Potent and Selective Inhibitor of the Norepinephrine Transporter

Inhibitor of matrix metalloproteinase-1 (MMP-1)

Potent and selective inhibitor of matrix metalloprotease MMP-13 (Collagenase-3)

Inhibitor of human collagenase-3 (MMP-13)

ATP-sensitive potassium channel opener

SGLT2 inhibitor

Very late adhesion molecule 4 (VLA-4) antagonist, inhibiting VLA-4/VCAM-1 ligation as a means of modulating eosinophil functions beyond its action on cell adhesion and migration

Nocel inhibitor of BMI1 promoter activity, decreasing BMI1 protein levels in HCT116 human colon carcinoma cells, significantly reducing levels of the CSC biomarker epithelial cell adhesion molecule and diminishing the self-renewal capability of CSCs

Mixed competitive/noncompetitive inhibitor of

Calmodulin antagonist, inhibiting Ca2+/calmodulin-regulated enzyme activities

Novel Probe of Putative MOR-CCR5 Heterodimers to Inhibit Opioid Exacerbated HIV-1 Infectivity

Allosteric modulator of A3 adenosine receptors

Potent histamine H4 receptor full agonist

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