potent, BP, NAPE-PLD zinc hydrolase inhibitor
brain penetrant IP tool compound
from HTS and optimization
Nat. Chem. Biol., May 11, 2020
Leiden University, Leiden, NL
LEI401 is a selective, brain-penetrant inhibitor of NAPE-PLD, an enzyme involved in the biosynthesis of various N-acylethanolamine (NAE) signaling lipids, and is a potentially useful tool molecule for understanding the basic biology around this target. The compound emerged as the result of an academic collaboration, including an HTS done with the European Lead Factory. This looks to be a promising example of how academic institutions can collaboratively generate and validate useful tools for basic research.