Summary of small molecule inhibitor screening data of CXCR4.

<p>(A) Layout of microplate. Wells marked in green are CXCR4 inhibitors. Controls are shown in white: column 10 shows data for CXCR4-eGFP and CXCR4-TagRFP transfected cells without inhibitor treatment; column 11 shows CXCR4-eGFP only cells without inhibitor treatment. In column 10 the concentration of CXCL12 is varied: row D is untreated while rows E and F are treated with 5 nM and 20 nM CXCL12 respectively. (B) Comparison of anisotropy and lifetime data showing that dimerisation and internalisation is blocked by CXCR4 inhibitors. Errors bars represent the standard deviation of repeated measurements in each well (4 images per well for each modality). (C) Plots of anisotropy and FRET efficiency for column 10, rows D, E and F: cells in the absence of any inhibitors (CXCL12 concentrations of 5 nM and 20 nM). (D) Percentage change in anisotropy and lifetime compared to controls.