GSK2879552 is an orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.

GSK2801 is a very potent inhibitor of the BAZ2 family of bromodomain containing proteins.

GSK269962A(GSK269962) is a potent ROCK inhibitor (IC50 values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively); displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases.

GSK2656157 is an ATP-competitive inhibitor of PERK enzyme activity with an IC50 of 0.9 nM. It is highly selective for PERK with IC50 values >100 nM against a panel of 300 kinases.

GSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. Phase 1/2a.

GSK2606414 is an orally available, potent, and selective PERK inhibitor with an IC50 of 0.4 nM.

GSK2578215A is a potent and highly selective LRRK2 inhibitor; exhibits IC50s of around 10 nM against both wild-type LRRK2 and the G2019S mutant.

GSK2256098 is small molecule FAK kinase inhibitor.

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.

GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively.

GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.

GSK-137647 is a potent and selective FFA4 (GPR120) agonist (pEC50 values are 6.3, 6.2 and 6.1 at the human, mouse and rat receptor, respectively). Exhibits ≥100-fold selectivity against a panel of 61 targets including FFA1, FFA2 and FFA3.

GSK1324726A (I-BET726) is a novel, potent, and selective small molecule inhibitor of BET proteins with high affinity to BRD2 (IC50= 41 nM), BRD3 (IC50= 31 nM), and BRD4 (IC50= 22 nM).

GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase with Ki value of 0.5 nM.

GSK1016790A is a novel and potent TRPV4 channel agonist.

GSK-0660 is a selective PPARδ antagonist (IC50 values are 0.155, > 10 and ≥ 10 μM at PPARδ, PPARα and PPARγ respectively).

GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM and inactive against a panel of demethylases of the JMJ family.

GS-9973 is an orally bioavailable, selective Syk inhibitor with IC50 of 7.7 nM. Phase 2.

GRL-0617 is a potent, noncovalent SARS-CoV papain-like protease (PLpro) inhibitor with IC50 of 0.6 uM, Ki of 0.49 uM.

Grapiprant is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2)

GR-127935 potent and selective 5-HT1B/1D receptor antagonist with pKi of 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptor.

GPR120 compound A is an orally available, high-affinity agonist of GPR120 (EC50 = ~0.35 µm) that demonstrates potent selectivity over another lipid-sensing G-protein, GPR40 (FFAR1).

GOT1 inhibitor 2c is a first-in-class, non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with IC50 of 8.2 uM..

Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ.

GNF-5, an analogue of GNF-2 with improved pharmacokinetic properties, is a selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 0.22±0.1 uM (Wild type Abl).

GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl, inhibiting the proliferation of the Bcr-Abl-expressing cells with IC50 of 138 nM.

GNE-9605 is a highly potent and selective Leucine-rich repeat kinase 2 (LRRK2) inhibitor

GNE-617 is a potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with IC50 value of 5nM.

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.

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