Novel potent and selective nonpeptide kinin B2 receptor antagonist

5-HT2A/D2 receptor antagonist

Potent, selective and orally bioavailable inhibitor of dipeptidyl peptidase 4 (DPP-4)

Novel Multi-Kinase Inhibitor, Triggering Mitotic Catastrophe of Glioma Stem Cells Mainly through MELK Kinase Inhibition

Inhibitor of cholesterol esterification

Prodrug of melarsen oxide (Mel Ox), irreversibly binding to vicinal sulfhydryl groups on pyruvate kinase, disrupting energy production in the parasite

Natural dual inhibitor of COX-2 and EGFR, improving program death 1 (PD-1) checkpoint blockade therapy through normalizing tumor vasculature and PD-L1 downregulation

Inducer of Megakaryocyte Differentiation in Erythroleukemia Cells, Impairing Bcr-Abl Signaling Cascades

Potent sPLA2 inhibitor, having no effect on arachidonic acid release and platelet activating factor synthesis

Progestational hormone, for the treatment of menstrual irregularities, prostatic hypertrophy, and endometrial carcinoma

Polyketide antibiotic, acting as a AKT selective kinase inhibitor, alkylating a regulatory loop cysteine

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