TABLE 2

Dependence on host cell for binding potencies of selected pyrazinyl-sulfonamides at recombinant 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 HEK-Gqi5 cells as described under Materials and Methods. Inhibition of the specific binding of FB-CCL22 was measured for the same CCR4 antagonists following equilibration with CCR4-CHO cells, also described under Materials and Methods. Fitted estimates of the pIC50 values were measured in separate experiments, and the average and standard error were calculated and are shown (the values in parentheses represent the number of experiments).


Compound

pIC50
CHO Membrane
CHO Cell
HEK Cell
2 8.0 ± 0.40 (7) 7.6 ± 0.10 (6) 7.7 ± 0.20 (7)
6 7.4 ± 0.15 (4) 5.4 ± 0.10 (4) 6.4 ± 0.12 (7)
8
7.6 ± 0.19 (8)
6.5 ± 0.22 (5)
7.5 ± 0.19 (5)