Affinity (pKd or pKi) of CXCR2 ligands at in silico based site-directed mutagenesis human CXCR2 mutants
Displacement of 125I-CXCL8 binding to COS-7 cell membranes expressing indicated human single point mutants. The data are presented as mean ± S.E.M. of at least three independent experiments.
| CXCR2 | pKd CXCL8 | pKi | |
|---|---|---|---|
| SB265610 | Compound 1 | ||
| WT | 9.40 ± 0.14 | 7.68 ± 0.11 | 7.18 ± 0.13 |
| S1072.63A | 9.09 ± 0.07 | 7.10 ± 0.13 | 6.73 ± 0.09 |
| F1303.36A | 9.65 ± 0.29 | 7.55 ± 0.17 | <4 |
| Q2165.43E | 9.01 ± 0.12 | 7.56 ± 0.09 | 6.47 ± 0.11 |
| F2205.47L | 9.06 ± 0.05 | 7.34 ± 0.12 | 6.07 ± 0.08 |
| L2716.55A | 9.18 ± 0.12 | 6.76 ± 0.31 | 6.22 ± 0.04 |
| E3007.39S | 9.04 ± 0.13 | 7.21 ± 0.12 | 6.79 ± 0.05 |
| E3007.39Q | 9.00 ± 0.14 | 7.26 ± 0.09 | 6.69 ± 0.09 |