Potent, selective, and orally active inhibitor of semicarbazide-sensitive amine oxidase (SSAO) activity, inhibiting vascular adhesion protein 1 (VAP-1) activity and decreasing the density of macrophages in inflamed atherosclerotic plaques in mice

Novel pan-inhibitor of sialyltransferase (ST)

The first fluorogenic dipeptide probe for

The first inhibitor of the catalytic activity of AChE and AChE-induced amyloid-beta aggregation protecting against reactive oxygen species

Lipid II binder, causing specific upregulation of the vancomycin-resistance associated gene vraX which is implicated in the cell wall stress stimulon that confers glycopeptide resistance

5HT-4 antagonist with moderate 5HT-3 antagonist properties

Novel Fused Benzodiazepine Hybrid Payload for Antibody-Drug Conjugate (ADC)

Natural capsid inhibitor

Novel inhibitor of the oncogenic Lin28-let-7 interaction

Potent positive inotropic agent, inhibiting myocardial cell apoptosis

Inhibitor of cholinephosphotransferase (CPT), phosphatidyl-N-methylethanolamine N-methyltransferase (PME-NMT), and phosphatidyl-N,N-dimethylethanolamine N-methyltransferase (PDE-NMT)

Novel inhibitor of AMA1–RON2 interaction, blocking merozoite invasion from schizont-infected RBCs; Cytochrome P450 inhibitor

Serotonin-norepinephrine-dopamine triple reuptake inhibitor (SNDRI); Anti-depressant

Natural precursor of histamine; reversible inhibitor of protein synthesis

Novel inhibitor of cystine stone formation for treatment of cystinuria

Novel S. typhimurium infection inhibitor on the activity of DUSP3, DUSP11, and DUSP27

Potent and specific pan-PIM inhibitor, inhibiting proliferation of several AML cell lines, showing dual antitumoral and bone antiresorptive effects

Novel irreversible inhibitor of cell division cycle 25B, inhibiting human cancer cells via ROS generation

Novel non-secosteroidal vitamin D receptor (VDR) ligand

Novel potent and selective antagonist of exportin-1, attenuating dual NF-κB signaling and the Nrf2 cytoprotection pathway via targeting exportin-1 in colitis mice

Hematologic malignancy-selective membranolytic peptide from the antimicrobial core (RRWQWR) of bovine lactoferricin

Selective estrogen receptor modulator (SERM)

Neuroprotective, anti-inflammatory, and anti-diabetic agent, protecting against DNA damage and apoptosis induced by ultraviolet light

Respiratory quinolone antibiotic, exhibiting enhanced activity against the important respiratory pathogen Streptococcus pneumoniae

Natural carnitine derivative, playing a role in mitochondrial metabolism and demonstrating beneficial cardiovascular effects

Watersoluble prodrug of Levcromakalim, being more chemically robust and efficacious at lowering IOP with once daily dosing in a normotensive mouse model.

Partial agonist (antagonist) at mu and delta opioid receptors.

Inhibitor of ERAAP function

Leukotriene B4 receptor antagonist

Orally bioavailable Smoothened (Smo) antagonist