Novel inhibitor of glutaminase 1 (GLS1) with high binding affinity (SPR, Kd = 24 nM; ITC, Kd = 37 nM), exhibiting a similar in vivo antitumor activity as CB839

The first-in-class, ATP-competitive inhibitor of MAPKAPK5

Ago-allosteric modulator of human GLP-2R

Enteroendocrine hormone, stimulating the growth of intestinal epithelium

Novel inhibitor of glyoxalase 1 (Glo1), increasing the cellular methylglyoxal levels in human cells and suppressing the osteoclast formation of mouse bone marrow-derived macrophages

Novel potent Glyoxalase 1 (GLO1) inhibitor, demonstrating to penetrate the blood-brain barrier, elevating levels of methylglyoxal in the brain, and reducing depression-like behavior in mice

Novel inhibitor of the acetyltransferase activity of Escherichia coli N-acetylglucosamine-1-phosphate-uridyltransferase/glucosamine-1-phosphate-acetyltransferase (GlmU).

Second-generation sulfonylurea, promoting the accumulation of fructose 2,6-bisphosphate in hepatocytes

Novel Galactofuranosyltransferase 2 (GlfT2) inhibitor

Novel 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor

Novel inhibitor of the cell cycle progression in M-phase; Inhibotor of endosome maturation

First-in-class liver-selective glucokinase activator for the treatment of type 2 diabetes

Novel and potent glucokinase activator (GKA)

Novel Allosteric Activator of Human Glucokinase in the Absence of Glucose

Novel water solubile prodrug of ICRF-193, penetrating into NVCMs, reaching intracellular concentrations sufficient to induce cytoprotective effects against ANT toxicity

First-in-Class, Potent, and Orally Bioavailable NADPH Oxidase Isoform 4 (Nox4) Inhibitor

Natural Activator of the Nrf2-Regulated Antioxidant Defense System in SH-SY5Y Cells, Binding to the Subpockets of Keap1 Kelch Domain

Natural suppressor of mesenchymal stem cell (MSC) differentiation

Novel suppressor of endoplasmic reticulum (ER) stress and oxidative stress, preventing protein aggregate accumulation in vitro and in cultured hippocampal HT22 neuronal cells, as well as glutamate-induced oxytosis and erastin-induced ferroptosis

Novel suppressor of endoplasmic reticulum (ER) stress and oxidative stress, preventing protein aggregate accumulation in vitro and in cultured hippocampal HT22 neuronal cells, as well as glutamate-induced oxytosis and erastin-induced ferroptosis

Potent mitochondrial benzodiazepine receptors (MBRs) ligand; Prodrug for its active metabolite bromo-nordazepam

Novel oral anti-nociceptive agent, showing peripheral opioid agonistic activity and hydrogen sulphide-releasing capacity

Potent EGFR/erbB2 dual inhibitor

Metalloproteinase inhibitor, specifically blocking TNF-alpha secretion both in vitro and in vivo

Novel nonpeptidic inverse agonist of the Ghrelin Receptor (GHSR)

Endogenous dipeptide, activating N-methyl-D-aspartate receptors

Natural non-covalent NRF2 activator, activating NRF2 in A KEAP1-dependent but Cys151-independent manner, conferring greater protection than a Cys151-dependent analog, geopyxin C

Natural covalent Cys151-dependent NRF2 activator

Metabolite of ganstigmine, a novel acetylcholinesterase inhibitor

Novel antifungal agent