CX3CR1 is a GPCR expressed on natural killer cells, cytotoxic T lymphocytes, and macrophages. The sole ligand for CX3CR1, fractalkine, is an unusual chemokine that is expressed as a transmembrane molecule with a CX3C domain and a mucin domain (Imai et al., 1997). Fractalkine is highly expressed on endothelial cells activated by TNFa and other proinflammatory cytokines, and fractalkine/CX3CR1 interactions mediate recruitment of macrophages into the atherosclerotic plaque (Lesnick et al., 2003; McDermott et al., 2003). In addition, fractalkine and CX3CR1 have been implicated in the pathogenesis of glomerulonephritis, HIV infection and rheumatoid arthritis (Ito et al., 2002; Faure et al., 2003; Nanki et al., 2002). Chemicon's CX3CR1 membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression; thus, they are ideal HTS tools for screening of antagonists of fractalkine/CX3CR1 interactions. The membrane preparations exhibit a Kd of 0.05 nM for [125I]-fractalkine. With 2.5 mg/well CX3CR1 Membrane Prep and 0.05 nM [125I]-fractalkine, a greater than 7-fold signal-to-background ratio is obtained.