ML-309 is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH1). It reversibly and selective inhibits IDH1R132H over wild-type IDH1 (IC50s = 96 and 36,500 nM, respectively). ML-309 reduces 2-hydroxyglutarate production in U87 MG glioblastoma cells (EC50 = 55 nM).
ML-252 is a potent, selective inhibitor of the Kv7.2 voltage-gated potassium channel, demonstrating an IC50 value of 69 nM in patch clamp assays. It exists as the (S)-enantiomer, which is significantly more effective than both its (R)-enantiomer counterpart and the racemic mixture, with respective IC50 values of 944 nM and 160 nM. ML-252 exhibits high selectivity for Kv7.2 over other potassium channel subtypes and shows minimal activity against more than 68 G protein-coupled receptors, various transporters, L- and N-type calcium channels, K_ATP, and hERG potassium channels. However, it does inhibit the melatonin MT1 receptor by 61% at a 10 µM concentration.