phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta | Phosphatidylinositol-4,5-bisphosphate 3-kinase family | IUPHAR/BPS Guide to PHARMACOLOGY

Top ▲

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

Target not currently curated in GtoImmuPdb

Target id: 2154

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

Abbreviated Name: PI3Kβ

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1070 3q21-qter PIK3CB phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta
Mouse - 1064 9 E4 Pik3cb phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta
Rat - 1070 8 q31 Pik3cb phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit beta
Previous and Unofficial Names
PI3Kbeta | PI3-kinase p110 subunit beta | PIK3C1 | phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform | ptdIns-3-kinase p110 | p110β/PIK3CB | phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit beta | phosphatidylinositol-4
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
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 Value Parameter Reference
neolymphostin A Hs Inhibition 8.2 pKd 11
pKd 8.2 (Kd 5.7x10-9 M) [11]
Description: Determined using an active-site dependent competition binding assay.
wortmannin Hs Inhibition 8.1 pKd 11
pKd 8.1 (Kd 7.6x10-9 M) [11]
bimiralisib Hs Inhibition 8.0 pKd
pKd 8.0 (Kd 1.1x10-8 M)
IPI549 Hs Inhibition 7.1 pKd 19
pKd 7.1 (Kd 8.2x10-8 M) [19]
LY 294002 Hs Inhibition 6.6 pKd 17
pKd 6.6 (Kd 2.7x10-7 M) [17]
compound 12b [PMID: 31465220] Hs Inhibition 5.1 pKd 6
pKd 5.1 (Kd 7.5x10-6 M) [6]
compound 82 [PMID: 21332118] Hs Inhibition 8.7 pKi 15
pKi 8.7 (Ki 2x10-9 M) [15]
taselisib Hs Inhibition 7.3 – 8.0 pKi 7,37
pKi 8.0 (Ki 9.1x10-9 M) [37]
pKi 7.3 (Ki 5.3x10-8 M) [7]
pictilisib Hs Inhibition 7.2 pKi 7
pKi 7.2 (Ki 7.02x10-8 M) [7]
GDC-0077 Hs Inhibition 7.0 pKi 7
pKi 7.0 (Ki 9.97x10-8 M) [7]
omipalisib Hs Inhibition 6.9 pKi 29
pKi 6.9 (Ki 1.3x10-7 M) [29]
KU-0060648 Hs Inhibition 9.3 pIC50 10
pIC50 9.3 (IC50 5x10-10 M) [10]
compound 15a [PMID: 32069401] Hs Inhibition 9.2 pIC50 55
pIC50 9.2 (IC50 5.8x10-10 M) [55]
compound 5d [PMID: 31335136] Hs Inhibition 9.1 pIC50 33
pIC50 9.1 (IC50 7x10-10 M) [33]
PI-103 Hs Inhibition 8.5 pIC50 44
pIC50 8.5 (IC50 3x10-9 M) [44]
copanlisib Hs Inhibition 8.4 pIC50 34
pIC50 8.4 (IC50 3.7x10-9 M) [34]
AZD8186 Hs Inhibition 8.4 pIC50 23
pIC50 8.4 (IC50 4x10-9 M) [23]
TGX-221 Hs Inhibition 8.3 pIC50 27
pIC50 8.3 (IC50 5x10-9 M) [27]
AZD6482 Hs Inhibition 8.0 pIC50 38
pIC50 8.0 (IC50 1x10-8 M) [38]
SAR260301 Hs Inhibition 7.6 pIC50 12
pIC50 7.6 (IC50 2.3x10-8 M) [12]
apitolisib Hs Inhibition 7.6 pIC50 47
pIC50 7.6 (IC50 2.7x10-8 M) [47]
ZSTK474 Hs Inhibition 7.4 – 7.8 pIC50 52,54
pIC50 7.4 – 7.8 (IC50 4.4x10-8 – 1.7x10-8 M) [52,54]
pictilisib Hs Inhibition 7.5 pIC50 20
pIC50 7.5 (IC50 3.3x10-8 M) [20]
fimepinostat Hs Inhibition 7.3 pIC50 43
pIC50 7.3 (IC50 5.4x10-8 M) [43]
BGT-226 Hs Inhibition 7.2 pIC50 35
pIC50 7.2 (IC50 6.3x10-8 M) [35]
VS-5584 Hs Inhibition 7.2 pIC50 24
pIC50 7.2 (IC50 6.8x10-8 M) [24]
samotolisib Hs Inhibition 7.1 pIC50 4
pIC50 7.1 (IC50 7.8x10-8 M) [4]
compound 20f [PMID: 28520415] Hs Inhibition 7.1 pIC50 42
pIC50 7.1 (IC50 7.94x10-8 M) [42]
duvelisib Hs Inhibition 7.1 pIC50 50
pIC50 7.1 (IC50 8.5x10-8 M) [50]
MEN1611 Hs Inhibition 6.9 pIC50 39
pIC50 6.9 (IC50 1.2x10-7 M) [39]
panulisib Hs Inhibition 6.8 pIC50 28
pIC50 6.8 (IC50 1.76x10-7 M) [28]
Description: Using a radiometric protein kinase (33PanQinase activity) assay.
LY 294002 Hs Inhibition 6.6 pIC50 10
pIC50 6.6 (IC50 2.7x10-7 M) [10]
PI 3-Kg inhibitor Hs Inhibition 6.6 pIC50 9
pIC50 6.6 (IC50 2.7x10-7 M) [9]
Example 51 [WO2012135160A1] Hs Inhibition 6.3 – 6.7 pIC50 8
pIC50 6.3 – 6.7 (IC50 5x10-7 – 2x10-7 M) [8]
Description: Binned value from patent.
pilaralisib Hs Inhibition 6.4 pIC50 52
pIC50 6.4 (IC50 3.83x10-7 M) [52]
AZD8835 Hs Inhibition 6.4 pIC50 5
pIC50 6.4 (IC50 4.31x10-7 M) [5]
dezapelisib Hs Inhibition <6.3 pIC50 32
pIC50 <6.3 (IC50 >5x10-7 M) [32]
idelalisib Hs Inhibition 6.3 pIC50 31
pIC50 6.3 (IC50 5.65x10-7 M) [31]
puquitinib Hs Inhibition 6.0 pIC50 53
pIC50 6.0 (IC50 9.592x10-7 M) [53]
PIK-75 Hs Inhibition 5.9 – 6.1 pIC50 25,30
pIC50 6.1 (IC50 8.5x10-7 M) [25]
pIC50 5.9 (IC50 1.3x10-6 M) [30]
PI-3065 Hs Inhibition 6.0 pIC50 1
pIC50 6.0 (IC50 1.078x10-6 M) [1]
TG-100-115 Hs Inhibition 5.9 pIC50 40
pIC50 5.9 (IC50 1.2x10-6 M) [40]
alpelisib Hs Inhibition 5.9 pIC50 21
pIC50 5.9 (IC50 1.2x10-6 M) [21]
PP121 Hs Inhibition 5.8 pIC50 3
pIC50 5.8 (IC50 1.4x10-6 M) [3]
nemiralisib Hs Inhibition 5.8 pIC50 18
pIC50 5.8 (IC50 1.584x10-6 M) [18]
Description: In a homogeneous time-resolved fluorescence (HTRF) assay
compound 41 [PMID: 31855425] Hs Inhibition 5.7 pIC50 26
pIC50 5.7 (IC50 1.995x10-6 M) [26]
seletalisib Hs Inhibition 5.7 pIC50 2
pIC50 5.7 (IC50 2.129x10-6 M) [2]
AMG319 Hs Inhibition 5.6 pIC50 14
pIC50 5.6 (IC50 2.7x10-6 M) [14]
acalisib Hs Inhibition 5.5 pIC50 46
pIC50 5.5 (IC50 3.377x10-6 M) [46]
Description: In an in vitro biochemical assay using recombinant enzyme.
tenalisib Hs Inhibition <5.4 pIC50 49
pIC50 <5.4 (IC50 >4x10-6 M) [49]
Description: In a high throughput biochemical assay.
RV6153 Hs Inhibition 5.3 pIC50 48
pIC50 5.3 (IC50 4.89x10-6 M) [48]
Description: In a biochemical enzyme activity assay.
compound 2q [PMID: 30986068] Hs Inhibition 5.3 pIC50 36
pIC50 5.3 (IC50 5.46x10-6 M) [36]
Description: In a biochemical HTRF assay measuring generation of PIP3 via phosphorylation of PIP2, using PI3Kβ 14-603 fragment.
serabelisib Hs Inhibition >5.0 pIC50 45
pIC50 >5.0 (IC50 <1x10-5 M) [45]
compound 15 [PMID: 29852070] Hs Inhibition <4.5 pIC50 41
pIC50 <4.5 (IC50 >3.16x10-5 M) [41]
Description: In a biochemical enzyme activity assay.
AZ2 Hs Inhibition 4.5 pIC50 22
pIC50 4.5 (IC50 3.162x10-5 M) [22]
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
PIK-108 Hs Negative 7.6 pIC50 13
pIC50 7.6 (IC50 2.8x10-8 M) [13]
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
Reference: 16,51

Key to terms and symbols Click column headers to sort
Target used in screen: PIK3CB
Ligand Sp. Type Action Value Parameter
PI-103 Hs Inhibitor Inhibition 8.8 pKd
pictilisib Hs Inhibitor Inhibition 7.8 pKd
TG-100-115 Hs Inhibitor Inhibition 7.1 pKd
PP-242 Hs Inhibitor Inhibition 6.9 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
GSK690693 Hs Inhibitor Inhibition <5.5 pKd
masitinib Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 2 GO processes
GO:0038096 Fc-gamma receptor signaling pathway involved in phagocytosis TAS
GO:0050900 leukocyte migration TAS
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes
GO:0019221 cytokine-mediated signaling pathway TAS
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 2 GO processes
GO:2000369 regulation of clathrin-dependent endocytosis TAS
click arrow to show/hide IEA associations
GO:0006897 endocytosis IEA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 4 GO processes
GO:0033031 positive regulation of neutrophil apoptotic process IMP
GO:0038095 Fc-epsilon receptor signaling pathway TAS
GO:0038096 Fc-gamma receptor signaling pathway involved in phagocytosis TAS
GO:0050852 T cell receptor signaling pathway TAS
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes
GO:0050900 leukocyte migration TAS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 3 GO processes
GO:0038095 Fc-epsilon receptor signaling pathway TAS
GO:0038096 Fc-gamma receptor signaling pathway involved in phagocytosis TAS
GO:0050852 T cell receptor signaling pathway TAS


Show »

1. Ali K, Soond DR, Piñeiro R, Hagemann T, Pearce W, Lim EL, Bouabe H, Scudamore CL, Hancox T, Maecker H et al.. (2014) Inactivation of PI(3)K p110δ breaks regulatory T-cell-mediated immune tolerance to cancer. Nature, 510 (7505): 407-11. [PMID:24919154]

2. 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]

3. 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]

4. 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.

5. 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]

6. Borsari C, Rageot D, Dall'Asen A, Bohnacker T, Melone A, Sele AM, Jackson E, Langlois JB, Beaufils F, Hebeisen P et al.. (2019) A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor. J. Med. Chem., 62 (18): 8609-8630. [PMID:31465220]

7. 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.

8. 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.

9. 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]

10. 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]

11. Castro-Falcón G, Seiler GS, Demir Ö, Rathinaswamy MK, Hamelin D, Hoffmann RM, Makowski SL, Letzel AC, Field SJ, Burke JE et al.. (2018) Neolymphostin A Is a Covalent Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitor That Employs an Unusual Electrophilic Vinylogous Ester. J. Med. Chem., 61 (23): 10463-10472. [PMID:30380865]

12. Certal V, Carry JC, Halley F, Virone-Oddos A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Karlsson A, Charrier V, Delorme C et al.. (2014) Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers. J. Med. Chem., 57 (3): 903-20. [PMID:24387221]

13. Certal V, Halley F, Virone-Oddos A, Delorme C, Karlsson A, Rak A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Carry JC et al.. (2012) Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers. J. Med. Chem., 55 (10): 4788-805. [PMID:22524426]

14. Cushing TD, Hao X, Shin Y, Andrews K, Brown M, Cardozo M, Chen Y, Duquette J, Fisher B, Gonzalez-Lopez de Turiso F et al.. (2015) Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease. J. Med. Chem., 58 (1): 480-511. [PMID:25469863]

15. D'Angelo ND, Kim TS, Andrews K, Booker SK, Caenepeel S, Chen K, D'Amico D, Freeman D, Jiang J, Liu L et al.. (2011) Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors. J. Med. Chem., 54 (6): 1789-811. [PMID:21332118]

16. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

17. Dittmann A, Werner T, Chung CW, Savitski MM, Fälth Savitski M, Grandi P, Hopf C, Lindon M, Neubauer G, Prinjha RK et al.. (2014) The commonly used PI3-kinase probe LY294002 is an inhibitor of BET bromodomains. ACS Chem. Biol., 9 (2): 495-502. [PMID:24533473]

18. Down K, Amour A, Baldwin IR, Cooper AW, Deakin AM, Felton LM, Guntrip SB, Hardy C, Harrison ZA, Jones KL et al.. (2015) Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease. J. Med. Chem., 58 (18): 7381-99. [PMID:26301626]

19. Evans CA, Liu T, Lescarbeau A, Nair SJ, Grenier L, Pradeilles JA, Glenadel Q, Tibbitts T, Rowley AM, DiNitto JP et al.. (2016) Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate. ACS Med Chem Lett, 7 (9): 862-7. [PMID:27660692]

20. Folkes AJ, Ahmadi K, Alderton WK, Alix S, Baker SJ, Box G, Chuckowree IS, Clarke PA, Depledge P, Eccles SA et al.. (2008) The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . J. Med. Chem., 51 (18): 5522-32. [PMID:18754654]

21. 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]

22. Gangadhara G, Dahl G, Bohnacker T, Rae R, Gunnarsson J, Blaho S, Öster L, Lindmark H, Karabelas K, Pemberton N et al.. (2019) A class of highly selective inhibitors bind to an active state of PI3Kγ. Nat. Chem. Biol., 15 (4): 348-357. [PMID:30718815]

23. 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]

24. 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]

25. 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]

26. Henley ZA, Amour A, Barton N, Bantscheff M, Bergamini G, Bertrand SM, Convery M, Down K, Dümpelfeld B, Edwards CD et al.. (2020) Optimization of Orally Bioavailable PI3Kδ Inhibitors and Identification of Vps34 as a Key Selectivity Target. J. Med. Chem., 63 (2): 638-655. DOI: 10.1021/acs.jmedchem.9b01585 [PMID:31855425]

27. Jackson SP, Schoenwaelder SM, Goncalves I, Nesbitt WS, Yap CL, Wright CE, Kenche V, Anderson KE, Dopheide SM, Yuan Y et al.. (2005) PI 3-kinase p110beta: a new target for antithrombotic therapy. Nat. Med., 11 (5): 507-14. [PMID:15834429]

28. Jalota-Badhwar A, Bhatia DR, Boreddy S, Joshi A, Venkatraman M, Desai N, Chaudhari S, Bose J, Kolla LS, Deore V et al.. (2015) P7170: A Novel Molecule with Unique Profile of mTORC1/C2 and Activin Receptor-like Kinase 1 Inhibition Leading to Antitumor and Antiangiogenic Activity. Mol. Cancer Ther., 14 (5): 1095-106. [PMID:25700704]

29. Knight SD, Adams ND, Burgess JL, Chaudhari AM, Darcy MG, Donatelli CA, Luengo JI, Newlander KA, Parrish CA, Ridgers LH et al.. (2010) Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin. ACS Med Chem Lett, 1 (1): 39-43. [PMID:24900173]

30. 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. Cell, 125 (4): 733-47. [PMID:16647110]

31. 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. Blood, 117 (2): 591-4. [PMID:20959606]

32. Li Y-L, Metcalf BW, Combs AP. (2011) Pyrimidinones as PI3K inhibitors. Patent number: WO2011008487. Assignee: Incyte Corporation. Priority date: 29/06/2009. Publication date: 20/01/2011.

33. Lin S, Jin J, Liu Y, Tian H, Zhang Y, Fu R, Zhang J, Wang M, Du T, Ji M et al.. (2019) Discovery of 4-Methylquinazoline Based PI3K Inhibitors for the Potential Treatment of Idiopathic Pulmonary Fibrosis. J. Med. Chem., 62 (19): 8873-8879. [PMID:31335136]

34. Liu N, Rowley BR, Bull CO, Schneider C, Haegebarth A, Schatz CA, Fracasso PR, Wilkie DP, Hentemann M, Wilhelm SM et al.. (2013) BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models. Mol. Cancer Ther., 12 (11): 2319-30. [PMID:24170767]

35. 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]

36. Methot JL, Zhou H, Kattar SD, McGowan MA, Wilson K, Garcia Y, Deng Y, Altman M, Fradera X, Lesburg C et al.. (2019) Structure Overhaul Affords a Potent Purine PI3Kδ Inhibitor with Improved Tolerability. J. Med. Chem., 62 (9): 4370-4382. [PMID:30986068]

37. Ndubaku CO, Heffron TP, Staben ST, Baumgardner M, Blaquiere N, Bradley E, Bull R, Do S, Dotson J, Dudley D et al.. (2013) Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity. J. Med. Chem., 56 (11): 4597-610. [PMID:23662903]

38. Nylander S, Kull B, Björkman JA, Ulvinge JC, Oakes N, Emanuelsson BM, Andersson M, Skärby T, Inghardt T, Fjellström O et al.. (2012) Human target validation of phosphoinositide 3-kinase (PI3K)β: effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kβ inhibitor. J. Thromb. Haemost., 10 (10): 2127-36. [PMID:22906130]

39. Ohwada J, Ebiike H, Kawada H, Tsukazaki M, Nakamura M, Miyazaki T, Morikami K, Yoshinari K, Yoshida M, Kondoh O et al.. (2011) Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. Bioorg. Med. Chem. Lett., 21 (6): 1767-72. [PMID:21316229]

40. Palanki MS, Dneprovskaia E, Doukas J, Fine RM, Hood J, Kang X, Lohse D, Martin M, Noronha G, Soll RM et al.. (2007) Discovery of 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction. J. Med. Chem., 50 (18): 4279-94. [PMID:17685602]

41. Pemberton N, Mogemark M, Arlbrandt S, Bold P, Cox RJ, Gardelli C, Holden NS, Karabelas K, Karlsson J, Lever S et al.. (2018) Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-γ Inhibitors. J. Med. Chem., 61 (12): 5435-5441. [PMID:29852070]

42. Perry MWD, Björhall K, Bonn B, Carlsson J, Chen Y, Eriksson A, Fredlund L, Hao H, Holden NS, Karabelas K et al.. (2017) Design and Synthesis of Soluble and Cell-Permeable PI3Kδ Inhibitors for Long-Acting Inhaled Administration. J. Med. Chem., 60 (12): 5057-5071. [PMID:28520415]

43. Qian C, Lai CJ, Bao R, Wang DG, Wang J, Xu GX, Atoyan R, Qu H, Yin L, Samson M et al.. (2012) Cancer network disruption by a single molecule inhibitor targeting both histone deacetylase activity and phosphatidylinositol 3-kinase signaling. Clin. Cancer Res., 18 (15): 4104-13. [PMID:22693356]

44. Raynaud FI, Eccles SA, Patel S, Alix S, Box G, Chuckowree I, Folkes A, Gowan S, De Haven Brandon A, Di Stefano F et al.. (2009) Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. Mol. Cancer Ther., 8 (7): 1725-38. [PMID:19584227]

45. Ren P, Liu Y, Li L, Chan K, Wilson TE, Campbell SF. (2013) Heterocyclic compounds and uses thereof. Patent number: US20130035324 A1. Assignee: Ren P, Liu Y, Li L, Chan K, Wilson TE, Campbell SF.. Priority date: 17/08/2009. Publication date: 07/02/2013.

46. Shugg RP, Thomson A, Tanabe N, Kashishian A, Steiner BH, Puri KD, Pereverzev A, Lannutti BJ, Jirik FR, Dixon SJ et al.. (2013) Effects of isoform-selective phosphatidylinositol 3-kinase inhibitors on osteoclasts: actions on cytoskeletal organization, survival, and resorption. J. Biol. Chem., 288 (49): 35346-57. [PMID:24133210]

47. Sutherlin DP, Bao L, Berry M, Castanedo G, Chuckowree I, Dotson J, Folks A, Friedman L, Goldsmith R, Gunzner J et al.. (2011) Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. J. Med. Chem., 54 (21): 7579-87. [PMID:21981714]

48. Taddei DMA, Onions ST, Smith AJ, Copmans AH, Broeckx RLM. (2016) Phosphoinositide 3-kinase inhibitors. Patent number: US9227977B2. Assignee: Respivert Ltd. Priority date: 15/03/2013. Publication date: 05/01/2016.

49. Vakkalanka SKVS, Bhavar PK, Viswanadha S, Babu G. (2017) Dual selective PI3 delta and gamma kinase inhibitors. Patent number: US9790224B2. Assignee: Rhizen Pharmaceuticals SA. Priority date: 07/06/2013. Publication date: 17/10/2017.

50. Winkler DG, Faia KL, DiNitto JP, Ali JA, White KF, Brophy EE, Pink MM, Proctor JL, Lussier J, Martin CM et al.. (2013) PI3K-δ and PI3K-γ inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem. Biol., 20 (11): 1364-74. [PMID:24211136]

51. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

52. Wu P, Hu Y. (2012) Small molecules targeting phosphoinositide 3-kinases. Medchemcomm, 3 (11): 1337-1355. DOI: 10.1039/C2MD20044A

53. Xie C, He Y, Zhen M, Wang Y, Xu Y, Lou L. (2017) Puquitinib, a novel orally available PI3Kδ inhibitor, exhibits potent antitumor efficacy against acute myeloid leukemia. Cancer Sci., 108 (7): 1476-1484. [PMID:28418085]

54. Yaguchi S, Fukui Y, Koshimizu I, Yoshimi H, Matsuno T, Gouda H, Hirono S, Yamazaki K, Yamori T. (2006) Antitumor activity of ZSTK474, a new phosphatidylinositol 3-kinase inhibitor. J. Natl. Cancer Inst., 98 (8): 545-56. [PMID:16622124]

55. Yu Y, Han Y, Zhang F, Gao Z, Zhu T, Dong S, Ma M. (2020) Design, Synthesis, and Biological Evaluation of Imidazo[1,2-a]pyridine Derivatives as Novel PI3K/mTOR Dual Inhibitors. J. Med. Chem., 63 (6): 3028-3046. [PMID:32069401]

How to cite this page

Select citation format: