GDC-0084 （RG7666）, is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity.

GDC-0326 is a potent and selective inhibitor of α-Isoform of Phosphoinositide 3-Kinase (PI3Kalpha inhibitor).

GDC-0941 2 MeSO3H salt is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

GDC-0941 is a potent inhibitor of PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ with IC50 of 3 nM, 33 nM, 3 nM and 75 nM, respectively.

GDC-0980 (RG7422) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM, respectively. Also a mTOR inhibitor with Ki of 17 nM, and highly selective versus others PIKK family kinases.

GNE-317 is a potent, brain-penetrant PI3K inhibitor.

GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR.

GNE-490 is a highly selective pan-PI3K inhibitor and demonstrates selectivity over mTOR.

GNE-493 is a potent, selective, and orally available dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/12/16/16/32 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ/mTOR respectively.

GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.

GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2 , respectively.

GSK-2269557 is a potent and selective PI3Kδ inhibitor over the closely related isoforms.

GSK2292767 is a potent and selective PI3Kδ inhibitor.

IC-87114 was the first isoform-selective PI3K inhibitor. p110δ(IC50 = 0.13 μM) vs. p110α(IC50 = 200 μM), p110β(IC50 = 16 μM) and p110γ(IC50 = 61 μM).

INK055 is a dual PI3Kg/d inhibitor.

IPI-145 is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities.

IPI-549 is an orally administered immuno-oncology development candidate that selectively inhibits PI3K-gamma.

Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor currently in phase II/III clinical trials for the treatment of immunodeficiency disorders.

LX-2343 is a novel non-ATP competitive PI3K inhibitor, negatively regulating AKT/mTOR signaling, thus promoting autophagy, and increasing A-beta clearance.

LY294002 is a PI3K inhibitor for p110α, p110δ and p110β with IC50 of 0.5 μM, 0.57 μM and 0.97 μM, respectively.

LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.

MTX-211 is a dual inhibitor of EGFR and PI3K, used for the treatment of cancer and other diseases.