Figure 4.
Competition curves for selected compounds in the AlphaScreen assay. a) Competition curves for different compounds using the AlphaScreen with the donor and acceptor beads brought together by Hsp90 peptide and TPR2A protein. Compounds 8–13 all show typical dose-dependent inhibition of the acceptor fluorescence. The inactive structural analogue compound does not. b) AlphaScreen in counter-screen format. A covalent linker peptide (biotin-His6 peptide) directly brings the donor and acceptor beads together. Any compounds that inhibit in this assay are considered to be false positives. Percent of control binding (no inhibition – 100%) is plotted against log[compound]. Error values were calculated from multiple experiments. c) Core structure representative of the hit compounds.