Inhibitor of NLRP3 inflammasome

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

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 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

Potent and selective

GAC0003A4 is an LXR inverse agonist that inhibits LXR transcriptional activity. GAC0003A4 also efficiently degrades LXRβ protein. GAC0003A4 has the potential to be used in advanced pancreatic cancer and other refractory malignancies.

Novel LXR inverse agonist, functioning as LXR a degrader, significantly reducing LXR protein levels in PDAC cell lines

Liver-specific magnetic resonance imaging (MRI) contrast agent

Novel viral RNA-dependent RNA polymerase (RdRP) inhibitor

Novel inhibitor of galactokinase (GALK)

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

Novel male contraceptive agent, blocking spermatogenesis

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

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

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

Novel acetylcholinesterase inhibitor

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

Novel potent CB1R ago-PAM

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

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