GSK583 is a Highly Potent and Selective Inhibitor of RIP2 Kinase (RIP2K bing IC50=5 nM; rat in vivo PD IC50 = 50 nM).

GSK547 (RIP1i, GSK 547) is a highly selective and potent inhibitor of RIP1 kinase that robustly targets RIP1 in vivo.

GSK503 is a specific EZH2 methyltransferase inhibitor.

GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.

GSK4112 is a Rev-erbα agonist with EC50 of 0.4 μM, also is a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα.

GSK3787 is as a potent and selective antagonist of PPARδ with pIC50 of 6.6.

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

GSK3145095 is an orally available, small-molecule inhibitor of RIPK1, with potential antineoplastic and immunomodulatory activities.

GSK3117391 (CHR5154) is a HDAC 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.

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

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

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).

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.