Novel potent RORγt inverse agonist

Novel RORγt agonist

Novel RORgammaT inhibitor

Novel potent and selective RORγt agonist, showing robust antitumor efficacy in syngeneic tumor models and improving the efficacy of anti‑PD‑1 in a murine lung cancer model

The first potent inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt

Allosteric modulator of dextromethorphan binding to high-affinity sigma receptors

Novel p38α kinase inhibitor; Antioxidant

Lipid modifying agent; Antihyperlipidemic and antiarteriosclerotic

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

Novel potent and selective ROCK inhibitor

Novel potent and selective ROCK inhibitor

Novel potent and selective ROCK inhibitor

Potent Rho--​kinase (ROCK) inhibitor

Novel potent ROCK inhibitor

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

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

Selective antagonist at the 5-HT1A receptor

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

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

Potent γ-secretase modulator (GSM)

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