Novel dual G-quadruplex/i-motif binder, binding to and stabilizing both G-quadruplex and i-motif, being effective in both oncogene replication and transcription

Novel high affinity, potent, and selective stabilizer of the MYC G-quadruplex (G4)., inducing cytotoxicity with corresponding decreased MYC mRNA and altering protein binding to the NHE III1 region

Novel potent and selective ferroptosis inducer, inhibiting glutathione peroxidase 4 (GPX4)

Novel HIV replication blocker (EC 50 = 1.66 μM), being actively against a panel of HIV mutant strains displaying resistance to individual drugs used in antiretroviral therapy

Novel potent GPR88 agonist (EC 50 = 59 nM)

Novel, potent, efficacious, and brain-penetrant GPR88 agonist (cAMP EC 50 = 14 nM)

Highly potent and specific GPR52 antagonist

The first orally active GPR52 agonist

Novel potent GPR52 agonist, dose-dependently suppressing methamphetamine-induced hyperlocomotion in mice

Novel potent GPR120 agonist, exhibiting significant glucose-lowering effect and high selectivity over GPR40

Potent PARP inhibitor

Novel selective non-steroidal agonist of G-protein bile acid receptor 1 (GPBAR1, also known as TGR5 or M-BAR)

Curcumin analog, exhibiting potent growth suppressive activity in human colorectal carcinoma cells

Natural potent inducer of apoptosis in MCF-7 cell lines

Antipsychotic and cognitive enhancer; Dopamine D1 and D2 receptor modulator

Natural inhibitor of Musashi family of RNA-binding proteins

Agonist of the GnRH receptor, inducing the secretion of the gonadotropins follicle-stimulating hormone and luteinizing hormone from the pituitary gland and to increase sex hormone production by the gonads

Dual Glycolate Oxidase/Lactate Dehydrogenase A (GO/LDHA) Inhibitor for Primary Hyperoxaluria

Novel potent GNMT inducer, inhibiting Huh7 cell growth in vitro and xenograft in vivo

Novel inhibitor of Gram-negative lipoprotein trafficking

Natural highly potent HIV latency-reversing agent

Dose dependent up-regulator of the level of E-cadherin in SW620 cells

Novel inhibitor of Plasmodium falciparum, killing both blood- and sexual-stage P. falciparum parasites

Novel Inhibitor of EGF-EGFR Interactions

Novel potent aryl hydrocarbon receptor (AHR) antagonist with the capacity to inhibit both DRE-dependent and -independent activity

Novel selective CHK1 inhibitor

Novel GluN2A-selective NMDA receptor positive allosteric modulator (PAM)

Negative control for GNE-2256

Novel inhibitor of nicotinamide phosphoribosyl transferase (NAMPT)

Novel NMDAR PAM with both an improved pharmacokinetic profile and increased selectivity against AMPARs