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Fig. 3 | Clinical Epigenetics

Fig. 3

From: Histone acetyltransferases: challenges in targeting bi-substrate enzymes

Fig. 3

Challenges to get from the concentration of inhibitor that gives 50 % of inhibition (IC50) to the assay independent inhibitory potency (K i) for a HAT inhibitor. In case of bi-substrate enzymes like HATs, many factors need to be considered when calculating the inhibitory potency from the IC50. Kinetic studies combined with affinity studies, crystal structures, dead-end inhibitors, and studies on the catalytic mechanism of HATs aid in deriving a K i for HAT inhibitors

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