Novel peroxisome proliferator activated receptor γ (PPARγ) ligand

Novel peroxisome proliferator activated receptor

Novel Inhibitor of BAF, activating latent HIV-1

Novel potent and nonselective MC3R and MC4R macrocyclic agonist. decreased food intake and respiratory exchange ratio (RER)

Novel potent and highly selective melanocortin-3 receptor (MC3R) agonist, showing greater than 140-fold selective for the mMC3R over the mMC4R, possessed 70 nM potency at the mMC3R, and partially stimulated the mMC4R at 100 μM concentrations without antag

Novel MC5R antagonist

Novel proteolysis-resistant self-localizing ligand (SL), sustaining PM localization of eDHFR-fusion proteins (over several hours to a day), inducing prolonged signal activation and cell differentiation

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