIC50 16
⤷ pIC50 6.1 (IC50 8.5x10-7 M) [16]
STK16-IN-1 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.1 pIC50 43
⤷ pIC50 6.1 (IC50 8.67x10-7 M) [43]
Description: In an in vitro enzymatic assay.
PP121 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.0 pIC50 4
⤷ pIC50 6.0 (IC50 1.1x10-6 M) [4]
AZD6482 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.0 pIC50 51
⤷ pIC50 6.0 (IC50 1.09x10-6 M) [51]
eCF309 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.9 pIC50 24
⤷ pIC50 5.9 (IC50 1.34x10-6 M) [24]
Description: In a biochemical assay.
acalisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.9 pIC50 60
⤷ pIC50 5.9 (IC50 1.389x10-6 M) [60]
Description: In an in vitro biochemical assay using recombinant enzyme.
LY 294002 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.5 – 5.9 pIC50 11,14
⤷ pIC50 5.5 – 5.9 (IC50 3.002x10-6 – 1.2x10-6 M) [11,14]
compound 2q [PMID: 30986068] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 5.4 pIC50 48
⤷ pIC50 5.4 (IC50 3.783x10-6 M) [48]
Description: In a biochemical HTRF assay measuring generation of PIP3 via phosphorylation of PIP2, using PI3Kγ 14-558 fragment.
nemiralisib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 5.2 pIC50 19
⤷ pIC50 5.2 (IC50 6.31x10-6 M) [19]
Description: In a homogeneous time-resolved fluorescence (HTRF) assay
serabelisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition >5.0 pIC50 59
⤷ pIC50 >5.0 (IC50 <1x10-5 M) [59]
quinostatin Small molecule or natural product Click here for species-specific activity table Hs Inhibition 4.5 pIC50 72
⤷ pIC50 4.5 (IC50 3x10-5 M) [72]
Description: Inhibition of lipid-kinase activity in vitro.
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 18,68
Key to terms and symbols Click column headers to sort
Target used in screen: PIK3CG
Ligand Sp. Type Action Value Parameter
TG-100-115 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.3 pKd
PI-103 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
pictilisib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.5 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.7 pKd
GSK-461364A Small molecule or natural product Hs Inhibitor Inhibition 5.7 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
The role of PI3Kγ in immuno-oncology is reviewed in [1]. A detailed analysis of the function of PI3Kγ in malignant B cells indicated that it is crucial for chemokine gradient sensing and adhesion to stromal cells (i.e. malignant B cell migration) [2].

The PI3Kγ isoform is of particular therapeutic interest in chronic obstructive airway diseases, such as severe asthma and COPD. This Class IB PI3K isoform has regulatory roles in mediating neutrophil migration (in response to asthmatic epithelial conditioned medium [64]) and degranulation that may contribute to inflammation-mediated tissue damage of the airways [49].
Immuno Process Associations
Immuno Process:  Inflammation
Comment:  Neutrophil degranulation (GO:0043312) [49,64].
Immuno Process:  T cell (activation)
Immuno Process:  B cell (activation)
Immuno Process:  Cytokine production & signalling
Immuno Process:  Chemotaxis & migration
Immuno Process:  Cellular signalling
Comment:  Neutrophil degranulation (GO:0043312) [49,64].
Immuno Process:  Antigen presentation
Immuno Process:  Immune regulation

References

Show »

1. Adams JL, Smothers J, Srinivasan R, Hoos A. (2015) Big opportunities for small molecules in immuno-oncology. Nat Rev Drug Discov, 14 (9): 603-22. [PMID:26228631]

2. Ali AY, Wu X, Eissa N, Hou S, Ghia JE, Murooka TT, Banerji V, Johnston JB, Lin F, Gibson SB et al.. (2018) Distinct roles for phosphoinositide 3-kinases γ and δ in malignant B cell migration. Leukemia, 32 (9): 1958-1969. [PMID:29479062]

3. Allen RA, Brookings DC, Powell MJ, Delgado J, Shuttleworth LK, Merriman M, Fahy IJ, Tewari R, Silva JP, Healy LJ et al.. (2017) Seletalisib: Characterization of a Novel, Potent, and Selective Inhibitor of PI3Kδ. J Pharmacol Exp Ther, 361 (3): 429-440. [PMID:28442583]

4. Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA. (2008) Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol, 4 (11): 691-9. [PMID:18849971]

5. Barda DA, Mader MM. (2013) PI3 kinase/mTOR dual inhibitor. Patent number: US8440829 B2. Assignee: Eli Lilly And Company. Priority date: 14/01/2011. Publication date: 14/05/2013.

6. Barlaam B, Cosulich S, Delouvrié B, Ellston R, Fitzek M, Germain H, Green S, Hancox U, Harris CS, Hudson K et al.. (2015) Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers. Bioorg Med Chem Lett, 25 (22): 5155-62. [PMID:26475521]

7. Bergamini G, Bell K, Shimamura S, Werner T, Cansfield A, Müller K, Perrin J, Rau C, Ellard K, Hopf C et al.. (2012) A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation. Nat Chem Biol, 8 (6): 576-82. [PMID:22544264]

8. Braun M-G, Hanan E, Staben ST, Heald RA, Macleod C, Elliott R. (2017) Benzoxazepin oxazolidinone compounds and methods of use. Patent number: US20170015678. Assignee: Genentech, Inc.. Priority date: 02/07/2015. Publication date: 19/01/2017.

9. Brown SD, Matthews DJ. (2012) (alpha- substituted aralkylamino and heteroarylalkylamino) pyrimidinyl and 1,3,5 -triazinyl benzimidazoles, pharmaceutical compositions containing them, and these compounds for use in treating proliferative diseases. Patent number: WO2012135160A1. Assignee: Pathway Therapeutics Inc.. Priority date: 28/03/2011. Publication date: 04/10/2012.

10. Camps M, Rückle T, Ji H, Ardissone V, Rintelen F, Shaw J, Ferrandi C, Chabert C, Gillieron C, Françon B et al.. (2005) Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nat Med, 11 (9): 936-43. [PMID:16127437]

11. Cano C, Saravanan K, Bailey C, Bardos J, Curtin NJ, Frigerio M, Golding BT, Hardcastle IR, Hummersone MG, Menear KA et al.. (2013) 1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity. J Med Chem, 56 (16): 6386-401. [PMID:23855836]

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