Table 4. Effects of Compounds 39 and 43 in Chemokine-Stimulated [35S]GTPγS Bindinga.
| receptor | compd | pEC50 ± SEM (EC50, nM) | Emax ± SEM (%)b |
|---|---|---|---|
| hCCR2 | CCL2 | 8.10 ± 0.06 (8) | 107 ± 2 |
| CCL2 + 10 nM 39 | 7.89 ± 0.04 (13) | 91 ± 1** | |
| CCL2 + 30 nM 39 | 7.60 ± 0.07 (26)** | 75 ± 4**** | |
| CCL2 + 100 nM 39 | 7.27 ± 0.10 (56)**** | 50 ± 3**** | |
| CCL2 + 1 nM 43 | 7.91 ± 0.10 (13) | 72 ± 4**** | |
| CCL2 + 3 nM 43 | 7.53 ± 0.12 (32)*** | 51 ± 5**** | |
| CCL2 + 10 nM 43 | 6.87 ± 0.13 (148)**** | 33 ± 3**** | |
| hCCR5 | CCL3 | 8.42 ± 0.06 (4) | 108 ± 2 |
| CCL3 + 100 nM 39 | 8.35 ± 0.09 (5) | 79 ± 5**** | |
| CCL3 + 300 nM 39 | 8.14 ± 0.12 (8) | 56 ± 2**** | |
| CCL3 + 1000 nM 39 | 8.14 ± 0.17 (9) | 25 ± 4**** | |
| CCL3 + 30 nM 43 | 8.30 ± 0.05 (5) | 81 ± 3**** | |
| CCL3 + 100 nM 43 | 8.21 ± 0.05 (6) | 58 ± 1**** | |
| CCL3 + 300 nM 43 | 8.05 ± 0.06 (9)* | 35 ± 2**** |
a
Data represent the mean ± standard error of the mean (SEM) of three independent experiments performed in duplicate. One-way ANOVA with Dunnett’s post hoc test was used to analyze differences in pEC50 and Emax values against CCL2 or CCL3 controls.
b
Maximum effect (Emax) of CCL2 or CCL3 measured in the absence or presence of fixed concentrations of compound 39 and 43 in CCR2 or CCR5, respectively.