Figure 2: Correlation of phenotypic potency with target engagement to intracellular HDAC isozymes.
From: Target engagement and drug residence time can be observed in living cells with BRET
(a) 48 h treatment with HDAC inhibitors results in antiproliferative effects in HeLa cells, as measured by intracellular ATP levels. Data are the mean of three independent experiments±s.e.m.. (b) Antiproliferative potency of HDAC inhibitors, as determined by cellular ATP levels in HeLa cells, is strongly correlated with target engagement to HDAC1. See Supplementary Fig. 2b and Supplementary Table 2 for the comparative correlation with other HDAC isozymes. Data are the mean of 3 independent experiments±s.d.
