Potent and irreversible inhibitor of GSK3

Novel highly potent cell-permeable, reversible, ATP-competitive inhibitor of GSK-3 (IC50 = 0.4 and 0.6 nM for GSK-3α and GSK-3β, respectively)

Novel DNMT1-selective inhibitor (IC 50 = 0.11 ± 0.02 µM)

Novel anti-TB agent against Mycobacterium tuberculosis and Mycobacterium bovis BCG, targeting MmpL3 and inhibiting EchA6

Novel inhibitor of prolyl hydroxylase (PHD) domain-containing enzyme

Novel lysine specific histone demethylase 1 (LSD1) inhibitor, exhibiting high selectivity to LSD1 over MAOs

Novel selective non-imidazole histamine H 3 receptor antagonist

Novel agonist of toll-like receptor 2 (TLR2), stimulating the release of G-CSF in activated THP-1 cells, peripheral blood mononuclear cells, and human umbilical vein endothelial cells

Promiscuous kinase inhibitor, a close analog of CTx-0294885

Novel selective inhibitor of G protein-coupled receptor kinase 2 (GRK2)

Potent and selective antagonist of P2X7 receptor

Novel potent RORγ inverse agonist

Novel quaternized GSK-3008348 derivative, acting as a highly selective αvβ6 Integrin Inhibitor

Novel inhbitor of protein kinase GRK1/2/5 and PKA

Novel human immune virus (HIV) maturation inhibitor

Novel potent and selective, SAM-competitive inhibitor of SMYD3

Novel selective inhibitor of G protein-coupled receptor kinase 2 (GRK2)

Betulin derivative as antitumor agent

Specific ATPase competitive kinesin-5 inhibitor

Novel selective histamine H3 receptor antagonist

Novel I-kappa-B kinase-3 (IKK3) inhibitor

Novel S1P1 receptor agonist

Novel highly potent, reversible soluble epoxide hydrolase (sEH) inhibitor, exhibiting potent cell-based activity, a concentration-dependent inhibition of the conversion of 14,15-EET to 14,15-DHET, attenuating cigarette smoke-induced inflammation by both i

Selective inhibitor of iE-DAP-stimulated IL-8 release via the NOD1 signaling pathway

Inhibitor of insulin receptor, also tageting IGF-1R and ALK

Novel inhibitor of T. brucei IPMK, partially inhibiting rTbIPMK activity

Novel insulin-like growth factor 1 receptor inhibitor, binding to a novel region of the GRK active site cleft that could likely be exploited to achieve more selectivity

Novel AKT Inhibitor, Enhancing Anti-Tumor Effects in Combination with the MEK Inhibitor

Novel selective non-imidazole histamine H 3 receptor antagonist

Novel competitive inhibitor of rTbIPMK with respect to Ins(1,4,5)P3