Fig. 7

Target protein occupancy measurement for PARP1 inhibitors. HeLa cells were treated with DMSO or Olaparib target ID probe 3 in the presence of indicating concentration of Olaparib. The cells were fixed and permeablized and protein binding 3 were conjugated with 100 nM Cy5-Tz for 5 min (scale bar: 50 μm). b Mean fluorescence of single cell nuclei (n = 300—520) with different concentration of Olaparib was shown in box plot. Histograms superimposed on the box plot was distribution of individual fluorescence intensities. Plotted data was from one representative experiment of (a). c PARP1 occupancy assay of Olaparib (black squares), Rucaparib (Red circles), and PJ34 (Blue triangles). Fluorescence intensity of 3 inside nuclei was measured in the presence of each compound. Reprinted with permission from ref 63. Copyright 2016 American Chemical Society