Novel highly selective negative allosteric modulator (NAM) of thyrotropin receptor (TSHR), binding at the ectodomain/TMD interface, between the converging helix, ECL1 and the IA, noncompetitively inhibiting PAM-C2-activation

Novel human thymic stromal lymphopoietin (TSLP) inhibitor

Novel isoform-selective inhibitor of the tumor-associated hCA IX and XII

Novel αvβ3 ligand, disrupting the integrin-MMP2 interaction and showing antiangiogenic activit, inhibiting angiogenesis and tumor growth in vivo

Novel antagonist of T-type calcium channels

First-in-class potent threonine tyrosine kinase (TTK) PROTAC, demonstrating strong TTK degradation in COLO-205 human colorectal cancer cells with DC 50 values of 1.7 nM

First-in-class potent threonine tyrosine kinase (TTK) PROTAC, demonstrating strong TTK degradation in COLO-205 human colorectal cancer cells with DC 50 values of 3.1 nM

Novel transthyretin (TTR) stabilizer, binding to the T4 binding pocket of TTR and preventing the dissociation of TTR to monomer

FLT3 Kinase Inhibitor, Overcoming Both Activating and Drug Resistance Mutations in FLT3 in Acute Myeloid Leukemia

LpxC substrate-analog inhibitor

Novel inhibitor of tubulin polymerization and caused HepG2 cells arrest in G2/M phase

Novel potent tubulin polymerization inhibitor, forming stable interactions in the colchicine-binding site of tubulin, showing significant antiproliferative activities on a panel of tumor cell lines

Novel allosteric modulator of free fatty acid receptor 3 (FFA3, previously GPR41)

Novel allosteric modulator of free fatty acid receptor 3 (FFA3, previously GPR41)

Long-acting beta2-adrenergic receptor agonist

Novel Inhibitor of Metastatic Cancer Cell Migration and Invasion

Antibiotic, inhibiting the first step in the N-linked glycosylation in eukaryotes and inducing ER stress to activate the unfolded protein response (UPR)

Inhibitor of bacterial biofilm formation in Staphylococcus epidermidis

Natural potent porcine pancreatic elastase (PPE) inhibitor

Novel anticancer agent, affecting steroid biosynthesis, increasing RagD expression, and causing abnormal cellular cholesterol localization

Novel disruptor of the bacterial protein, FtsZ

Chymase inhibitor, preventing the development and progression of non-alcoholic steatohepatitis, improving vascular dysfunction and survival in stroke-prone spontaneously hypertensive rats