Novel potent and selective agonist of dopamine D 2 receptor (D 2 R; K i = 4.58 nM)

Novel dopamine D2 receptor antagonist as a potent multi-target ligand of aminergic G protein-coupled receptors (GPCRs) which dose-dependently stimulates growth, survival of neurons, and promotes their integrity

Novel ERK2 inhibitor

Promoter of spinal muscular atrophy (SMA)

Novel antiviral agent, blocking microtubule polymerization, disrupting the Golgi complex and inhibiting viral trafficking to the plasma membrane during virus egress

Novel potent, selective and metabolically stable LRRK2 inhibitor

Highly potent and selective H4R antagonist

Unique first-in-class antibiofilm antibiotic for biofilm-related wound infections caused by Acinetobacter baumannii

Unique first-in-class antibiotic, being more effective at killing pathogenic methicillin resistant Staphylococcus aureus (MRSA) bacteria than two clinical gold-standard antibiotics-vancomycin and gentamicin

Inhibitor of cysteine protease

Inhibitor of cholinesterase activity, β-amyloid aggregation and Ca overload; Novel multi-target-directed ligand (MTDL); Activator of kinase 1 and 2 (ERK1/2) and Akt/protein kinase B (PKB) pathways

NRAS inhibitor, targeting the post-translational S-palmitoyl modification of NRAS, causing a dose-dependent decrease in NRAS palmitoylation and inhibiting downstream signaling in melanoma cells with an activating mutation in NRAS

Inhibitor of Pentaglycine Interpeptide Bridge Synthesis

Novel potent tri-vector cyclophilin inhibitor

Novel non-peptidic inhibitor of cyclophilin D as neuroprotective agents in Aβ-induced mitochondrial dysfunction

Novel CypD inhibitor, binding strongly to CypD and attenuating mitochondrial and cellular perturbation insulted by Aß and calcium stress

Novel fungal lanosterol 14α-demethylase (CYP51)/histone deacetylase dual inhibitor, blocking ergosterol biosynthesis and HDAC catalytic activity in fungus, suppressing the function of efflux pump, yeast-to-hypha morphological transition, and biofilm forma

Novel covalent allosteric CYP3A4-effector

Novel potent and selective CYP1A1 inhibitor, antagonizing B[a]P mediated activation of aromatic hydrocarbon receptor (AhR) in yeast cells, and protecting human cells from CYP1A1-mediated B[a]P toxicity in human cells

Potent and selective human CYP11B1 inhibitor

Novel short-acting KOR antagonist

Novel non-peptidic NPBWR1 (GPR7) antagonist

Novel S1PR4 antagonist

Cyclic alkylaminoluciferin substrate for firefly luciferase

Non-peptidic, potent, and orally active stromelysin inhibitor;

Cyclic alkylaminoluciferin substrate for firefly luciferase, emitting 4.7-fold more light than aminoluciferin, and 2.6-fold more light than D-luciferin

immunosuppressive agent

Macrocyclic immunosuppressive peptide, exhibiting a higher plasma concentration than Cyclophilin A

Immunosuppressant

Immunosuppressant