Competitive, reversible antagonist of the orphan receptor GPR35 (Ki
= 12.8 nM). Blocks the GPR35-mediated increase in ERK1/2 phosphorylation and β
-arrestin recruitment induced by pamoic acid
(Cat. No. 4298).
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Targeting of the orphan receptor GPR35 by pamoic acid: a potent activator of extracellular signal-regulated kinase and β-arrestin2 with antinociceptive activity.
Zhao et al.
Antagonists of GPR35 display high species ortholog selectivity and varying modes of action.
Jenkins et al.