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. Author manuscript; available in PMC: 2023 Oct 19.
Published in final edited form as: J Am Chem Soc. 2022 Oct 6;144(41):18861–18875. doi: 10.1021/jacs.2c05030

Figure 3. Biochemical potency versus selectivity plot of HDAC10 inhibitors.

Figure 3.

Cap group modifications of DKFZ-728 modulate HDAC10 potency, but do not achieve an increase in selectivity beyond that of DKFZ-728, 28, and 33. Dot size represents ligand efficiency (LE = 1.37 × pIC50(HDAC10) / number of heavy atoms) (38). Colors represent from which “box” from Table 1 and Figures 2 and 3 the compounds originate: Blue dots: “aza-scan” compounds (Figure 2); Red dots: cap modifications based on DKFZ-728 (Figure 3); Grey dots: cap attachment amide modifications (Table 1); Purple dots: amine to cap amide linker length variations of DKFZ-728 scaffold (Table 1); Green dots: cyclic γ-amine linkers (Table 1). For a tabulated and extended version of this plot with 95% confidence intervals, see Table S2.