Description
1st ERAP2 selective inhibitors
Several series of ERAP1 inhibitors
Achievements:
•More than 100 analogues
•IC50s from 200 nM to 4 nM
•ERAP2 potent selective inhibitors: KTGS chemistry
•Good ADME properties (on current ERAP2 lead)
•In vivo proof of concept on a psoriasis model
•ERAP-humanized animal created and available