ARTICLE | Product R&D

It’s the assay...

How Genentech redesigned a discovery assay to find a specific Nav1.7 blocker

February 2, 2018 3:02 AM UTC

Genentech and Xenon have reported that the key to finding a selective Nav1.7 blocker is devising a better screen, not using a bigger compound library. By retooling a commonly used assay, the partners identified a new lead and established principals for tailoring screen construction to improve drug discovery for this and other ion channels.

Nav1.7 belongs to a family of voltage-gated sodium channels that show a high degree of sequence and structural conservation, making selective inhibition a challenge. Yet individual members play distinct roles in physiology and disease. ...