LNP-023
Inhibitor of CFB
Structure
In Cells
In Model Organisms
Probe LNP-023 is in the process of SERP review.
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SERP ratings and comments
SERP Ratings
SERP Comments:
LNP023 is a first in class, potent reversible inhibitor of the serine protease factor B (FB). This protease is a key component of the alternative complement pathway. This pathway is dysregulated in a number of diseases, and a number of targets in the pathway are active subjects of drug discovery programs. The compound was optimized using structure-based drug design and a number of useful crystal structures have been deposited. LPN023 has IC50 values >30 micromolar for 41 other proteases tested. The selectivity is likely due to unique features of the FB active site. It also is inactive (IC50>30 micromolar) across a panel of 110 enzymes, receptors, and ion channels. It exhibits the expected on-target pharmacology and in vivo activity. Phase 1 trials have been completed and it is in phase 2 trials for several diseases.
(last updated: 12 Mar 2021 )