TABLE 1

Effect of cell permeabilization to normalize binding potencies in cells and membranes for selected pyrazinyl-sulfonamides at CCR4

Competition for the specific binding of 1 nM [³H]compound 1 was measured for the CCR4 antagonists following equilibration with CCR4 in CHO membranes or cells in the presence or absence of saponin as described under Materials and Methods. Fitted estimates of pIC₅₀ values from separate experiments were calculated, and the average and standard deviation are shown (the values in parentheses represent the number of experiments).