Really pleased to share this story from Amphista Therapeutics on the discovery and MoA of a potent and selective BRD9 "targeted glue" degrader. The compound also works in vivo and is orally bioavailable! Fantastic work from the team on a super fun project!
www.biorxiv.org/content/10.1...
Great work Andrea & team! Nice example of blurring the lines between glues and PROTACs. Also showing just what a boost a (reversible) covalent mechanism can give you in the kinetic, event-driven world! Satisfying to see pM activity, oral in vivo effects and a target which isn't BRD4!
02.01.2025 18:17 — 👍 1 🔁 0 💬 0 📌 0