Novel potent and substrate-competitive PTP1B and TCPTP dual inhibitor

Novel Wnt/β-Catenin Inhibitor, Preferentially Inhibiting the Growth of Breast Cancer Stem-like Cells

Potent antimalarial agent against Plasmodium falciparum 3D7

Potent antimalarial agent against Plasmodium falciparum 3D7

Novel orally efficacious antimalarial agent against P. falciparum 3D7 ( IC50: 51 nM)

Potent serine protease inhibitor, targeting the S 2 S 3 thrombin and FXa subsites

Direct thrombin inhibitor, preventing occlusive arterial and venous thrombosis in a canine model of vascular injury

Novel potent and selective inhibitor of PI5P4Ks

Inhibitor of PIM, suppressing cyclin-Dependent Kinase 2 (CDK2)

Novel potent pregnane X Receptor (PXR) agonist

Novel dual PXR and AhR agonist

Potent anti-cancer agent

Inducer of demyelination and motor dysfunction via upregulation of IGF-1

Agonist for the cannabinoid receptors, with Ki values of 59.21 nM at CB1 and 136.38 nM at CB2 and EC50 values of 11.98 nM at CB1 and 16.2 nM at CB2

5-HT1A receptor agonist

Novel r(CUG) repeat expansion cleaver, specifically recognizing the 3-dimensional structure of r(CUG)exp, cleaving it more selectively among transcripts containing short, nonpathogenic r(CUG) repeats than an oligonucleotide that recognizes RNA sequence vi

Novel fluorescent RXR agonist

Novel Serotonin 5-HT 2C Receptor Positive Allosteric Modulator (PAM) with Enhanced Drug-like Properties

Inhibitor of prostate-specific membrane antigen (PSMA)

Novel anticancer agent, effectively killing multi-drug resistant cancer cells and a panel of different cancer cells originated from a variety of different tissues including breast and skin, preventing tubulin polymerization, leading to the cell cycle arre

Novel anticancer agent, effectively killing multi-drug resistant cancer cells and a panel of different cancer cells originated from a variety of different tissues including breast and skin, preventing tubulin polymerization, leading to the cell cycle arre

Novel cell permeable degrader of BRD4

Novel potent dual inhibitor of ALK and c-Met

Dual inhibitor of angiogenesis and lysophosphatidic acid acyltransferase

Novel G9a (EHMT2) inhibitor, binding tightly inside the active site cavity of G9a, inhibiting the activity of G9a in both enzyme and cell based assays with much lesser toxicity than BIX-0129

Novel substrate-competive c-Src inhibitor

Novel modulator of PI3K and NF-κB activities, blocking migration and production of inflammatory mediators

Novel photoisomerizable potent and selective M1 ligand, mimicing the tricyclic chemical structure and display reversibly controlled activity, showing stronger inhibition upon illumination both in vitro and in cardiac atria ex vivo

Inhibitor of gene products associated with cell survival, proliferation, invasion, and angiogenesis, targeting NF-κB pathway, showing antiproliferative activity and unique mode of action

Novel water-soluble, potent, and selective TRPM8 receptor agonist