TABLE 4

G protein activation by CCL2 measured by [35S]GTPγS binding

Potency and maximum effect of CCL2 in the absence or presence of different concentrations of CCR2-RA-[R]. Data are presented as mean ± S.E.M. of at least three experiments

pEC50 ± S.E.M.Emax ± S.E.M. (%)
Control8.3 ± 0.1104 ± 4
+1 nM INCB33447.6 ± 0.1*103 ± 7
+3 nM INCB33447.0 ± 0.3*102 ± 14
+10 nM INCB33446.2 ± 0.9ND
+10 nM CCR2-RA-[R]7.7 ± 0.1*81 ± 6**
+30 nM CCR2-RA-[R]7.7 ± 0.1*55 ± 4***
+100 nM CCR2-RA-[R]7.6 ± 0.1*30 ± 3***
  • ND, not determined.

  • * P < 0.05; **P < 0.001; ***P < 0.0001 versus control, Student’s t test.