Novel robust and fatigue-resistant photoswitchable GPCR antagonist

Partial agonist in hH 4 R-mediated G protein signalling and β-arrestin2 recruitment, bounding covalently to the hH4R

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

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)

Highly Potent Human Histamine H4 Receptor Inverse Agonist

Potent human H4 receptor inverse agonist

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

Potent H4R ligand

Novel full inverse agonist at CXCR3 N3.35A

Potent histamine H3 receptor silent antagonist

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

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

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

Novel CNS penetrant pan-muscarinic antagonist

Novel M4 positive allosteric modulator (PAM)

Novel Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM)

Novel Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM)

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

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

Novel modulator of mammalian inward rectifying potassium (Kir) channels

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

mGlu1 positive allosteric modulator (PAM)

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

Potent and selective mGlu5 negative allosteric modulator (NAM)

Novel potent and selective metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulator (PAM)

Novel, CNS Penetrant Glucagon-Like Peptide 1 Receptor (GLP-1R) Positive Allosteric Modulator (PAM)

Selective orthosteric M1 antagonist

Highly selective muscarinic M1 PAM

Novel negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety

Novel mGlu4 positive allosteric modulator (PAM)