Selective FXR antagonist, ameliorates glucose homeostasis in type 2 diabetic mice

Potent and efficacious mobilizing agent of hematopoietic stem and progenitor cells (HSPCs), activating MMP-9 expression and disrupting the SDF-1α/CXCR4 axis, exhibiting more significant mobilizing effects than G-CSF or AMD3100

Novel selective inhibitor of succinate dehydrogenase (complex II) of dermatophyte species

Potent ligand of the central CB1 receptor

Novel inhibitor of the MDM2-p53 interaction

Novel potent dual MDM2/XIAP inhibitor

Potent Peptide dual inhibitor of MDM2/X, inhibiting p53 interactions with MDM2 (IC50 = 10 nmol/L) and MDMX (IC50 = 100 nmol/L), inducing apoptosis and cell cycle arrest of cell lines with overexpressed MDM2/X

Dual inhibitor of angiotensin-converting enzyme and neutral endopeptidase

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