Novel CB1R allosteric agonist-positive allosteric modulator (ago-PAM), exhibiting moderate ago-PAM potency and improved aqueous solubility with therapeutic reduction of intraocular pressure in murine glaucoma models

Novel CB1R allosteric agonist-positive modulator (ago-PAM), exhibiting augmented allosteric-agonist and PAM activities in neuronal cultures, improved metabolic stability, and enhanced orthosteric agonist binding (CP55940)

Novel CB1R allosteric agonist biased toward G protein- vs β-arrestin1/2-dependent signaling

Novel potent CB1R ago-PAM

Novel allosteric activator and positive modulator of α7 nicotinic acetylcholine receptors (nAChR), more active (+)-enantiomer of 4BP-TQS

Novel GAS41 YEATS inhibitor, blocking proliferation of NSCLC cells, and modulating expression of GAS41-dependent genes, demonstrating on-target inhibition of GAS41 in cancer cells

Novel acetylcholinesterase inhibitor

Mammalian metabolite, identified in plasma and cerebrospinal fluid from hyperammonaemic patients

Natural antibiotic, displaying potent and selective bactericidal activity against key Gram-positive pathogens (including Staphylococcus aureus and enterococci)

Novel acid-tolerant green RSFP, exhibiting negative switching with especially high contrast in acidic conditions, and its off switching is caused by trans-to-cis isomerization of the chromophore hydroxyphenyl ring that accompanies protonation

Novel male contraceptive agent, blocking spermatogenesis

First-in-class transforming growth factor-β receptor type I inhibitor

Novel inhibitor of galactokinase (GALK)

Novel viral RNA-dependent RNA polymerase (RdRP) inhibitor

Liver-specific magnetic resonance imaging (MRI) contrast agent

Potent and selective

Novel potent competitive γ-aminobutyric acid type A receptor (GABA A R) antagonist (K i = 180 nM), targeting extrasynaptic α4βδ subtype, showing efficiently rescue inhibition of T cell proliferation

Novel G6PD inhibitor, revealing immune dependence on pentose phosphate pathway. depleting NADPH most strongly in lymphocytes, markedly decreasing inflammatory cytokine production in T calls, suppressing respiratory burst in neutrophils

Novel antibacterial and anti-biofilm agent against antibiotic resistant clinical isolates

Inhibitor of NLRP3 inflammasome

Novel fluorescent specific ligand of human telomeric G-quadruplex DNA, binding to both G-tetrad and the lateral loop near the 5-end, reducing the telomere length and downregulating hTERC and hTERT mRNA expression in HeLa cells

Novel potent and highly specific MEK inhibitor (MEKi)

Novel antiviral agent against Rift Valley fever virus (RVFV) by blocking virus budding from the trans Golgi.

Novel, Potent, and Nonsteroidal Farnesoid X Receptor (FXR) Selective Antagonist

Novel potent and selective inhibitor of FXIa, producing a robust and dose-dependent inhibition of both arterial thrombosis and MES

Novel highly potent Factor XIa inhibitor with selectivity against most of the relevant serine proteases

Novel slow-releasing hydrogen sulfide (H2S) donor, inhibiting NF-κB activity and inducing cell apoptosis

Natural neuroprotective agent on glutamate-mediated HT22 cell death, controlling the amount of ubiquinone, up-regulating p21 expression in a p53-dependent manner, decreasing Akt phosphorylation and resulting in increased Fas ligand production and caspase-

Insecticide, acting as an EC 3.1.1.7 (acetylcholinesterase) inhibitor

Novel potent Hepatitis C virus (HCV) NS3/4A protease inhibitor