Description
First selective ERAP2 inhibitors
Several series of ERAP1 inhibitors
Achievements:
•Over 100 analogs
•IC₅₀ values ranging from 200 nM to 4 nM
•Potent and selective ERAP2 inhibitors: KTGS chemistry
•Good ADME properties (for the current lead compound targeting ERAP2)
•In vivo proof of concept in a psoriasis model
•Humanized animal model for ERAP created and available
IP: PCT, priority date: December 18, 2020
EP, US, CA, CN, JP, IL