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.

GSK481 is a Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitor (RIP1 inhibitor). The recent discovery of the role of receptor interacting protein 1 (RIP1) kinase in tumor necrosis factor (TNF)-mediated inflammation has led to

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.

GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases.

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 free acid (compound 3) is a potent, specific and oral bioavailable receptor interacting protein 2 (RIP2) kinase inhibitor. GSK2983559 free acid has excellent activity in blocking many proinflammatory cytokine responses in vivo and in human infl

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).

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.