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. 2017 Sep 1;8(9):981–986. doi: 10.1021/acsmedchemlett.7b00315

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)