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. 2022 Dec 19;66(1):149–169. doi: 10.1021/acs.jmedchem.2c01658

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

graphic file with name jm2c01658_0013.jpg

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