Novel mGlu2/3 negative allosteric modulator (NAM)

Selective negative allosteric modulator of mGlu3

Novel highly potent dual NK1/NK3 receptor antagonist

Novel Glucokinase Activator for the Treatment of Type 2 Diabetes

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

Novel potent, orally available GPBAR1 agonist

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

Potent γ-secretase modulator (GSM)

Novel potent and selectve LPA1 antagonist, attenuating NHLF human lung fibroblast cell proliferation and contraction in vitro, reducing plasma histamine levels in mouse LPA-challenge model

Novel potent γ-secretase modulator (GSM) with high solubility, balanced lipophilicity, and showing no phototoxicity and PIK4CB side bing activity

Selective antagonist at the 5-HT1A receptor

Platelet-activating factor (PAF-R) antagonist, selectively for intracellular PAF binding sites

Novel potent competitive inhibitor of Rho-associated coiled-coil-containing protein kinase 2 (ROCKII)

Novel potent ROCK inhibitor

Potent Rho--​kinase (ROCK) inhibitor

Novel potent and selective ROCK inhibitor

Novel potent and selective ROCK inhibitor

Novel potent and selective ROCK inhibitor

Anti-cancer agent, acting through gastrin antagonism and H /K -ATPase inhibition, modulating apoptosis pathways, antidyslipidemic, antiadipogenic, gastroprotective, antifertility, and antileishmanial

Lipid modifying agent; Antihyperlipidemic and antiarteriosclerotic

Novel p38α kinase inhibitor; Antioxidant

Allosteric modulator of dextromethorphan binding to high-affinity sigma receptors