TABLE 3

Inhibition of CCL2-induced cellular responses measured in [35S]GTPγS membrane binding assays as well as β-arrestin recruitment and xCELLigence label-free whole-cell assays

Data are presented as mean ± S.E.M. of three experiments performed in duplicate.

Compound[35S]GTPγS Binding Inhibition IC50 ± S.E.M.β-Arrestin Recruitment Inhibition IC50 ± S.E.M.xCELLigencea IC50 ± S.E.M.
nM
INCB33442.8 ± 0.83.2 ± 0.22.0 ± 0.5
BMS225.5 ± 1.84.8 ± 0.421 ± 6*
RS50439319 ± 7**68 ± 387 ± 15
Teijin183 ± 4867 ± 13292 ± 66*
JNJ-271414913.9 ± 1.0**29 ± 125 ± 4
CCR2-RA-[R]24 ± 325 ± 464 ± 14***
  • a Inhibition of CCL2 was calculated from concentration-response curves derived from peak-analysis of CI changes.

  • * P < 0.05, versus β-arrestin data, analysis of variance (ANOVA), Tukey’s multiple comparison test; **P < 0.05, versus β-arrestin and xCELLigence data, ANOVA, Tukey’s multiple comparison test; ***P < 0.05, versus [35S]GTPγS and β-arrestin data, ANOVA, Tukey’s multiple comparison test.