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

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

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma has curated GtoImmuPdb data

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1102 7q22 PIK3CG phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma
Mouse - 1102 12 B 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
p120-PI3K | PI3Kgamma | p110γ/PIK3CG | phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit gamma | phosphatidylinositol-4
Database Links
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
PDB Id:  1E8Y
Resolution:  2.0Å
Species:  Human
References:  41
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:  10
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.
Ligand:  AMG319
Resolution:  2.7Å
Species:  Human
References:  12
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
IPI549 Hs Inhibition 9.5 pKd 16
pKd 9.5 (Kd 2.9x10-10 M) [16]
CZC 24832 Hs Inhibition 7.7 pKd 6
pKd 7.7 [6]
bimiralisib Hs Inhibition 7.6 pKd
pKd 7.6 (Kd 2.5x10-8 M)
taselisib Hs Inhibition 8.8 – 9.0 pKi 7,33
pKi 9.0 (Ki 9.7x10-10 M) [33]
pKi 8.8 (Ki 1.43x10-9 M) [7]
GDC-0077 Hs Inhibition 7.7 pKi 7
pKi 7.7 (Ki 1.82x10-8 M) [7]
omipalisib Hs Inhibition 7.6 pKi 26
pKi 7.6 (Ki 2.4x10-8 M) [26]
pictilisib Hs Inhibition 7.4 pKi 7
pKi 7.4 (Ki 4.18x10-8 M) [7]
berzosertib Hs Inhibition 6.7 pKi 17
pKi 6.7 (Ki 2.2x10-7 M) [17]
compound 82 [PMID: 21332118] Hs Inhibition 8.3 pIC50 13
pIC50 8.3 (IC50 4.7x10-9 M) [13]
dactolisib Hs Inhibition 8.3 pIC50 31
pIC50 8.3 (IC50 5x10-9 M) [31]
PI 3-Kg inhibitor Hs Inhibition 8.1 pIC50 8
pIC50 8.1 (IC50 8x10-9 M) [8]
apitolisib Hs Inhibition 7.8 pIC50 40
pIC50 7.8 (IC50 1.4x10-8 M) [40]
PI-103 Hs Inhibition 7.8 pIC50 38
pIC50 7.8 (IC50 1.5x10-8 M) [38]
pilaralisib Hs Inhibition 7.6 pIC50 44
pIC50 7.6 (IC50 2.3x10-8 M) [44]
LY3023414 Hs Inhibition 7.6 pIC50 4
pIC50 7.6 (IC50 2.38x10-8 M) [4]
VS-5584 Hs Inhibition 7.6 pIC50 23
pIC50 7.6 (IC50 2.5x10-8 M) [23]
CZC 24832 Hs Inhibition 7.6 pIC50 6
pIC50 7.6 (IC50 2.7x10-8 M) [6]
duvelisib Hs Inhibition 7.6 pIC50 42
pIC50 7.6 (IC50 2.7x10-8 M) [42]
CH5132799 Hs Inhibition 7.4 pIC50 35
pIC50 7.4 (IC50 3.6x10-8 M) [35]
BGT-226 Hs Inhibition 7.4 pIC50 32
pIC50 7.4 (IC50 3.8x10-8 M) [32]
ZSTK474 Hs Inhibition 7.3 – 7.3 pIC50 44-45
pIC50 7.3 – 7.3 (IC50 5.3x10-8 – 4.9x10-8 M) [44-45]
PIK-75 Hs Inhibition 7.1 – 7.4 pIC50 24,27
pIC50 7.4 (IC50 4x10-8 M) [24]
pIC50 7.1 (IC50 7.6x10-8 M) [27]
compound 11j [PMID: 23021994] Hs Inhibition 7.2 pIC50 21
pIC50 7.2 (IC50 6x10-8 M) [21]
pictilisib Hs Inhibition 7.1 pIC50 18
pIC50 7.1 (IC50 7.5x10-8 M) [18]
TG-100-115 Hs Inhibition 7.1 pIC50 36
pIC50 7.1 (IC50 8.3x10-8 M) [36]
idelalisib Hs Inhibition 7.1 pIC50 28
pIC50 7.1 (IC50 8.9x10-8 M) [28]
AZD8835 Hs Inhibition 7.1 pIC50 5
pIC50 7.1 (IC50 9x10-8 M) [5]
INK-128 Hs Inhibition 6.7 pIC50 25
pIC50 6.7 (IC50 2.21x10-7 M) [25]
PI 3-Kg inhibitor II Hs Inhibition 6.6 pIC50 8
pIC50 6.6 (IC50 2.5x10-7 M) [8]
alpelisib Hs Inhibition 6.6 pIC50 20
pIC50 6.6 (IC50 2.5x10-7 M) [20]
seletalisib Hs Inhibition 6.6 pIC50 2
pIC50 6.6 (IC50 2.82x10-7 M) [2]
CUDC-907 Hs Inhibition 6.5 pIC50 37
pIC50 6.5 (IC50 3.11x10-7 M) [37]
dezapelisib Hs Inhibition <6.3 pIC50 29
pIC50 <6.3 (IC50 >5x10-7 M) [29]
KU-0060648 Hs Inhibition 6.2 pIC50 9
pIC50 6.2 (IC50 5.9x10-7 M) [9]
AZD8186 Hs Inhibition 6.2 pIC50 22
pIC50 6.2 (IC50 6.75x10-7 M) [22]
AMG319 Hs Inhibition 6.1 pIC50 12
pIC50 6.1 (IC50 8.5x10-7 M) [12]
STK16-IN-1 Hs Inhibition 6.1 pIC50 30
pIC50 6.1 (IC50 8.67x10-7 M) [30]
Description: In an in vitro enzymatic assay.
PP121 Hs Inhibition 6.0 pIC50 3
pIC50 6.0 (IC50 1.1x10-6 M) [3]
AZD6482 Hs Inhibition 6.0 pIC50 34
pIC50 6.0 (IC50 1.09x10-6 M) [34]
eCF309 Hs Inhibition 5.9 pIC50 19
pIC50 5.9 (IC50 1.34x10-6 M) [19]
Description: In a biochemical assay.
LY 294002 Hs Inhibition 5.5 – 5.9 pIC50 9,11
pIC50 5.5 – 5.9 (IC50 3.002x10-6 – 1.2x10-6 M) [9,11]
nemiralisib Hs Inhibition 5.2 pIC50 15
pIC50 5.2 (IC50 6.31x10-6 M) [15]
Description: In a homogeneous time-resolved fluorescence (HTRF) assay
serabelisib Hs Inhibition >5.0 pIC50 39
pIC50 >5.0 (IC50 <1x10-5 M) [39]
quinostatin Hs Inhibition 4.5 pIC50 46
pIC50 4.5 (IC50 3x10-5 M) [46]
Description: Inhibition of lipid-kinase activity in vitro.
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
Reference: 14,43

Key to terms and symbols Click column headers to sort
Target used in screen: PIK3CG
Ligand Sp. Type Action Affinity Units
TG-100-115 Hs Inhibitor Inhibition 8.3 pKd
PI-103 Hs Inhibitor Inhibition 7.8 pKd
PP-242 Hs Inhibitor Inhibition 7.4 pKd
pictilisib Hs Inhibitor Inhibition 7.3 pKd
lestaurtinib Hs Inhibitor Inhibition 6.5 pKd
staurosporine Hs Inhibitor Inhibition 5.7 pKd
GSK-461364A Hs Inhibitor Inhibition 5.7 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
The role of PIK3CG in immuno-oncology is reviewed in [1].
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 9 GO processes
GO:0002407 dendritic cell chemotaxis TAS
GO:0006954 inflammatory response TAS
GO:0010818 T cell chemotaxis TAS
GO:0030593 neutrophil chemotaxis TAS
GO:0035747 natural killer cell chemotaxis TAS
GO:0043303 mast cell degranulation TAS
GO:0045087 innate immune response TAS
GO:0072672 neutrophil extravasation TAS
click arrow to show/hide IEA associations
GO:0002675 positive regulation of acute inflammatory response IEA
Immuno Process:  T cell (activation)
GO Annotations:  Associated to 3 GO processes
GO:0002250 adaptive immune response TAS
GO:0042098 T cell proliferation TAS
GO:0042110 T cell activation TAS
Immuno Process:  B cell (activation)
GO Annotations:  Associated to 1 GO processes
GO:0002250 adaptive immune response TAS
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes
GO:0001816 cytokine production TAS
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 5 GO processes
GO:0002407 dendritic cell chemotaxis TAS
GO:0010818 T cell chemotaxis TAS
GO:0030593 neutrophil chemotaxis TAS
GO:0035747 natural killer cell chemotaxis TAS
GO:0072672 neutrophil extravasation TAS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 3 GO processes
GO:0042098 T cell proliferation TAS
GO:0042110 T cell activation TAS
GO:0043303 mast cell degranulation TAS
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0006897 endocytosis IEA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0002675 positive regulation of acute inflammatory response IEA


Show »

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19. Fraser C, Carragher NO, Unciti-Broceta A. (2016) eCF309: a potent, selective and cell-permeable mTOR inhibitor. Med. Chem. Commun.7 (3): 471-477.

20. Furet P, Guagnano V, Fairhurst RA, Imbach-Weese P, Bruce I, Knapp M, Fritsch C, Blasco F, Blanz J, Aichholz R et al.. (2013) Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. Bioorg Med Chem Lett.23 (13): 3741-8. [PMID:23726034]

21. Gopalsamy A, Bennett EM, Shi M, Zhang WG, Bard J, Yu K. (2012) Identification of pyrimidine derivatives as hSMG-1 inhibitors. Bioorg. Med. Chem. Lett.22 (21): 6636-41. [PMID:23021994]

22. Hancox U, Cosulich S, Hanson L, Trigwell C, Lenaghan C, Ellston R, Dry H, Crafter C, Barlaam B, Fitzek M et al.. (2015) Inhibition of PI3Kβ signaling with AZD8186 inhibits growth of PTEN-deficient breast and prostate tumors alone and in combination with docetaxel. Mol. Cancer Ther.14 (1): 48-58. [PMID:25398829]

23. Hart S, Novotny-Diermayr V, Goh KC, Williams M, Tan YC, Ong LC, Cheong A, Ng BK, Amalini C, Madan B et al.. (2013) VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Mol. Cancer Ther.12 (2): 151-61. [PMID:23270925]

24. Hayakawa M, Kawaguchi K, Kaizawa H, Koizumi T, Ohishi T, Yamano M, Okada M, Ohta M, Tsukamoto S, Raynaud FI et al.. (2007) Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. Bioorg. Med. Chem.15 (17): 5837-44. [PMID:17601739]

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27. Knight ZA, Gonzalez B, Feldman ME, Zunder ER, Goldenberg DD, Williams O, Loewith R, Stokoe D, Balla A, Toth B et al.. (2006) A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell125 (4): 733-47. [PMID:16647110]

28. Lannutti BJ, Meadows SA, Herman SE, Kashishian A, Steiner B, Johnson AJ, Byrd JC, Tyner JW, Loriaux MM, Deininger M et al.. (2011) CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood117 (2): 591-4. [PMID:20959606]

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30. Liu F, Wang J, Yang X, Li B, Wu H, Qi S, Chen C, Liu X, Yu K, Wang W et al.. (2016) Discovery of a Highly Selective STK16 Kinase Inhibitor. ACS Chem. Biol.11 (6): 1537-43. [PMID:27082499]

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32. Markman B, Tabernero J, Krop I, Shapiro GI, Siu L, Chen LC, Mita M, Melendez Cuero M, Stutvoet S, Birle D et al.. (2012) Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTOR inhibitor BGT226 in patients with advanced solid tumors. Ann. Oncol.23 (9): 2399-408. [PMID:22357447]

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Phosphatidylinositol kinases: phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma. Last modified on 08/02/2018. Accessed on 20/03/2018. IUPHAR/BPS Guide to PHARMACOLOGY,