Table 5.
The binding affinities and cooperativity factor (α) values for unlabelled antagonists and chemokines against [125I]CCL17, [3H]compound 5 and [3H]compound 8 in CHO CCR4 membranes. Data are the mean ± SEM of at least three separate determinations with 95% confidence limits shown in parentheses where appropriate
| Radioligand | [125I]CCL17 | [3H]compound5 | [3H]compound8 | |
|---|---|---|---|---|
| Compound | pKi | α | pKi | pKi |
| 1 | 6.34 ± 0.07 | – | 6.21 ± 0.06 | <6.00 |
| 2 | 7.74 ± 0.41 | – | ND | 8.26 ± 0.05 |
| 3 | 8.21 ± 0.141 | 0.14 (0.09, 0.21) | ND | 8.22 ± 0.01 |
| 4 | 8.56 ± 0.08 | – | 8.76 ± 0.06 | ND |
| 5 | 9.10 ± 0.09 | – | 9.14 ± 0.03 | ND |
| 6 | 8.70 ± 0.21 | – | 8.66 ± 0.05 | ND |
| 7 | 7.53 ± 0.05 | – | ND | 7.56 ± 0.04 |
| 8 | 9.04 ± 0.171 | 0.03 (0.02, 0.04) | ND | 9.19 ± 0.04 |
| 9 | 8.74 ± 0.091 | 0.03 (0.02, 0.05) | ND | 8.73 ± 0.07 |
| CCL17 | 9.64 ± 0.10 | – | ND | ND |
| CCL22 | 10.2 ± 0.05 | – | ND | ND |
| CCL223-69 | 8.17 ± 0.09 | – | ND | ND |
| CCL11 | 6.17 ± 0.06 | – | ND | ND |
ND: Ehlert equation not fitted due to poor definition of the individual inhibition curves.
1
Data derived from fitting the equation of Ehlert (1988).