TABLE 2

ML-145 displays greater potency as an antagonist at human GPR35 than CID-2745687

Human GPR35-β-arrestin-2 interaction assays were conducted by using EC80 amounts of the indicated agonists and varying concentrations of either ML-145 or CID-2745687. In all cases a maximally effective concentration of either antagonist ligand was able to fully reverse the effects of the agonist ligand. Data are means ± S.E.M. from nine independent experiments.

AgonistAntagonist
ML-145CID-2745687
Zaprinast7.57 ± 0.076.70 ± 0.09
Cromolyn disodium7.65 ± 0.076.27 ± 0.08
Pamoate8.08 ± 0.127.16 ± 0.12