Full agonist of hH4R with ~300-fold selectivity over hH3R and hH2R, but showing potent inverse agonistic activity at hH1R

Novel full inverse agonist at CXCR3 N3.35A

Adenosine A3 receptor (A3AR) allosteric modulator

H3R inverse agonist

Histamine H3 receptor antagonist

Novel photoswitchable modulator of the CXCR3 chemokine receptor

Novel CXCR3 ligand, photoswitching from antagonism to agonism

Novel photoswitchable modulator of the CXCR3 chemokine receptor

Novel inhibitor of Hbp secretion, activating σE stress, impairing Hbp secretion and decreasing the abundance of OMPs, consistent with impaired BAM function

Novel robust and fatigue-resistant photoswitchable GPCR antagonist

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