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

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

Novel Photosensitive and Photoswitchable TRPA1 Agonist, Optically Control Pain through Channel Desensitization

Fluroquinolone antibiotic, suppressing c-Myc transcription and myeloma growth, inhibiting pannexin-1 channels through which ATP is released as find-me signals in apoptotic Jurkat cells

Serotonin 5-HT3 receptor antagonist

Potent and selective 5-HT3 receptor antagonist

First-in-class highly potent and selective inhibitor of TrmD (bacterial t-RNA-(N1G37) methyltransferase)

Novel potent and selective inhibitor of Tropomyosin-related kinase A (TrkA)

Novel opioid ligand for treatment of overactive bladder, acting as a μ-opioid receptor partial agonist

First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitor that Overcome Clinically Acquired Resistance

Novel anti-secretory and antiulcer agent for treatment of peptic ulcer disease and hypersecretory disorders

Copper ion chelator, causing the triple response phenotype by affecting copper ion transport in ethylene signaling from ATX1 to RAN1

Specific inhibitor of the histone H3 lysine 9 demethylase KDM4 in HeLa cells.

Antipsychotic and sedative agent as a potent antagonist of H1, 5-HT2A, and alpha1-adrenergic receptors

Metabolite of nicotinamide; Specific and potent inhibitor of NNMT, increasing histone methylation at H3K4 and methylated H3K4 occupancy at gene promoters

Novel Bromodomain Binding Mimic of Lysine Acetylation

Metabolite of Trifluoperazine; Antidepressant and antipsychotic

Potent NAE-hydrolyzing acid amidase (NAAA) inhibitor

AKT Inhibitor, Enhancing Gemcitabine Activity in Pancreatic Cancer Cells