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. 2016 Jan 6;7(3):223–228. doi: 10.1021/acsmedchemlett.5b00278

Table 3. Incorporation of Polar Functional Groups on Aryl Ethera.

graphic file with name ml-2015-00278z_0010.jpg

  R CDK8 IC50 (nM) PPB % bound (H/R/M) kinetic solubility (μM)
23 Me 6.0 97.2/95.9/96.1 <1
24 OMe 25 93.6/94.0/90.2 10
25 OCF3 12 97.9/96.8/97.2 <1
26 CN 5.1 84.7/87.3/89.1 8
27 CONH2 21 77.3/76.8/78.3 7
28 NHAc 29 91.0/84.8/79.6 18
a

PPB figures in human, rat, and mouse plasma (H/R/M).