“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 electron-transfer mechanism (as for tranylcypromine and MAOs). Interestingly, the 4,4-spiro amine provided an improvement to in vitro [...]
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Sep. 18, 2021
Compound 34: A Mechanism-Based Inhibitor of Lysine-Specific Demethylase LSD1
“compound 34”
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
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