A novel small-molecule inhibitor of androgen receptor (AR) N-terminal domain inhibitor for the treatment of advanced prostate cancer.

A novel small-molecule inhibitor of androgen receptor (AR) N-terminal domain inhibitor for the treatment of advanced prostate cancer.

A novel small-molecule arenaviruse inhibitor that exhibits strong anti-LCMV activity (IC50<1 uM) without cell toxicity.

A novel small molecule Wnt signaling inhibitor that targets the cysteine-rich domain of Frizzled, specifically binds to the Wnt binding site on the Frizzled8 cysteine-rich domain with Kd of 2.9 uM, IC50 of 5.7 uM..

A novel small molecule that overcomes HdmX-mediated p53 repression, binds directly to HdmX (Kd=450 nM) to prevent p53-HdmX complex formation.

A novel small molecule that activates GATA4/NKX2-5 transcriptional synergy with EC50 of 7 uM in cell reporter assay. .

A novel small molecule STAT3 inhibitor that inhibits STAT3 DNA binding activity with IC50 of 1.16 uM, binds to the STAT3 coiled-coil domain (CCD).

A novel small molecule sirtuin-1 (SIRT1) activator that reduces acetylation of mutant 53 and exhibits anti-proliferative effects against TNBC cells carrying mutant p53.

A novel small molecule KLF5 inhibitor derived from ML264, demonstrates >10-fold enhanced efficacy in multiple cancer cell lines with IC50 of 1.5-10 uM.

A novel small molecule inhibitor that inhibits PP2A and β-catenin interaction by selectively engaging PR55α binding site (Kd=45 pM).

A novel small molecule inhibitor of transforming acidic coiled-coil-containing protein 3 (TACC3) that selectively inhibits the nucleation of centrosome microtubules in ovarian cancer cells.

A novel small molecule inhibitor of transforming acidic coiled-coil-containing protein 3 (TACC3) that selectively inhibits the nucleation of centrosome microtubules in ovarian cancer cells.

A novel small molecule inhibitor of the DNA repair protein Ku70/80, disrupts of Ku70/80-DNA interaction with IC50 of 3.5 uM in EMSA assay.

A novel small molecule inhibitor of PDE6δ/KRas interaction with Kd of 203 pM.

A novel small molecule inducer of heme oxygenase-1 that protect human iPSC-derived cardiomyocytes from oxidative stress.

A novel small molecule ALDH inhibitor with IC50 of 600 nM, 800 nM and 1000 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively.

A novel small molecule activator of Kv 11.1 (hERG) channel (216% over control at 3 uM for hERG1a activation).

A novel SirReal-based PROTAC that induces isotype-selective Sirt2 degradation (IC50=0.25 uM)..

A novel selective, small-molecule inhibitor of sirtuin SITR2 with IC50 of 21.8 uM.

A novel selective, small molecule large-conductance Ca(2+)-activated K(+) channel (BKCa, KCa1.1, MaxiK) positive modulator with EC50 of 11 uM.

A novel selective STAT3 inhibitor with IC50 of 4.2 uM, does not inhibit STAT1, STAT5, or NFkB signaling pathways (IC50>50 uM).

A novel selective small molecule Rac1 inhibitor that blocks Rac1-PAK1 complex formation with IC50 of 95±21 nM.

A novel selective small molecule Rac1 inhibitor that blocks Rac1-PAK1 complex formation with IC50 of 88±48 nM.

A novel selective small molecule inhibitor of PDE6δ/KRas interaction with Kd of 358 pM..

A novel SAM-competitive, highly selective, orally bioavailable EZH1/2 dual inhibitor with IC50 of 16/50 nM, respectively.

A novel P-selectin inhibitor that directly binds to P-selectin.

A novel potent, subtype-selective sigma 2 receptor/PGRMC1 ligand with Ki of 61 nM, 9-fold selectivity over sigma 1 receptors (Ki=556 nM).

A novel potent, subtype-selective sigma 2 receptor/PGRMC1 ligand with Ki of 16.2 nM, 574-fold selectivity over sigma 1 receptors..

A novel potent, specific, orally available GPR40 agonist that influences glucose-dependent insulin secretion both in vitro pancreas β-cell-derived cells and in vivo.

A novel potent, specific, covalent USP7 inhibitor with Kd of 7.8 uM (USP7 catalytic domain).