molecules of the month

“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

1 min read

“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 microsomal stability over the corresponding piperidine analog without a significant change in cLogD. The compound demonstrated activity in a xenograft model at doses as low as 0.5 mg/kg QD.

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