Novel γ-secretase modulator photoaffinity probe, identifying distinct allosteric binding sites on presenilin that can be exploited to reduce levels of pathogenic Aβ species

Novel potent, orally available GPBAR1 agonist

Orally active chemokine receptor CCR2 antagonist preventing glomerulosclerosis and renal failure in type 2 diabetes

Novel Glucokinase Activator for the Treatment of Type 2 Diabetes

Novel highly potent dual NK1/NK3 receptor antagonist

Selective negative allosteric modulator of mGlu3

Novel mGlu2/3 negative allosteric modulator (NAM)

Beta(1) adrenoceptor-selective agonist

Potent and selective inhibitor of the p38 MAPK catalytic domain

Dual inhibitor of HDAC and MMP

Novel reversible inhibitor of interleukin-2 (IL-2)

Vitamin D analogue, showing significant in vitro and in vivo antitumor activity.

Potent and selective Candida albicans N-myristoyltransferase (CaNmt) inhibitor, exhibiting antifungal activity in vivo

Potent and selective Candida albicans N-myristoyltransferase (CaNmt) inhibitor

NMDA receptor antagonist , specifically suppressing the severe autoimmune phenotypes of chs3-2D (chilling sensitive 3, 2D), including the arrested growth morphology and heightened PR (Pathogenesis Related) gene expression

Novel NR2B selective, non-competitive, voltage-independent antagonist

Selective, non-competitive Metabotropic_glutamate_receptor>mGlu2 antagonist

Competitive AMPA receptor antagonist

ADAM17-selective inhibitor

Potent protein kinase C (PKC) inhibitor

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