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. 2016 Aug 18;7(10):944–949. doi: 10.1021/acsmedchemlett.6b00264

Figure 1.

Figure 1

BRD2879, but not its stereoisomers, potently inhibits IDH1-R132H in vitro. (a) Structure of BRD2879. (b) The (2S, 5R, 6R) configuration shows >10× lower IC50 than its stereoisomers. Values are geometric means of three independent experiments; typical CV is 35%. (c) NADPH-dependent ketoreductase activity of IDH1-R132H after incubation with compounds. BRD2879 inhibits IDH1-R132H with comparable potency and Hill slope to previously disclosed AGI-5198. Values are mean ± SD of three independent experiments.