Table 6. Potency of 47 and 49 for Inhibition of Cellular Responses Mediated by the Human CCR4 Receptor.
cell system | assay readout | 47 (pIC50 mean ± SEM) | 49 (pIC50 mean ± SEM) |
---|---|---|---|
inhibition of CCL22 Ca2+ response | MDC-induced Ca2+ flux | 7.5 ± 0.04 (n = 3) (CHO cells expressing hCCR4) | 8.4 ± 0.1 (n = 4) (HEK cells expressing hCCR4) |
inhibition of Th2 cell CCL22 driven chemotaxis in 0.3% HSA | MDC-induced chemotaxis | 6.3 ± 0.2 (n = 3) | 6.8 ± 0.2 (n = 3) |
inhibition of Th2 cell CCL17 driven chemotaxis in 0.3% HSA | TARC-induced chemotaxis | 6.3 ± 0.1 (n = 3) | 6.5 (n = 1) |