Antibiotic, binding within the mRNA channel of the 30S subunit and inhibiting protein synthesis

Novel antimalarial agent, providing protection to malaria-infected mice

Novel mGlu4 ligand

Natural anti-inflammatory agent, inhibiting the NF-κB-mediated transactivation of a luciferase reporter gene, IL-6 production, and COX-2 expression

Natural anti-inflammatory agent, inhibiting the NF-κB-mediated transactivation of a luciferase reporter gene, IL-6 production, and COX-2 expression

Novel inhibitor of the interaction of the N-terminally truncated RXR

Novel inhibitor of the interaction of the N-terminally truncated RXR

Novel norditerpenoid inhibitor of testosterone-5α-reductase

Novel antagonist for proteinase-activated receptor 2 (PAR2)

Novel inhibitor of peptidoglycan synthesis targeting the lipid II precursor

Novel dual CLK1 and CLK3 inhibitor

Novel potent and selective inhibitor of PIM kinases

Potent, highly selective, and irreversible ABHD6 Inhibitor

Inhibitor of all three monoamine transporters

Novel irreversible β-Glucocerebrosidase modulator

Novel β-Glucocerebrosidase modulator, promoting dimerization of β-glucocerebrosidase and revealing an allosteric binding site, stabilizing wild-type and N370S mutant GCase and increases GCase abundance in patient-derived fibroblast cells

Selective modulator of GABAA receptors containing the α5 subunit

Potent vanilloid receptor (VR1) agonist

Potent TRPV1 agonist

High-affinity partial agonist of the vanilloid receptor

Novel BH3 α-helix mimetic, inducing apoptosis in a subset of cancer cells (lung cancer, colon cancer and mesothelioma) by disrupting Bcl-xL and Mcl-1 protein-protein interactions with Bak

Novel potent stimulator of glucagon-like peptide-1 (GLP-1) secretion in vitro, also potently stimulating Ca(2+) influx through TRPA1 cation channels, being one of the most potent non-electrophilic TRPA-1 channel agonists

Potent cannabinoid (CB) receptor agonist

Novel BET selective inhibitor, targeting BRD4

Novel neuroprotective agent, improving cognitive performances in a transgenic mouse model of AD

Novel live-cell peobe of voltage-dependent structural changes of voltage-gated Kv2.1 channels

Specific inhibitor of factor Xa

Novel K(ATP) channel opener

Novel inhibitor of urate transporter 1 (URAT1)

Novel orally active and selective transient receptor potential vanilloid 1 (TRPV1) antagonist