Novel potent negative allosteric modulator (NAM) of mGlu2

Novel Dual Fluorescent and Magnetic Resonance False Neurotransmitter

Radiographic Contrast Agent

Non-depolarizing muscle relaxant

Dopamine D2 antagonist, antiemetic

Highly Selective Class II MET Inhibitor

Peripherally restricted μ-opioid antagonist

Novel Class of Cannabinoid CB2 Receptor Inverse Agonist

Metablite of PRIMA-1 and APR-246, covalently binding to cysteine residues in mutant p53 and wild type p53, and being increased in unfolded p53, inducing massive apoptosis in p53 null tumor cells

Novel inhibitor of ABCG2 transporter function

Novel photosensitizer as a photodynamic antimicrobial agent against Staphylococcus aureus, Escherichia coli, Candida albicans, and Methicillin-resistant S. aureus (MRSA)

Useful pharmaceutical building block

Inhibitor of pro-inflammatory mediator release from mast cells

Natural potent anti-proliferative agent, inducing apoptotic cell death

Potent, long-lasting, and selective antagonist of morphine-mediated antinociception

Cyclooxygenase 3 (COX3) inhibitor, acting as a potent inductor of cytochrome P450 isoenzymes CYP2B6 and CYP3A4

Novel selective GPR120 agonist

Novel selective and potent full KOP receptor agonist with fewer side effects (e.g., sedation or anhedonia) than classic KOP receptor

Anabolic and androgenic agent

LXR-α antagonist, inhibiting hepatic lipid accumulation by activating AMP-activated protein kinase in human HepG2 cells

Apoptosis inducer, triggering ROS dependent autophagy-associated apoptosis in a variety of human cancer cell lines and against mutant KRAS expressing cancer cells involving AKT-dependent ROS production

Potent cell-permeable, ATP site-targeting inhibitor of CDKs

Potent cell-permeable, ATP site-targeting inhibitor of CDKs

Novel Cell Death-Inducing Kinase Inhibitor with Enhanced Selectivity for Cyclin-Dependent Kinases; Antimalarial

Novel potent and selective nonpeptide kinin B2 receptor antagonist

5-HT2A/D2 receptor antagonist

Potent, selective and orally bioavailable inhibitor of dipeptidyl peptidase 4 (DPP-4)

Novel Multi-Kinase Inhibitor, Triggering Mitotic Catastrophe of Glioma Stem Cells Mainly through MELK Kinase Inhibition

Inhibitor of cholesterol esterification

Prodrug of melarsen oxide (Mel Ox), irreversibly binding to vicinal sulfhydryl groups on pyruvate kinase, disrupting energy production in the parasite