Potent and selective antagonist of NMDA glutamate receptors containing the NR2B subunit

Selective alpha1A/1L-adrenoceptor partial agonist

Selective antagonist of NMDA receptors NR2B subunits

Novel potent and specific RNA-binding ligand, targeting riboswitches and other RNAs at proximal subsites

Potent, reversible, non-carbonyl inhibitor of fatty acid amide hydrolase (FAAH)

The first irreversible covalent MPS1 inhibitor, targeting a poorly conserved cysteine in the kinase's hinge region

Novel Fluorescent ER-Tracker dye, showing potent cytotoxic activity on several types of cancer cells, being accumulated into the endoplasmic reticulum (ER) as highlighted by its colocalization

Novel MOR agonist

Promising pro-apoptotic agent, showing activity on various cancer cell lines

Novel gastrocolokinetic ghrelin agonist, approximately sixfold greater potency than natural ghrelin

Novel potent and highly selective GPR6 inverse agonist, inhibiting GPR6 cAMP signalling in TR-FRET assays with a EC50 = 16 nM and >100 fold selectivity against GPR3 and GPR12

Novel selective inhibitor of activated fibroblasts, inhibiting the enhanced migration of fibroblasts cocultured with cancer cells by binding to β-arrestin1 and interfering with β-arrestin1-mediated cofilin signaling pathways

Novel potent and selective SIRT2 inhibitor, increasing the acetylation level of eukaryotic translation initiation factor 5A (eIF5A) and reducing cell viability of human breast cancer cells accompanied with a decrease in c-Myc expression

Natural selective inhibitor of protein tyrosine phosphatases (PTPases)

Novel inhibitor of dengue virus NS5 RNA-dependent RNA polymerase (RdRp), inhibiting the DENV type 2 (DENV2) RdRp activities

Novel potent Liver Receptor Homolog-1 (LRH-1) modulator

Highly selective α4β2 subtype nicotinic receptor agonist

Novel peroxisome proliferator-activated receptor gamma (PPARgamma) agonist

Novel IAP-based selective RIPK2 degrader

First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific inhibitor

Natural inducer of apoptosis by significantly upregulating Bcl-2, mitigating expression of Bcl2 in HCT 15 cells and attenuating the apoptotic markers and cell cycle regulatory proteins

Novel antidiabetic agent, impairing glucose uptake by muscle tissue, excessing hepatic gluconeogenesis, and increasing beta-cell apoptosis

HIV-1 reverse transcriptase inhibitor, also acting as an EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor

Natural antibiotic, inhibiting prokaryotic DNA-dependent RNA synthesis and protein synthesis; blocking RNA-polymerase transcription initiation, modulating ß2m aggregation

Antibiotic for tuberculosis (TB) treatment

Selective antagonist of the serotonin 5-HT3 receptor

Potent inhibitor of the Rho pathway

Selective sigma-2 ligand, inducing apoptosis in EMT-6 breast cancer cells

Quorum sensing modulator as a RhlR antagonist

Novel potent and selective RhlR antagonist, strongly inhibiting biofilm formation, and reducing production of virulence factors in P. aeruginosa