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Sep. 18, 2021

JNJ-54717793: A Selective Antagonist of the Orexin-1 Receptor


oral, BP, selective OX1R GPCR antagonist orally efficacious in panic attack models from optimization of internal OX2R antagonist ACS Med. Chem. Lett., May 5, 2020 Janssen R&D, San Diego, CA

Drug Hunter Team

JNJ-54717793 is a selective antagonist of the orexin-1 receptor intended for use in anxiety disorders, in contrast to dual orexin-1/2 inhibitors and orexin-2 inhibitors typically applied for sleep disorders. It’s a surprisingly large molecule (three aromatic rings and a bicycle) for an oral, brain-penetrant clinical candidate with predicted [...]



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