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. Author manuscript; available in PMC: 2021 Jul 16.
Published in final edited form as: Cell Chem Biol. 2020 May 14;27(7):866–876.e8. doi: 10.1016/j.chembiol.2020.04.008

Figure 3. Validation of Cellular Target Engagement Assay and Preliminary Screening.

Figure 3.

(A) and (B) Chemical structures and bioactivity test of known IMiDs through cellular target engagement. (C) and (D) Chemical structures and bioactivity test of selected thalidomide derivatives with partial linkers through cellular target engagement. See also Figure S2 MM1S cells were treated with CRBN ligand or vehicle (1 h), then degrader or vehicle (5 h) and analyzed by in-cell ELISA. Bar graphs were generated as means of HDAC6 relative expression (n = 3) with ± SD as the error bar. Variances were analyzed by unpaired two-tail student t-test in comparison with “pomalidomide” group. *P ≤ 0.05, **P ≤ 0.01, ***P ≤ 0.001, ****P ≤ 0.0001.