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. Author manuscript; available in PMC: 2020 Dec 8.
Published in final edited form as: Nat Chem Biol. 2020 Jun 8;16(9):997–1005. doi: 10.1038/s41589-020-0555-4

Figure 3. Summary of findings from Structure-Activity Study.

Figure 3.

Overview of SAR and data on key compounds to emerge from the study of >70 analogues of 4 (see Supplementary Information). Compounds were evaluated in dose response mode against purified mouse and human LYPLAL1, and at 10 μM against mLYPLAL1 overexpressed in HEK293 cells. aEC50 (μM); bfold increase in FP-rhodamine labeling of LYPLAL1 assessed by gel-based ABPP; crelative activation of mLYPLAL1 overexpressed in HEK293 cells expressed as a percentage of the effect of 4; dstructure determined by X-ray; enot determined. ABPP data shown is representative of two or more independent experiments that yielded similar results.