TABLE 2 Intrinsic relative activity (RAi) and relative efficacies of the partial agonist CCR2 ligands
The intrinsic relative activity (RAi) was estimated, using the formula Emax_BEC50_A/Emax_AEC50_B [eq. 25 in Ehlert (2005) and eq. 17 in Ehlert (2008)]. Using the pIC50 determined by heterologous displacement of 125I-CCL2 (Fig. 1, Table 1) as an independent measure of ligand affinity, relative efficacies were also determined [using the formula KBEmax_BEC50_A/KAEmax_AEC50_B, eq. 19 in Ehlert (2008)]. For the analysis of Gαi1 signaling, the data obtained with Gαi1-122-RLuc have been used.