Novel potent mGlu4 PAM with an attractive DMPK profile, and robust efficacy in preclinical Parkinsons disease model, haloperidol-induced catalepsy (HIC)

mGlu1 positive allosteric modulator (PAM)

Novel cyclooxygenase-1 (COX-1)-selective inhibitor

Novel modulator of mammalian inward rectifying potassium (Kir) channels

Novel selective negative allosteric modulator (NAM) of metabotropic glutamate receptor subtype 2

Novel potent and highly selective mGlu1 PAM (22nM), reducing striatal DA release in vivo and displaying antipsychotic efficacy

Novel Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM)

Novel Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM)

Novel M4 positive allosteric modulator (PAM)

Novel CNS penetrant pan-muscarinic antagonist

Novel PAM of Group III (mGlu4/6/7/8) mGlu receptors

Novel selective mGlu3 NAM, showing efficacy in tail suspension, elevating zero maze and marble burying, suggesting selective inhibition of mGlu3 affords anxiolytic-like and antidepressant-like phenotypes in mice

First-in-class selective mGlu7 positive allosteric modulator (PAM), displaying CNS penetration in both mice (Kp = 2.74) and rats (Kp= 4.78)

Potent histamine H3 receptor silent antagonist

Novel full inverse agonist at CXCR3 N3.35A

Potent H4R ligand

Novel potent ligand at 5-HT3A and 5-HT3AB receptors with different activities

VUF10497 is a potent histamine H4 receptor (H4R) inverse agonist with anti-inflammatory activity.

Potent human H4 receptor inverse agonist

Highly Potent Human Histamine H4 Receptor Inverse Agonist

Potent CXCR3 Antagonist, extending from the minor pocket into the major pocket of the transmembrane domains and binding between residues in helices 1 (Y1.39), 2 (W2.60), 3 (F3.32), 4 (D4.60), 6 (Y6.51), and 7 (S7.39, Y7.43)

First reported nonpeptidomimetic agonist on The G protein-coupled chemokine receptor CXCR3