Affinity (pKd or pKi) and inhibition of CXCL8-induced [35S]GTPγS binding (pKb) of CXCR2 ligands at key constructs
Displacement of 125I-CXCL8 binding to COS-7 cell membranes expressing indicated key receptors. The data are presented as mean ± S.E.M. of at least three independent experiments. CXCL8 stimulated [35S]GTPγS binding to COS-7 membranes expressing indicated receptors and inhibition of CXCL8-induced [35S]GTPγS after 30 min before incubation with SB265610 and compound 1. The data are presented as mean ± S.E.M. of at least three independent experiments.
| CXCR2 | pKd CXCL8 | pKi | pEC50 CXCL8 | pKb | ||
|---|---|---|---|---|---|---|
| SB265610 | Compound 1 | SB265610 | Compound 1 | |||
| Human WT | 9.40 ± 0.14 | 7.68 ± 0.11 | 7.18 ± 0.13 | 7.06 ± 0.07 | 8.71 ± 0.06 | 7.48 ± 0.13 |
| Baboon WT | 9.33 ± 0.08 | 7.28 ± 0.10 | <4 | 7.86 ± 0.06 | 8.51 ± 0.13 | <4 |
| Human S2175.44T/N2686.52H | 9.43 ± 0.20 | 7.27 ± 0.16 | <4 | 7.03 ± 0.07 | 8.73 ± 0.07 | <4 |
| Baboon T2125.44S/H2636.52N | 9.61 ± 0.08 | 7.13 ± 0.17 | 7.40 ± 0.14 | 7.68 ± 0.06 | 8.11 ± 0.23 | 6.86 ± 0.20 |