Vertex recently disclosed a CNS-penetrant ELOVL1 inhibitor, in which they described preclinical safety findings in rat and cyno. In this article, they disclose a structurally distinct series which displayed similar ocular toxicity in rat, and skin and CNS toxicities in cyno. A third structurally distinct series (undisclosed) also showed [...]
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Jan. 17, 2022
Compound 22: a CNS-Penetrant ELOVL1 Inhibitor
“compound 22”
ELOVL1 fatty acid elongase inhibitor on-target toxicity suggested from HTS and property-based optimization Journal of Medicinal Chemistry Vertex, Boston, MA