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

Fluorescent probe, binding to neurofibrillary tangles with high contrast and selectivity over amyloid

Fluorescent probe in vitro and in vivo aiming at a tau-based diagnosis of Alzheimer's disease

Novel proteasome inhibitor, protecting against cerebral ischaemia through HIF1A accumulation and enhanced angioneurogenesis

Protein kinase C (PKC) activator

Novel Ca V channels blocker, binding in the central cavity of the pore on the intracellular side of the selectivity filter, physically blocking the ion-conducting pathway

Novel PTP1B inhibitor

Antitumor agent

Mucolytic agent used in the treatment of respiratory disorders associated with viscid or excessive mucus.

Inhibitor of the reuptake of both dopamine and serotonin in the brain

Reversible inhibitor of monoamine oxidase A, acting on epinephrine, norepinephrine, serotonin, and dopamine

Highly κ/μ-selective potent κ ligand

Active-site-directed inactivator of bacterial beta-lactamases

Novel water-soluble, DNA-binding photosensitizer for the eradication of both Gram-negative and Gram-positive bacteria

Novel specific inhibitor of the hypomorph growth of EfpA, a largely uncharacterized, but essential efflux pump in Mtb

Novel inhibitor of dihydroorotate dehydrogenase (DHODH), showing in vitro activity against multidrug-resistant blood-stage parasites

Novel specific inhibitor of the hypomorph growth