Novel inhibitor of heat shock protein 90 (Hsp90)

Thiazolidine-containing cyclic peptide antibiotic, suppressing growth of species of disease-causing bacteria in that part of the human microbiome

Hybrid ortho/allosteric ligand of the adenosine A(1) receptor

Human adenosine A1 receptor antagonist

A1 adenosine receptor antagonist

Potent mGlu5 receptor positive allosteric modulator (PAM)

Potent and selective adenosine A2A receptor antagonist

Novel β2i-specific inhibitor, displaying moderate trypanocidal activity

Novel potent β2c-specific inhibitor, displaying moderate trypanocidal activity

Novel β2-specific inhibitor, potently targeting both β2c and β2i, displaying moderate trypanocidal activity

Novel potent and selective LMP2 inhibitor, also inhibiting mouse 20S proteasomes

Novel, potent, selective and brain penetrant positive allosteric modulator of alpha-7 nicotinic acetylcholine receptors

Novel potent and selective inhibitor of LRRK2, inhibiting LRRK2 WT, the overactive variant G2019S, and the resistant mutant A2016T56 at 12 nM, 19 nM and 93 nM, respectively

Novel potent and selective hA2A receptor antagonist

Brain penetrant high affinity α1A-adrenoceptor ligand

Novel PI 3-kinase delta inhibitor

Peptide metabolite

Novel inhibitor of the interactions of CFTR-associated ligand (CAL) and PSD-95/Dlg1/ZO-1 (PDZ) domain

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

Novel potent xanthine oxidase inhibitor

Selective inhibitor of P-glycoproteins (P-gp)

Precursor for 11C-radiolabelling LSN3172176 PET scan

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

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

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 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

The first small molecule antagonist of LRH-1 activity.

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

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