A novel, long-acting and orally active, selective mu-opioid agonist that displays higher binding affinity (Ki=237 nM) at the MOR than kappa and delta opioid receptors (>100-fold).

A novel, highly potent inhibitor of the FabI enzyme of both Staphylococcus aureus and Escherichia coli.

A novel, highly potent and selective phosphodiesterase 4 (PDE4) inhibitor with IC50 of 0.026 nM.

A novel, high affinity and long-acting antagonist of human M3 muscarinic acetylcholine receptor with pKi of 9.03-9.21.

A novel, dual-acting muscarinic receptor antagonist and β2-adrenoceptor agonist (MABA) with pKi of 9.21/9.53 for hM2/M3, pKi of 9.37 for β2-adrenoceptor.

A novel, cell-permeable, potent and selective inhibitor of MELK kinase domain with IC50 of 37 nM.

A novel, broadly acting non-nucleoside inhibitor of HCV NS5B polymerase with IC50 of 3 nM and 2 nM for GT1b and GT2a, respectively.

A novel uridine nucleotide analog HCV NS5B polymerase inhibitor for treatment of HCV infection combined with Grazoprevir and Ruzasvir..

A novel tubulin inhibitor that inhibits the proliferation of cancer cell lines with IC50 of 0.2-1.0 uM.

A novel synthetic, orally bioavailable TLR4/MD2 ligand, significantly reduces the IL-6 secretion by subsequent challenge with LPS at 0.63 uM.

A novel specific, cell permeant modulator of Kv3 channels with EC50 of 0.9 and 1.9 uM for Kv3.1b and Kv3.2a, respectively.

A novel specific TRPM8 channel antagonist for treatment or prevention vasomotor symptoms..

A novel specific ROCK1 kinase inhibitor with IC50 of 11.2 uM, without inhibitory activity against ROCK2.

A novel specific p110β inhibitor with IC50 of 5.74 nM.

A novel specific CRAC channel inhibitor that blocks function of effector but not regulatory T cells in vitro and attenuates the pogression and severity of EAE in vivo.

A novel sodium glucose transporter type 1 and type 2 (SGLT1/2) inhibitor for the oral treatment of type 2 diabetes..

A novel small-molecule Wnt signaling inhibitor that inhibits TCF-dependent transcription with IC50 of 6.1 uM in 7dF3 reporter assay.

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.