Table 2 Biochemical and cellular data for compounds 1–4

From: Biostructural, biochemical and biophysical studies of mutant IDH1

Compound

1

2

3

4

IDH1 wt IC50

> 20 µM (n = 11)

> 20 µM (n = 44)

> 20 µM (n = 2)

> 20 µM (n = 1)

IDH1 R132H IC50

48 ± 59 nM (n = 16)

79 ± 48 nM (n = 79)

6 ± 2 nM (n = 5)

18 ± 5 nM (n = 7)

IDH1 het dimer IC50

245 ± 227 nM (n = 12)

705 ± 232 nM (n = 67)

47 ± 2 nM (n = 2)

297 nM (n = 1)

MOG R132H cellular IC50

0.7 μM (n = 1)

1.3 ± 0.9 µM (n = 308)

66 ± 20 nM (n = 4)

205 ± 37 nM (n = 8)

  1. IC50 values were determined using a sigmodal dose-response curve in Graph Pad Prism v10. Data are mean values ± SD (Standard Deviation).
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