molecules of the month

“Compound 6g”

potent, reversible MAGL serine hydrolase inh.

orally efficacious in inflamm. pain model

from optimization of prior ligand

Bioorg. Med. Chem. Lett., May 7, 2020

Janssen R&D, Spring House, PA

Structure of compound 6g
1 min read

“Compound 6g” is a potent, selective, and reversible inhibitor of monoacylglycerol lipase (MAGL), which degrades the cannabinoid receptor (CB) agonist 2-arachidononylglycerol (2-AG) to arachadonic acid (AA). Inhibition of MAGL therefore indirectly agonizes CB receptors and reduces inflammatory AA levels, which may be beneficial for a range of disorders. In contrast to most prior MAGL inhibitors which are covalent modifiers, this compound is a reversible inhibitor.

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