A potent, specific and orally active 5-Lipoxygenase-activating protein (FLAP) inhibitor with IC50 of 1.6 nM in FLAP binding assay.

A potent, specific and orally bioavailable soluble epoxide hydrolase (sEH) inhibitor with IC50 of 1.3 nM.

A potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 5.4 nM.

VU 0465350 is a potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 92.3 nM; shows no activity for ALK2/4/5, also shows affinity for TGFBR2, VEGFR2 and AMPK; blocks SMAD phosphorylation in vitro and in vivo, and enhances liver regeneration after partial hepatectomy.

A potent, specific CDC-like kinase (CLK) inhibitor with IC50 of 78, 16 and 86 nM for CLK1, 2 and4, respectively.

A potent, specific cell-active VHL E3 ubiquitin ligase inhibitor that inhibits VHL/HIF-α interaction with Kd of 90 nM in ITC assays.

A potent, specific GSK-3 inhibitor with IC50 of 5 nM and 10 nM for GSK3β and GSK3α, respectively.

A potent, specific immunoproteasome LMP7 subunit inhibitor with IC50 of 25 nM, >100-fold selectivity over β5c, β1i, β1c, β2i and β2c subunits (IC50>3 uM).

A potent, specific immunoproteasome β1i (LMP2) subunit inhibitor with IC50 of 104 nM, 144- and 10-fold selectivity over β1c and β5 subunit respectivey.

A potent, specific immunoproteasome β5 subunit inhibitor with IC50 of 17 nM, 21-fold and 13-fold selectivity for β5 over LMP7 and LMP2 subunits, respecitvely..

A potent, specific immunoproteasome β5 subunit inhibitor with IC50 of 44 nM, 105 and 225-fold selectivity over β2i and β1i subunit, respecitvely.

A potent, specific immunoproteasome β5 subunit inhibitor..

A potent, specific inhibitor of HCV NS5B polymerase and HCV replication (IC50=1.28 uM, replicon assay).

A potent, specific inhibitor of the SGK1 kinase activity, induces autophagy, apoptosis and ER stress in cancer cells.

A potent, specific mechanism-based human NAD(P)H: quinone oxidoreductase 1 (NQO1) inhibitor that demonstrates efficient inactivation of NQO1 at 100 nM in in cellular systems.

A potent, specific P-gp inhibitor with Kd of 5.1 nM.

A potent, specific proteasome β5 subunit inhibitor with IC50 of 0.26 uM, 7.3 and 17.3-fold selectivity over β2i and β1i subunit, respecitvely..

A potent, specific RARα agonist with Ki of 2 nM, displays no significant effects on RARγ in reporter based assays..

A potent, specific S1P2 receptor (Edg-5) antagonist with IC50 of 3 nM, with no agonistic or antagonistic activities on other S1PRs.

A potent, specific survivin inhibitor that inhibits survivin promoter activity with IC50 of 0.54 nM.

A potent, specific, allosteric and cell-active inhibitor of KSP with IC50 of 11 nM.

A potent, specific, allosteric inhibitor of KSP motor domain ATPase with Ki of 12 nM.