Novel LOX-activity sensor for cross-linking with a collagen peptide to chemoselectively target endogenous aldehydes generated by LOX

Potent ligand of the 5-HT7 receptor

Potent antimitotic and oral tubulin binding agent, significantly inhibiting growth of a human non-small-cell lung tumor

Novel potent and selective peripheral AAK1 inhibitor

Novel inhibitor of both renal SGLT1 and SGLT2

Novel LPA 1-3 agonist, inducing a calcium response in hLPA 1-3 cells within a range of 0.4 to 1.5-log lower potency, as compared to LPA

Novel LPA 1-3 agonist, inducing a calcium response in hLPA 1-3 cells within a range of 0.4 to 1.5-log lower potency, as compared to LPA

Novel p53 activator through the inhibition of MDM2

Novel potent and specific inhibitor of O-linked β-N-acetylglucosamine transferase (OGT)

Novel agonist of liver receptor homolog-1 (LRH-1), reducing the expression of lipogenic genes in mouse liver, and inflammation and disease severity in a mouse model of ulcerative colitis

Novel potent agonist of the liver receptor homolog-1 (LRH-1, NR5A2)

The first small molecule antagonist of LRH-1 activity.

Novel selective and reversible LSD1 inhibitor (IC50 value of 60 nM), exhibiting the antiproliferative activity against HTB5, HTB3, HT1376, and HTB1 cells with IC50 values of 1.87, 0.18, 0.09, and 0.93 μM, respectively

Novel selective inhibitor of histone lysine specific demethylase 1 (LSD1/KDM1A), displaying FAD-competitive binding to LSD1, concentration-dependently inducing accumulation of H3K4me1/me2 and H3K9me2, increasing expression levels of epithelial cell marker

Novel prodrug of Lisofylline, maintaining a steady fasting blood glucose level with a significant increase in insulin level

Novel prodrug of Lisofylline, maintaining a steady fasting blood glucose level with a significant increase in insulin level

First-in-class inhibitor of NF-κB signaling pathway by preventing the maturation of a rate-limiting multiprotein complex necessary for IKK activation

Novel positive allosteric modulator (PAM) of the GLP-1R, enhancing insulin secretion in a glucose-, ligand- and GLP-1R-dependent manner

Precursor for 11C-radiolabelling LSN3172176 PET scan

Selective inhibitor of P-glycoproteins (P-gp)

Novel potent xanthine oxidase inhibitor

Novel potent inhibitor of FLT3 mutations, also inhibiting CDK2 and CDK6