Table 2. SAR of PEG Linker Length and Active-Site Inhibitors.

| entry | compound no. | PEG repeats | active-site inhibitor | pS6K IC50 (nM) | p4EBP1 IC50 (nM) | pAKT IC50 (nM) | selectivity |
|---|---|---|---|---|---|---|---|
| 1 | 20 | 8 | PP121 | 0.22 | 1.0 | 17 | 17.0 |
| 2 | 24 | 6 | 0.24 | 31 | 110 | 3.5 | |
| 3 | 18 | 8 | PP242 | 0.28 | 1.4 | 18 | 12.9 |
| 4 | 25 | 6 | 0.59 | 370 | 120 | 0.3 | |
| 5 | 19 | 8 | BGT226 | 0.02 | 0.06 | 0.52 | 8.7 |
| 6 | 26 | 6 | 0.03 | 0.08 | 0.74 | 9.3 | |
| 7 | 16 | 8 | MLN | 0.42 | 1.1 | 3.1 | 2.8 |
| 8 | 27 | 6 | 0.26 | 1.1 | 5.2 | 4.7 | |
| 9 | 28 | 5 | 0.37 | 25 | 33 | 1.3 |