. Author manuscript; available in PMC: 2019 Oct 22.

Published in final edited form as: Biochem J. 2018 Oct 22;475(20):3221–3238. doi: 10.1042/BCJ20180424

Table 2. Biochemical IC₅₀ measurements for selective inhibitors of IDH1 mutants.

Percent activity of an incubation of IDH1, NADPH, and αKG with increasing concentrations of inhibitor were determined and plotted against log[inhibitor] and fit to a sigmoidal function. The 95% confidence intervals are shown as determined from the deviation from these fits.

IDH1	ML309 IC₅₀ (μ-M) [confidence interval]	AGI-5198 IC₅₀ (μM) [confidence interval]
WT	80 [60–100]	1000 [480–2100]
R132H	0.04 [0.03–0.05]	0.04 [0.03–0.06]
R132Q	5 [4–7]	650 [330–1300]
R132C	0.04 [0.02–0.07]	0.2 [0.07–0.4]
R132G	0.09 [0.07–0.1]	0.23 [0.20–0.27]
R132L	0.01 [0.009–0.14]	0.009 [0.008–0.011]
R132S	0.1 [0.096–0.15]	0.3 [0.2–0.5]
R132V	0.0035 [0.0027–0.0044]	0.02 [0.02–0.03]

Table 2. Biochemical IC50 measurements for selective inhibitors of IDH1 mutants.

Table 2. Biochemical IC₅₀ measurements for selective inhibitors of IDH1 mutants.