TABLE 1

Inhibition of CXCL8 binding

Compound inhibition at CXCR receptors and mutated receptor constructs was determined by measuring the displacement of 125I-CXCL8 binding to membranes. Compound, CXCL8, and membranes were incubated for 2 h at 22°C. Inhibition of specifically bound CXCL8 was determined and analyzed by nonlinear regression. pIC50 values were derived from experiments presented in Fig. 9 and are the mean ± S.E.M. of three to six individual determinations.


Construct

pIC50
Compound A
Compound B
CXCR1 6.3 ± 0.17 5.9 ± 0.13
CXCR2 8.9 ± 0.13 8.7 ± 0.11
CXCR1 N311K 8.1 ± 0.13 8.3 ± 0.11
CXCR2 K320N
7.9 ± 0.15
7.5 ± 0.22