Novel partial PPARgamma ligand, displaying partial agonist activity in biochemical and cell-based transactivation assays, and reversed insulin resistance

Novel valproic acid (VPA) derivative, as a potent STAT3 inhibitor

Diuretic agent, impling an increase in the Na+ excretion and showing antihypertensive effect

First-in-class highly potent PROTAC degrader of MDM2

Novel SARS-CoV-2 Main Protease (Mpro) inhibitor, binding to Subsites S1 and S2 (Kd=1.3 µM)

Novel highly selective inhibitor of monocarboxylate transporter 4 (MCT4/SLC16A3), resulting in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells

Novel potent and selective inhibitor of the apoptosis regulating proteins Mcl-1

The first reversible covalent inhibitor for Mcl-1, a protein-protein interaction (PPI) target

Novel selective Mcl-1 inhibitor

Novel reversible covalent inhibitor for Mcl-1 with improved water solubility than Mcl-1 Inhibitor-5

Novel potent and selective degrader of Mcl-1

Novel inhibitor of p53-MDM2 interaction

Selective NA reuptake inhibitor with 5-HT3 receptor antagonism

Novel potent F508del-CFTR corrector, modulating poly-ADP ribose polymerase 3 and poly-ADP ribose polymerase 16 activities

Albumin-binding prodrug of Doxorubicin

Novel inverse agonist for the pancreatic-type ATP-sensitive K channel as vascular relaxing agent

First-in-class inhibitor of MFS efflux pump CaMdr1p

Novel selective inhibitor of the Polo-box domain of Polo-like kinase 1 (PLK1)

Specific and highly fluorescent substrate for caspase-1, also acting as a substrate for caspase-4

Novel neurotropic agent

Potent P-gp inhibitor with good selectivity towards BCRP pump (EC50 values 0.05 μM, 0.69 μM, 9.3 μM, and 73 μM for Caco-2, MDR1, MRP1, and BCRP inhibition, respectively)

Novel hybrid retinoid-HDAC inhibitor

Novel selective PARP1 inhibitor, inhibitng apoptosis and blocking poly ADP-ribosylation of histone H1 in hydrogen peroxide treated SH-SY5Y neuroblastoma cells

The first inhibitor of forkhead Box Protein C2 (FOXC2)

Novel potent acetylcholinesterase (AChE) inhibitor

Potent and HDAC class I-selective inhibitor

Topical nonnucleoside reverse transcriptase inhibitor, partially preventing vaginal RT-SHIV infection of macaques

Novel specific inhibitor of HA-mediated viral entry, inhibiting HPAI H5N1 virus strain A/Hong Kong/H5N1

Antibacterial agent, with a relatively narrow spectrum against bacteria and a very high CC 50 value

Novel antibacterial agent, remarkably potent against antibiotic-resistant bacterial strains such as MDR A. baumannii , ESBL-producing Klebsiella pneumoniae, VRE, and MRSA