Novel sensitizer of BRAF wild-type melanoma cells to vemurafenib, significantly reducing melanoma cell viability, with limited toxicity for normal human fibroblasts

Natural inhibitor of BACE1

β-Hairpin Octapeptide, acting as a potent mouse melanocortin-4 receptor (mMC4R) antagonist

Novel potent and selective PTP-1B inhibitor

Novel promising spectroscopic probe for inositol 5-phosphatase(s)

Novel Gemini vitamin D analog, targeting CD44-STAT3 signaling and inhibiting breast cancer invasion

Highly selective inhibitor of AChE

Novel BB2 receptor antagonist. attenuating the feeding responses evoked by exogenous gastrin releasing peptide-29

Selective 11beta-hydroxysteroid dehydrogenase type 1 (11betaHSD1) inhibitor

Novel 11β-HSD1 inhibitor

Natural inhibitor of microRNA-21, reducing growth of cancer cells

Potent inducer of anemia

Direct-acting vasodilator with anti-tachycardiac effect

Potent and selective agonist of μ-opioid receptor (MOR) with relatively low affinity for the δ-opioid receptor and the κ-opioid receptor

Negative control for BTZO-1

Novel effective reversible and noncovalent inhibitor of DprE1.

Novel unique Na V modulator, acting as a conspicuous outlier, eliminating fast but not slow inactivation

Novel inhibitor of alpha2beta1 integrin, decreasing average platelet adhesion in individuals with the C/T807T genotype but not in those harboring C807C

The first small-molecule inhibitor with significant selectivity among the KCa2 channel subtypes

Novel potent inhibitor of Bruton’s tyrosine kinase (BTK)

Novel potent and selective covalent inhibitor of Bruton’s tyrosine kinase (BTK), targeting a noncatalytic cysteine residue (Cys481) for covalent bond formation

Novel selective and potent competitive inverse agonist of human GPR43

Novel activator of BtGH84, the first experimentally discovered small molecule activator of a glycoside hydrolase

Novel activator of PC1/3 and inhibitor of PC2

Novel cell-permeable modulator of cellular morphogenesis in yeast and mammalian cells

Novel cell-permeable modulator of cellular morphogenesis in yeast and mammalian cells; Inhibitor of SARS-CoV Mpro activity via intensive H-bond network and hydrophobic interactions

Novel respiratory syncytial virus (RSV) fusion inhibitor

Novel potent inhibitor of both HIV-1 and HIV-2 replication, being also active against the erythrocytic stages of P. falciparum

Novel potent covalent inhibitor of gut bacterial bile salt hydrolases (BSH)

Fluorescent probe visualizing neurofibrillary tangles in Alzheimer's disease