Novel highly potent and selective TYK2 JH2 inhibitor, providing robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model

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

Novel disruptor of the bacterial protein, FtsZ

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

Natural potent porcine pancreatic elastase (PPE) inhibitor

Inhibitor of bacterial biofilm formation in Staphylococcus epidermidis

Novel Inhibitor of Metastatic Cancer Cell Migration and Invasion

Long-acting beta2-adrenergic receptor agonist

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

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

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

LpxC substrate-analog inhibitor

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

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

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

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

Novel antagonist of T-type calcium channels

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

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

Novel human thymic stromal lymphopoietin (TSLP) inhibitor

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

Natural Polycyclic Peptide from a Fungus-Derived Streptomycete

Natural DNA gyrase inhibitor, blocking leukotriene production, inhibiting P-glycoprotein, and showing anti-inflammatory and anti cancer activities

Novel TrxR1 inhibitor, selectively killing of gastric cancer cells by a small molecule via targeting TrxR1 and ROS-mediated ER stress activation

Novel selective TRPV6 inhibitor

Novel agonist of the transient receptor potential melastatin 8 (TRPM8) ion channel

Novel selective inhibitor of the transient receptor potential melastatin 2 (TRPM2) channel, exhibiting TRPM2 selectivity over TRPM8 and TRPV1 channels as well as phospholipase A2 and showing neuroprotective activity in vitro, and significantly reducing ce

Novel potent and selective TRPA1 inhibitor, interacting with the N-terminal ankyrin repeat (ankyrinR) domain

Novel potent and selective TRPA1 inhibitor, interacting with the N-terminal ankyrin repeat (ankyrinR) domain