TABLE 3.
Binding and signaling parameters of CCR2
Binding and functional parameters were measured on HEK293 or CHO-K1 cells expressing CCR2. The pIC50, pEC50, and Emax values were obtained from experiments as displayed in Figs. 2, 7, 8, and 9. The values represent the means ± S.E. of at least three independent experiments. ND, not determined.
| Ligands | [125I]CCL2 |
Gαi1 |
Gαob |
Gα12 |
β-Arr2 |
cAMP |
Ca2+ |
|||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| pIC50 | pKi | pEC50 | Emax | pEC50 | Emax | pEC50 | Emax | pEC50 | Emax | pEC50 | Emax | pEC50 | Emax | |
| CCL2 | −9.6 ± 0.1 | −10.0 ± 0.1 | −8.7 ± 0.2 | −0.13 ± 0.01 | −8.0 ± 0.1 | −0.15 ± 0.01 | −8.4 ± 0.4 | −0.042 ± 0.004 | −8.5 ± 0.1 | 0.14 ± 0.01 | −9.1 ± 0.3 | 31 ± 4 | −8.2 ± 0.1 | 86 ± 5 |
| CCL7 | −9.2 ± 0.1 | −9.6 ± 0.1 | −8.4 ± 0.2 | −0.10 ± 0.01 | −8.2 ± 0.1 | −0.12 ± 0.01 | −8.2 ± 0.2 | −0.030 ± 0.003 | −7.7 ± 0.1 | 0.12 ± 0.01 | −9.3 ± 0.2 | 29 ± 4 | −7.5 ± 0.2 | 86 ± 8 |
| CCL8 | −8.5 ± 0.1 | −8.9 ± 0.1 | −8.5 ± 0.2 | −0.06 ± 0.01 | −8.8 ± 0.4 | −0.05 ± 0.01 | ND | ND | −7.7 ± 0.1 | 0.03 ± 0.01 | −8.4 ± 0.2 | 31 ± 4 | ND | ND |
| CCL13 | −7.9 ± 0.1 | −8.3 ± 0.1 | −8.5 ± 0.4 | −0.06 ± 0.01 | −7.9 ± 0.2 | −0.08 ± 0.01 | ND | ND | −7.0 ± 0.1 | 0.14 ± 0.01 | ND | ND | ND | ND |