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Article

Novel bicyclic pyrazoles as potent ALK2 (R206H) inhibitors for the treatment of fibrodysplasia ossificans progressiva.

Bioorganic & medicinal chemistry letters - 15 Apr 2021

Yamamoto Hirofumi, Sakai Naoki, Ohte Satoshi, Sato Tomohiro, Sekimata Katsuhiko, Matsumoto Takehisa, Nakamura Kana, Watanabe Hisami, Mishima-Tsumagari Chiemi, Tanaka Akiko, Hashizume Yoshinobu, Honma Teruki, Katagiri Takenobu, Miyazono Kohei, Tomoda Hiroshi, Shirouzu Mikako, Koyama Hiroo

Abstract excerpt

Mutant activin receptor-like kinase-2 (ALK2) is associated with the pathogenesis of fibrodysplasia ossificans progressiva, making it an attractive target for therapeutic intervention. We synthesized a new series of bicyclic pyrazoles and evaluated their mutant ALK2 enzyme inhibitory activities, leading to the identification of 8 as the most potent inhibitor. This compound showed moderate microsomal metabolic...

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Share to Activin Receptors, Type I
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Identifiers

PMID: 33609658
DOI: 10.1016/j.bmcl.2021.127858

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 6 Sept 2026.

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