Displacement of 125I-CCL2, [3H]INCB3344, and [3H]CCR2-RA from U2OS membranes expressing CCR2
Data are presented as mean ± S.E.M. of at least three experiments performed in duplicate.
| Compound | 125I-CCL2 Displacement IC50 ± S.E.M. | [3H]INCB3344 Displacement Ki ± S.E.M. | [3H]CCR2-RA Displacement Ki ± S.E.M. |
|---|---|---|---|
| nM | nM or % binding | ||
| CCL2 | 0.19 ± 0.04 | 79 ± 2%a | 77 ± 4%a |
| INCB3344 | 5.4 ± 0.8 | 1.2 ± 0.1 | 169 ± 17%b* |
| BMS22 | 27 ± 4 | 5.1 ± 1.3 | 164 ± 16%b* |
| RS504393 | 132 ± 25 | 62 ± 3 | 157 ± 16%b* |
| Teijin | 220 ± 26 | 107 ± 10 | 159 ± 17%b* |
| JNJ-27141491 | 172 ± 15 | 112 ± 3%b* | 12 ± 3 |
| CCR2-RA-[R] | 103 ± 18 | 109 ± 1%b* | 5.0 ± 0.8 |
↵a Percentage of radioligand binding in the presence of 100 nM CCL2. 100% was determined in the presence of buffer, and therefore values <100% represent displacement.
↵b Percentage of radioligand binding in presence of 1 μM antagonist. 100% was determined in the presence of buffer, and therefore values >100% represent enhancement.
↵* P < 0.05, Student’s t test.