Novel, potent, and systemically bioavailable mGlu2/3 receptor agonist, exhibiting both antipsychotic and analgesic properties in vivo

Orally active cell-permeable inhibitor of human

Potent 5-HT3 serotonin receptor antagonist

Selective negative allosteric modulator of mGlu3

Potent antioxidant, being cytoprotective in models of focal and global cerebral ischemia

Novel mGlu2/3 receptor agonist; Prodrug of LY-404039

Novel glucokinase activator (GKA)

Novel, potent, orally-bioavailable kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders

Novel LRRK2 kinase inhibitor against the wild-type and G2019S mutant LRRK2 kinase being 1526.00 ± 0.87 nM, 1165.00 ± 1.18 nM, respectively

Novel LRRK2 kinase inhibitor against the wild-type and G2019S mutant LRRK2 kinase being 424.40 ± 1.31 nM, 378.80 ± 1.20 nM, respectively

Novel potent HIF-1 inhibitor, also downregulating the protein level of HIF-1alpha, which depended on von Hippel-Lindau for proteasome degradation, showing in vivo anticancer efficacy by decreasing the HIF-1alpha expression in nude mice bearing MX-1 tumor

Novel Manassantin A Derivative, Inhibiting Hypoxia-Inducible Factor 1 and Tumor Growth

Novel selective LXRβ agonist, reducing total brain Aβ

Novel Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma

Immune modulator with SARS-CoV-2 antiviral activity via a multi-target mechanism including localized, self-limiting reactive oxygen species (ROS) scavenging activities that were demonstrated in a model of lipopolysaccharide (LPS)-induced joint inflammatio

Novel inhibitor of heat shock protein 90 (Hsp90)

Thiazolidine-containing cyclic peptide antibiotic, suppressing growth of species of disease-causing bacteria in that part of the human microbiome

Hybrid ortho/allosteric ligand of the adenosine A(1) receptor

Human adenosine A1 receptor antagonist

A1 adenosine receptor antagonist

Potent mGlu5 receptor positive allosteric modulator (PAM)

Potent and selective adenosine A2A receptor antagonist

Novel β2i-specific inhibitor, displaying moderate trypanocidal activity

Novel potent β2c-specific inhibitor, displaying moderate trypanocidal activity

Novel β2-specific inhibitor, potently targeting both β2c and β2i, displaying moderate trypanocidal activity

Novel potent and selective LMP2 inhibitor, also inhibiting mouse 20S proteasomes

Novel, potent, selective and brain penetrant positive allosteric modulator of alpha-7 nicotinic acetylcholine receptors

Novel potent and selective inhibitor of LRRK2, inhibiting LRRK2 WT, the overactive variant G2019S, and the resistant mutant A2016T56 at 12 nM, 19 nM and 93 nM, respectively

Novel potent and selective hA2A receptor antagonist

Brain penetrant high affinity α1A-adrenoceptor ligand