Target family: Phosphatidylinositol-4,5-bisphosphate 3-kinase family (type: enzyme)
Target: phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha

Ligand: STX-478 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.150000095367432 pKd
Reference (Journal): STX-478, a Mutant-Selective, Allosteric PI3K&#x3b1; Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3K&#x3b1;-Mutant Xenografts.
Published in: Cancer Discov

Ligand: STX-478 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.329999923706055 pKd
Reference (Journal): STX-478, a Mutant-Selective, Allosteric PI3K&#x3b1; Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3K&#x3b1;-Mutant Xenografts.
Published in: Cancer Discov

Ligand: taselisib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.539999961853027 pKi
Reference (Journal): 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.
Published in: J Med Chem

Ligand: taselisib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.050000190734863 pKi
Reference (Patent): Benzoxazepin oxazolidinone compounds and methods of use

Ligand: tenalisib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Patent): Dual selective PI3 delta and gamma kinase inhibitors

Ligand: TG-100-115 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.889999866485596 pIC50
Reference (Journal): 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.
Published in: J Med Chem

Ligand: VS-5584 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.800000190734863 pIC50
Reference (Journal): VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer.
Published in: Mol Cancer Ther

Ligand: vulolisib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pIC50
Reference (Patent): Three fused ring derivative-containing salt or crystal form and pharmaceutical composition thereof

Ligand: wortmannin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.270000457763672 pKd
Reference (Journal): Neolymphostin A Is a Covalent Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitor That Employs an Unusual Electrophilic Vinylogous Ester.
Published in: J Med Chem

Ligand: wortmannin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 pKi
Reference (Journal): Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro.
Published in: J Med Chem

Ligand: zandelisib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pIC50
Reference (Patent): (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

Ligand: ZSTK474 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.800000190734863 pIC50
Reference (Journal): Small molecules targeting phosphoinositide 3-kinases.
Published in: Medchemcomm