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. 2018 Sep 10;13(9):2406–2413. doi: 10.1021/acschembio.8b00534

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Copyright © 2018 American Chemical Society

This is an open access article published under a Creative Commons Non-Commercial No Derivative Works (CC-BY-NC-ND) Attribution License, which permits copying and redistribution of the article, and creation of adaptations, all for non-commercial purposes.

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Off-target profiling of β-lactam based MAGL inhibitor (6) and clinical candidate ABX-1431 in mouse brain membrane proteome. (A) Chemical structure of 6 and 7. (B) Dose response inhibition with 6 shows several off-targets in the mouse brain membrane. (C) Dose response inhibition with 7 shows selective MAGL inhibition in the mouse brain membrane. (D) pIC₅₀ curves and values of 6 against MAGL. (E) pIC₅₀ curves and values of 6 against its off-targets. (F) pIC₅₀ curves and values of 7 against MAGL.