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. 2018 Jun 11;9(7):746–751. doi: 10.1021/acsmedchemlett.8b00182

Table 2. Cellular Potency and CLint in Rat Liver Microsomes.

graphic file with name ml-2018-00182j_0009.jpg

Cmpd X Y R Cellular HCT116-IDH1R132H/+ (IC50/μM) Rat liver microsomal CLint (μL/min/mg)
10 Cl F Me 0.047 103
11 Cl F Et 0.013 448
12 Cl F (R)-1-F-Et 0.24 237
13 Cl F (S)-1- F-Et 0.022 272
14 Cl F F-Me 0.024 28
15 Cl H i-Pr 0.015 489
16 Cl H (S)-1- F-Et 0.004 148
17 Cl H F-Me 0.030 75
18 CF2H H (S)-1- F-Et 0.015 72
19 CF3 H F-Me 0.039 7