Fig. 1.

Pharmacological characterization of Compound A. A–C: equilibrium binding studies and heterologous competition studies of Compound A on CRTH2 and DP1 transfectants. Radioligand binding analysis was performed as detailed in materials and methods, with triplicate wells per concentration of ligand in a minimum of n = 4 separate experiments. D: effect of Compound A on DK-PGD₂-induced calcium mobilization in CRTH2-L1.2 transfectants (representative of n = 3 separate experiments). DK-PGD₂ was used at concentrations ranging from 1 to 100 nM, the trace represented in Fig. 1 being from an experiment using 10 nM. E: lack of competitive inhibition by Compound A on the binding of cognate ligands to prostaglandin, leukotriene, and thromboxane receptors (see materials and methods; triplicate assessments in n = 3 separate experiments).