Table 3.
In vitro inhibition of mutant and wild type IDH2 enzymes by selected target compounds.
| Compound | IC50 nM ± SDa |
Compound |
aIC50 nM ± SD |
||
|---|---|---|---|---|---|
| IDH2R140Q | IDH2wt | IDH2R140Q | IDH2wt | ||
| 6a | 372.90 ± 18.20 | NTb | 7a | 130.10 ± 6.35 | 5418 ± 210 |
| 6c | 101.70 ± 4.97 | 2928 ± 110 | 7c | 88.93 ± 4.34 | 3128 ± 120 |
| 6d | 1868 ± 91.20 | NT | 7d | 369.6 ± 18.00 | NT |
| 6e | 67.01 ± 3.27 | 2295 ± 90 | 7e | 176.00 ± 8.60 | 5071 ± 200 |
| 6g | 336.20 ± 16.40 | NT | 7g | 505.40 ± 24.70 | NT |
| 6l | 158.00 ± 7.72 | 3438 ± 130 | 7l | 159.80 ± 7.81 | 9496 ± 370 |
| Enasidenib | 75.5 ± 3.69 | 2330 ± 90 | |||
aThe mean ± SD of three experiments; bNT: not tested.