Fig. 10.

CID-2745687 and ML-145 block both constitutive and agonist-mediated IP₁ accumulation only at the human ortholog of GPR35. The capacity of varying concentrations of ML-145 (A) or CID-2745687 (B) to limit IP₁ accumulation in response to EC₈₀ concentrations of zaprinast (left), pamoate (center), or cromolyn (right) was assessed in cells transfected to express the noted ortholog of FLAG-GPR35-eYFP with G_q135. Note the marked reduction of IP₁ below basal levels (defined as 0% on y-axis), which is indicative of inverse agonism, produced by higher concentrations of ML-145 (A) and CID-2745687 (B) at the human ortholog.