mech.-based inh. of monoamine oxidase LSD1

orally efficacious in xenograft model

from optimization of known starting point

ACS Med. Chem. Lett., May 12, 2020

Constellation Pharma., Cambridge, MA

“Compound 34” is a mechanism-based inhibitor of lysine-specific demethylase LSD1 (aka KDM1A). LSD1 has an FAD co-factor which is covalently modified by the cyclopropylamine in compound 34 likely through an…

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