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

Table 3. SAR of Active-Site Inhibitors with the C40-Carbamate Chemical Handle.

graphic file with name jm2c01658_0014.jpg

entry compound no. PEG repeats active-site inhibitor pS6K IC50 (nM) p4EBP1 IC50 (nM) pAKT IC50 (nM) selectivity
1 29 8 MLN 0.61 1.7 3.6 2.1
2 30 8 “rigid MLN” 0.19 0.42 4.7 11.2
3 31 8 XL388 0.23 0.70 2.9 4.1