GS-9451 (Vedroprevir) is a potent HCV NS3/4A protease inhibitor with Ki of 0.41 nM, inhibits HCV GT-1b NS3/4A with IC50 of 3.2 nM in enzymatic assays.

GS-9695 is a potent, non-catalytic site HIV integrase inhibitor with wild type EC50 of 1.2 nM..

GS-9822 is a novel, potent NCINI with a higher barrier to resistance relative to early prototype NCINIs, including GS-9695.

GSA-10 is a novel small-molecule positive modulator of Smoothened with EC50 of 1.2 uM in the differentiation assay.

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.

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

GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, respectively.

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) .

GSK2334470 is a novel PDK1 inhibitor with IC50 of ~10 nM, with no activity at other close related AGC-kinases.

GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).

GSK2814338, also known as Lp-PLA2 -IN-1, is a Lp-PLA2 inhibitor

GSK2983559 active metabolite is an active metabolite of GSK2983559. GSK2983559 active metabolite is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.

GSK3039294 is a Serum amyloid P component inhibitor.

GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.

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

GSK8612 is a highly selective and potent Tank-binding Kinase-1 (TBK1) inhibitor, with a pIC50 of 6.8 for recombinant TBK1.

GSK-A1 is a potent inhibitor of PI4KA. In vitro using HEK-AT1 cells, GSK-A1 had an IC50 of about 3 nM.

GSK-F1 is a potent inhibitor of PI4KA.

GSK-J1 is a potent and selective inhibitor of the H3K27 histone demethylases JMJD3 and UTX (IC50 = 60 nM for human JMJD3 in vitro).

GSM-1 (GSM1) is a γ-secretase modulator that directly targets the transmembrane domain (TMD) 1 of presenilin 1, shows potent Aβ42-lowering effect (IC50=0.348 uM) in a cell-based assay.