TABLE 2

Affinity (pKd or pKi) of CXCR2 ligands at human-baboon chimeras

Displacement of 125I-CXCL8 binding to COS-7 cell membranes expressing indicated chimeric receptors HHB, BBH, HBB, BHH, HBH, and BHB. The data are presented as mean ± S.E.M. of at least three independent experiments.

CXCR2pKd CXCL8pKi
SB265610Compound 1
Embedded ImageHuman9.40 ± 0.147.68 ± 0.117.18 ± 0.13
Embedded ImageBaboon9.33 ± 0.087.28 ± 0.10<4
Embedded ImageHHB chimera
Embedded ImageBBH chimera9.41 ± 0.217.17 ± 0.196.70 ± 0.10
Embedded ImageHBB chimera
Embedded ImageBHH chimera9.52 ± 0.096.93 ± 0.206.66 ± 0.11
Embedded ImageHBH chimera9.49 ± 0.117.33 ± 0.166.90 ± 0.10
Embedded ImageBHB chimera9.43 ± 0.077.20 ± 0.04<4
  • —, 125I-CXCL8 does not bind to this construct.