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).

GPR39-C3 is the first potent, selective and orally bioavailable GPR39 agonist with an EC50 ~0.8 nM for human GPR39 and ~0.4 nM for rodent GPR39.

GPR4 antagonist 3 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. Anti-inflammatory activities.

GpTx-1 is a potent, selective, 34-residue peptide antagonist of Nav1.7 sodium channel with IC50 of 10 nM, displays 20- and 1000- fold selectivity over NaV1.4 and NaV1.5..

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.

GR3027 (Golexanolone) is a GABA-A receptor modulating steroid antagonist that selectively antagonizes the enhanced activation of GABAA receptors by neurosteroids such as allopregnanolone and THDOC.

GR-73632 is a potent and selective tachykinin NK1 receptor agonist with EC50 of 2 nM, promotes differentiation but not survival of rat chromaffin cells in vitro..

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.

GS-6207 (GS6207, GS-CA1) is a potent, selective inhibitor of HIV-1 capsid function with potency and potential to be clinically effective against a broad range of HIV-1 strains..

GS-7340(Tenofovir alafenamide) is a prodrug of tenofovir (TFV) that more efficiently delivers TFV into lymphoid cells and tissues than TFV disoproxil fumarate.

GS-7340(Tenofovir alafenamide) is a prodrug of tenofovir (TFV) that more efficiently delivers TFV into lymphoid cells and tissues than TFV disoproxil fumarate.

GS-9620 is a potent and selective orally active small molecule agonist of Toll-like receptor 7(TLR-7) in chimpanzees with chronic HBV infection.

GS967 is a novel, potent, and selective inhibitor of cardiac late sodium current(late INa).

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

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

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

GSK 5959 is a potent, cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM).

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.

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

GSK1016790A is a novel and potent TRPV4 channel agonist.

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).