GRA Ex-25 is an orally active human glucagon receptor antagonist in a transgenic murine pharmacodynamic model at 10 and 30 mpk.

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

GSK 525762A is a potent small molecule inhibitors that disrupt the function of the BET family of bromodomains (Brd2, Brd3, and Brd4).

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.

GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM; displays >100-fold selectivity against the closely related Aurora A-TPX2 complex(IC50=490 nM).

GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes.

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.

GSK2256098 is small molecule FAK kinase inhibitor.

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

GSK2292767 is a potent and selective PI3Kδ inhibitor.

GSK2330672 is a highly potent, nonabsorbable ASBT(apical sodium-dependent bile acid transporter) inhibitor (hASBT IC50=42 ± 3 nM) .

GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.

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

GSK2881078 (GSK-2881078 ) is a selective androgen receptor modulator (SARM).

GSK2981278 is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma).

GSK2982772 is a potent and ATP competitive RIP1 inhibitor with an IC50 of 16 nM.

GSK3117391 (CHR5154) is a HDAC inhibitor.

GSK3179106 (GSK-3179106, GSK 3179106) is a potent, selective, first-in-class and gut-restricted with IC50 of 0.4 and 11 nM in the biochemical assay and cellular assay respectively.

GSK3326595(EPZ015938) is the first-in-class protein arginine methyltransferase-5 (PRMT5) inhibitor.

GSK690693 is a pan-Akt inhibitor targeting Akt1, Akt2 and Akt3 with IC50 of 2 nM, 13 nM, and 9 nM, respectively.

GSK923295 is a first-in-class, specific allosteric inhibitor of CENP-E kinesin motor ATPase with Ki of 3.2 nM, and less potent to mutant I182 and T183.

Guanfacine Hydrochloride is a selective α2A-adrenoceptor agonist with anti-hypertensive effect.