Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T05031 Target Info
Target Name PI3-kinase beta (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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Target Type Clinical trial Target
Gene Name PIK3CB
Biochemical Class Kinase
UniProt ID
PK3CB_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) AZD8186 Drug Info IC50 = 12 nM Click to Show More [1]
2 Buparlisib Drug Info IC50 = 110 nM [7]
3 PQR309 Drug Info IC50 = 451 nM [7]
4 PA-799 Drug Info IC50 = 500 nM [6]
Co-Target Name PI3-kinase alpha (PIK3CA) Successful Target
UniProt ID PK3CA_HUMAN
Gene Name 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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Representative Drug(s) PA-799 Drug Info IC50 = 14 nM Click to Show More [2]
2 Drug Info IC50 = 15 nM [3]
3 PQR309 Drug Info Ki = 17 nM [4]
4 Buparlisib Drug Info IC50 = 20 nM [5]
5 AZD8186 Drug Info IC50 = 35 nM [1]
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) PA-799 Drug Info IC50 = 36 nM Click to Show More [6]
2 Buparlisib Drug Info IC50 = 256 nM [8]
3 AZD8186 Drug Info IC50 = 675 nM [1]
4 PQR309 Drug Info IC50 = 708 nM [7]
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) PQR309 Drug Info Ki = 62 nM Click to Show More [4]
2 Buparlisib Drug Info IC50 = 94 nM [7]
Co-Target Name Mammalian target of rapamycin complex 1 (mTORC1) Clinical trial Target
UniProt ID MTOR_HUMAN-RPTOR_HUMAN-LST8_HUMAN-AKTS1_HUMAN-DPTOR_HUMAN
Gene Name MTOR-RPTORA-MLST8-KT1S1-DEPTOR
Synonyms
mTORC1; Mechanistic target of rapamycin complex 1
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Representative Drug(s) PQR309 Drug Info IC50 = 205 nM [9]
Co-Target Name PI3K p110 alpha/p85 alpha (PIK3CA/PIK3R1) Co-Target
UniProt ID PK3CA_HUMAN-P85A_HUMAN
Gene Name PIK3CA-PIK3R1
Representative Drug(s) Buparlisib Drug Info IC50 = 11 nM Click to Show More [10]
2 PQR309 Drug Info Ki = 17 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) Buparlisib Drug Info IC50 = 125 nM [10]
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 [11]
Co-Target Name mTORC2 Co-Target
UniProt ID MTOR_HUMAN; RICTR_HUMAN; SIN1_HUMAN; LST8_HUMAN
Gene Name MTOR; RICTOR; MAPKAP1; MLST8
Synonyms
mTOR Complex 2; Mechanistic target of Rapamycin 2
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Representative Drug(s) PQR309 Drug Info IC50 = 139 nM [9]
References  Top
REF 1 Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): a potent and selective inhibitor of PI3Kbeta and PI3Kdelta for the treatment of PTEN-deficient cancers. J Med Chem. 2015 Jan 22;58(2):943-62.
REF 2 Small molecules targeting phosphoinositide 3-kinases. Medchemcomm. 2012;3:1337-55.
REF 3 6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors. Eur J Med Chem. 2016 Oct 21;122:731-743.
REF 4 (S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase. J Med Chem. 2019 Jul 11;62(13):6241-6261.
REF 5 Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases. J Med Chem. 2019 Aug 8;62(15):6992-7014.
REF 6 Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1767-72.
REF 7 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 8 Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer. Eur J Med Chem. 2019 Dec 1;183:111718.
REF 9 A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor. J Med Chem. 2019 Sep 26;62(18):8609-8630.
REF 10 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 11 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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