Table 1. IDH1R132H Biochemical Activity of HTS Hits and Pure Resynthesized Diastereomers.
chirality at amine (Am) | chirality at oxazolidinone (Ox) | biochem. LCMS IC50 (μM) | |
---|---|---|---|
1a | R/S = 1:1 | S | 0.8 |
1b | R/S = 1:1 | R | 8.5 |
1c | R | R | 19.7 |
1d | S | R | 4.2 |
1e | R | S | 4.6 |
1f (IDH125) | S | S | 0.22 |