Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T80276 Target Info
Target Name PI3-kinase alpha (PIK3CA)
Synonyms
p110alpha; Serine/threonine protein kinase PIK3CA; PtdIns3kinase subunit p110alpha; PtdIns3kinase subunit alpha; PtdIns-3-kinase subunit p110-alpha; PtdIns-3-kinase subunit alpha; Phosphoinositide3kinase catalytic alpha polypeptide; Phosphoinositide-3-kinase catalytic alpha polypeptide; Phosphatidylinositol 4,5bisphosphate 3kinase catalytic subunit alpha isoform; Phosphatidylinositol 4,5bisphosphate 3kinase 110 kDa catalytic subunit alpha; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha; PI3kinase subunit alpha; PI3Kalpha; PI3K-alpha; PI3-kinase subunit alpha
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Target Type Successful Target
Gene Name PIK3CA
Biochemical Class Kinase
UniProt ID
PK3CA_HUMAN
Co-Targets of This Target  Top
Co-Target Name PI3-kinase delta (PIK3CD) Successful Target
UniProt ID PK3CD_HUMAN
Gene Name PIK3CD
Synonyms
PtdIns-3-kinase subunit p110-delta; PtdIns-3-kinase subunit delta; Phosphoinositide 3-kinase delta; Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit, delta isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit delta; PI3Kdelta; PI3K-delta; PI3-kinase subunit delta; PI3-kinase p110 subunit delta; P110delta
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Representative Drug(s) GDC-0032 Drug Info Ki = 0.12 nM Click to Show More [1]
2 BAY 80-6946 Drug Info IC50 < 0.7 nM [2]
3 Buparlisib Drug Info IC50 = 110 nM [6]
4 Alpelisib Drug Info IC50 = 290 nM [7]
5 PA-799 Drug Info IC50 = 500 nM [4]
Co-Target Name PI3-kinase gamma (PIK3CG) Successful Target
UniProt ID PK3CG_HUMAN
Gene Name PIK3CG
Synonyms
p120-PI3K; p110gamma; Serine/threonine protein kinase PIK3CG; PtdIns-3-kinase subunit p110-gamma; PtdIns-3-kinase subunit gamma; PtdIns-3-kinase p110; Phosphoinositol-3 kinase; Phosphoinositide-3-kinase catalytic gamma polypeptide; Phosphoinositide 3-Kinase gamma; Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit, gamma isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit gamma; PI3Kgamma; PI3K-gamma; PI3K; PI3-kinase subunit gamma; PI3-kinase p110 subunit gamma
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Representative Drug(s) BAY 80-6946 Drug Info IC50 = 0.7 nM Click to Show More [3]
2 GDC-0032 Drug Info Ki = 0.97 nM [1]
3 PA-799 Drug Info IC50 = 36 nM [4]
4 Alpelisib Drug Info IC50 = 250 nM [7]
5 Buparlisib Drug Info IC50 = 256 nM [3]
Co-Target Name Serine/threonine-protein kinase mTOR (mTOR) Successful Target
UniProt ID MTOR_HUMAN
Gene Name MTOR
Synonyms
Target of rapamycin; TOR kinase; Rapamycin target protein 1; Rapamycin target protein; Rapamycin and FKBP12 target 1; RAPT1; RAFT1; Mechanistic target of rapamycin; Mammalian target of rapamycin; FRAP2; FRAP1; FRAP; FKBP12-rapamycin complex-associated protein; FKBP-rapamycin associated protein; FK506-binding protein 12-rapamycin complex-associated protein 1
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Representative Drug(s) BAY 80-6946 Drug Info IC50 = 45 nM Click to Show More [5]
2 Buparlisib Drug Info IC50 = 94 nM [6]
Co-Target Name PI3-kinase beta (PIK3CB) Clinical trial Target
UniProt ID PK3CB_HUMAN
Gene Name PIK3CB
Synonyms
p110beta; PtdIns3kinase subunit p110beta; PtdIns3kinase subunit beta; PtdIns-3-kinase subunit p110-beta; PtdIns-3-kinase subunit beta; Phosphatidylinositol 4,5bisphosphate 3kinase catalytic subunitbeta isoform; Phosphatidylinositol 4,5bisphosphate 3kinase 110 kDa catalyticsubunit beta; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit beta; PIK3C1; PI3kinase subunit beta; PI3Kbeta; PI3K-beta; PI3-kinase subunit beta
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Representative Drug(s) BAY 80-6946 Drug Info IC50 = 3.7 nM Click to Show More [3]
2 GDC-0032 Drug Info Ki = 9.1 nM [1]
3 PA-799 Drug Info IC50 = 120 nM [8]
4 Buparlisib Drug Info IC50 = 165.96 nM [9]
Co-Target Name PI3K p110 delta/p85 alpha (PIK3CD/PIK3R1) Co-Target
UniProt ID PK3CD_HUMAN-P85A_HUMAN
Gene Name PIK3CD-PIK3R1
Representative Drug(s) BAY 80-6946 Drug Info IC50 = 0.18 nM Click to Show More [10]
2 Buparlisib Drug Info IC50 = 125 nM [11]
Co-Target Name PI3K p110 beta/p85 alpha (PIK3CB/PIK3R1) Co-Target
UniProt ID PK3CB_HUMAN-P85A_HUMAN
Gene Name PIK3CB-PIK3R1
Representative Drug(s) BAY 80-6946 Drug Info IC50 = 4.57 nM Click to Show More [10]
2 Buparlisib Drug Info IC50 = 234 nM [11]
Co-Target Name PI3K-gamma/PI3K regulatory subunit 5 (PIK3CG-PIK3R5) Co-Target
UniProt ID PK3CG_HUMAN-PI3R5_HUMAN
Gene Name PIK3CG-PIK3R5
Representative Drug(s) Buparlisib Drug Info IC50 = 129 nM [12]
Co-Target Name Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta (PIK3C2B) Co-Target
UniProt ID P3C2B_HUMAN
Gene Name PIK3C2B
Synonyms
PI3K-C2-beta; PtdIns-3-kinase C2 subunit beta; C2-PI3K; Phosphoinositide 3-kinase-C2-beta
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Representative Drug(s) GDC-0032 Drug Info IC50 = 292 nM [1]
Co-Target Name Phosphatidylinositol 3-kinase catalytic subunit type 3 (PIK3C3) Co-Target
UniProt ID PK3C3_HUMAN
Gene Name PIK3C3
Synonyms
PI3-kinase type 3; PI3K type 3; PtdIns-3-kinase type 3; Phosphatidylinositol 3-kinase p100 subunit; Phosphoinositide-3-kinase class 3; hVps34
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Representative Drug(s) GDC-0032 Drug Info IC50 = 374 nM [1]
References  Top
REF 1 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 beta-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity. J Med Chem. 2013 Jun 13;56(11):4597-610.
REF 2 Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168). ACS Med Chem Lett. 2017 Jul 24;8(8):808-13.
REF 3 Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer. Eur J Med Chem. 2019 Dec 1;183:111718.
REF 4 Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1767-72.
REF 5 Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective. J Med Chem. 2019 May 23;62(10):4815-4850.
REF 6 5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology. J Med Chem. 2017 Sep 14;60(17):7524-7538.
REF 7 Discovery of a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Kalpha inhibitor with high PI3K isoform selectivity and potent cellular activity. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3582-4.
REF 8 Small molecules targeting phosphoinositide 3-kinases. Medchemcomm. 2012;3:1337-55.
REF 9 Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy. J Med Chem. 2020 Jan 9;63(1):122-139.
REF 10 Design, Synthesis, and Biological Evaluation of Imidazo[1,2- a]pyridine Derivatives as Novel PI3K/mTOR Dual Inhibitors. J Med Chem. 2020 Mar 26;63(6):3028-3046.
REF 11 Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines. ACS Med Chem Lett. 2018 Jun 25;9(7):719-724.
REF 12 Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. J Med Chem. 2016 Aug 11;59(15):7268-74.

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