Novel potent small molecule lligand of miR-21, binding to the major groove of miR-21 hairpin conformation

Novel effective immune checkpoint inhibitor (ICI) against the suppression of T-cell activation, proliferation, and tumor cell eradication.

Novel TNF-α inhibitor

Novel Nef Protein Inhibitor; Anti-HIV

Novel blocker of AKT1-FAK interaction, reducing the stimulation of FAK phosphorylation in response to extracellular pressure in human SW620 colon cancer cells without affecting basal FAK phosphorylation

Potent VEGFR-2 inhibitor

Novel antagonist for mLST8

The first nonpeptidic inhibitor of ovarian cancer cells growth targeting human thymidylate synthase (hTS)

Growth promotant, acting as a ß-AR (ß-Adrenergic) agonist

Atypical analgesic agent for the amelioration of severe and chronic pain

Fluorogenic peptide substrate for a direct fluorometric assay of urokinase, tissue-type plasminogen activator, trypsin and thrombin

Novel Potent and Orally Bioavailable Hypoxia-Inducible Factor 2α (HIF-2α) Agonist

Novel inhibitor of pro-HGF activation

Novel daul inhibitor of GSK-3β (IC 50 = 71 nM) and DYRK1A (IC 50 = 103 nM) with good blood-brain barrier penetrability, inhibiting hyperphosphorylation of tau protein in okadaic acid (OKA)-induced SH-SY5Y cells

Site specific inhibitor of tissue transglutaminase

Novel potent HDAC inhibitor with IC50 values for class I HDACs 1, 2, and 3 below 4 nM, and IC50 for HDAC6 at 6 nM.

ZDHHC (zinc finger Asp-His-His-Cys) substrate peptide, a 15-mer peptide sequence from KRas4a plus two tryptophan residues

Potassium channel opener

Vascular targeting agent (VTA)

Potent, orally active inhibitor of 5-lipoxygenase (5-LO)

Endothelin Receptor Antagonist

Novel camptothecin derivative, revealing potent antitumor activities mainly through cell apoptosis pathway, being more effective than CPT-11 and SN38 at inhibiting topoismerase-1

Serotonin 5-HT3 receptor antagonist

Inhibitor of the nuclear division in germinating zoospore cysts of Phytophthora capsici via destruction of the microtubule cytoskeleton, and a consequent inhibition of mitosis

Novel USP10 inhibitor

Novel potent dual σ1/2 ligand (σ1 K i =5nM, σ2 K i =3nM), showing anti-allodynic in a model of neuropathic pain

Novel riboswitch activator, binding ZTP riboswitches, and activating transcription more strongly than ZMP in vitro

Novel potent ligand of σ2 receptor (K i =7nM)

Novel first-in-class inhibitor of BRD4 and EGFR kinase

Novel activator of JNK, binding directly to microtubules, inducing ERK-mediated mitotic arrest and subsequent apoptosis