oral, brain-penetrant, reversible MAGL inh.
in vivo PK/PD in CNS (0.3-10 mpk PO)
from HTS and SBDD
Journal of Medicinal Chemistry
Takeda, Fujisawa, Japan
The Takeda MAGL inhibitor, “compound 4f”, was selected by reviewer Joachim Rudolph. “MAGL (monoacylglycerol lipase) is implicated in neuroinflammation, and inhibitors of this enzyme are of interest as therapeutics in neurodegenerative…