Novel CCR5 inhibitor, inhibiting the replication of wild-type R5-HIV-1

Novel, potent, and selective G protein-coupled receptor kinase 6 (GRK6) inhibitor with an IC50 value of 6 nM against GRK6 and selectivity against a panel of 85 kinases

Novel potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor

Natural Potent Inhibitor for Glioblastoma Stem Cell via Targeting RHOA and PI3K/AKT

Novel oral specific TRPV1 antagonist, decreasing bladder overactivity and noxious bladder input in cystitis animal models

Novel orally available, potent and selective inhibitor of Transient Receptor Potential Ankyrin 1 (TRPA1) with IC50 value less than 10 nM

Natural blocker of the voltage-gated sodium channels located in the cell membrane of neurons

Novel Nrf2 modulator via a thus far uncharacterized mechanism

Potent 5HT3 antagonist

Bacterial siderophore with a diazeniumdiolate ligand system

5-HT3 receptor antagonist

5-HT1B/5-HT1D serotonin receptor antagonist

Novel inhibitor of the EGFr and C-erbB-2.

Selective and brain penetrant NK1-receptor antagonist

Negative control for GI181771X

Potent TrkA kinase inhibitor

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