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target has curated data in GtoImmuPdb
Target id: 2153
Nomenclature: phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
Abbreviated Name: PI3Kα
Family: Phosphatidylinositol-4,5-bisphosphate 3-kinase family, Phosphatidylinositol kinases
Gene and Protein Information  |
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| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | - | 1068 | 3q26.32 | PIK3CA | phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha | |
| Mouse | - | 1068 | 3 15.7 cM | Pik3ca | phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha | |
| Rat | - | 1068 | 2 q25 | Pik3ca | phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit alpha | |
| Previous and Unofficial Names |
| caPI3K | PI3K | PI3Kalpha | PtdIns-3-kinase subunit alpha | p110α/PIK3CA | phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit alpha | phosphatidylinositol-4 |
| Database Links |
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| Alphafold | P42336 (Hs), P42337 (Mm) |
| BRENDA | 2.7.1.153, 2.7.11.1 |
| CATH/Gene3D | 2.60.40.150, 1.10.1070.11 |
| ChEMBL Target | CHEMBL4005 (Hs), CHEMBL2499 (Mm) |
| Ensembl Gene | ENSG00000121879 (Hs), ENSMUSG00000027665 (Mm), ENSRNOG00000056371 (Rn) |
| Entrez Gene | 5290 (Hs), 18706 (Mm), 170911 (Rn) |
| Human Protein Atlas | ENSG00000121879 (Hs) |
| KEGG Enzyme | 2.7.1.153, 2.7.11.1 |
| KEGG Gene | hsa:5290 (Hs), mmu:18706 (Mm), rno:170911 (Rn) |
| OMIM | 171834 (Hs) |
| Orphanet | ORPHA117820 (Hs) |
| Pharos | P42336 (Hs) |
| RefSeq Nucleotide | NM_006218 (Hs), NM_008839 (Mm), NM_133399 (Rn) |
| RefSeq Protein | NP_006209 (Hs), NP_032865 (Mm), NP_596890 (Rn) |
| SynPHARM |
80835 (in complex with PF-04691502) 80594 (in complex with wortmannin) |
| UniProtKB | P42336 (Hs), P42337 (Mm) |
| Wikipedia | PIK3CA (Hs) |
| Selected 3D Structures |
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| Enzyme Reaction |
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Download all structure-activity data for this target as a CSV file 
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| DiscoveRx KINOMEscan® screen |
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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: 23,78 |
 
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| Target used in screen: PIK3CA | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Target used in screen: PIK3CA(C420R) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Target used in screen: PIK3CA(E542K) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Target used in screen: PIK3CA(E545A) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Target used in screen: PIK3CA(E545K) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Target used in screen: PIK3CA(H1047L) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Target used in screen: PIK3CA(H1047Y) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Target used in screen: PIK3CA(I800L) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Target used in screen: PIK3CA(M1043I) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Target used in screen: PIK3CA(Q546K) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Displaying the top 10 most potent ligands View all ligands in screen » | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Immunopharmacology Comments |
| PI3Kα is primarily recognised for its oncogenic function. We have included it in GtoImmuPdb based on its numerous GO immune process associations. |
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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.
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10. Burger MT, Pecchi S, Wagman A, Ni ZJ, Knapp M, Hendrickson T, Atallah G, Pfister K, Zhang Y, Bartulis S et al.. (2011) Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer. ACS Med Chem Lett, 2 (10): 774-9. [PMID:24900266]
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12. Canaud G. (2017) BYL719 (ALPELISIB) FOR USE IN THE TREATMENT OF PIK3CA-RELATED OVERGROWTH SPECTRUM (PROS - CLOVES SYNDROME). Patent number: WO2017140828. Assignee: INERM, CNRS, UNIVERSITÉ PARIS DESCARTES, ASSISTANCE PUBLIQUE-HÔPITAUX DE PARIS. Priority date: 17/02/2017. Publication date: 24/08/2017.
13. 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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15. 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]
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17. Cheng H, Orr STM, Bailey S, Brooun A, Chen P, Deal JG, Deng YL, Edwards MP, Gallego GM, Grodsky N et al.. (2021) Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195). J Med Chem, 64 (1): 644-661. [PMID:33356246]
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20. Cooke NG, Fernandes GDSP, Graveleau N, Hebach C, Hogenauer K, Hollingworth G, Smith AB, Soldermann N, Stowasser F, Strang R et al.. (2012) Tetrahydro-pyrido-pyrimidine derivatives. Patent number: WO2012004299. Assignee: Novartis Ag. Priority date: 06/07/2010. Publication date: 12/01/2012.
21. 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]
22. 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]
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24. 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]
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