Figure 3.

Structure, biophysical properties and biological activities of PEG-linked PROTAC Set 1. Coloring is added to aid visualization. (A) The general structure of a set of PROTACs (10–19, Set 1) is shown in the top left, comprised of AR ligands 1–4, proteolysis directing groups 6–8, and a PEG-linker. The PAMPA permeability for compounds 1–4 and 6–8 is shown in the outer edge of the table. The main body of the table shows the PROTAC compound number in bold (10–19), composed from AR ligand 1–4 and proteolysis directing group 6–8, followed by PAMPA permeability. The same table format is used in (B–C). BLQ = Below limit of quantification. (B) HSA % free determined by HPLC and as described in methods section. (C) chromLogD_7.4 determined by HPLC as described in the methods section.