Table 1.
Inhibition of the histone demethylase JMJD2E (100 nM) by bipyridyl compounds. IC50s represent the result of three independent experiments, where standard errors in the log(IC50) are less than 10 %. Ranking of binding strength by ESI-MS is as shown in Figure 3. All compounds were counter-screened against FDH at the same concentrations used for IC50 determinations, and inhibition of FDH was not observed under these conditions, implying that the compounds only inhibited JMJD2E.
