SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious RORγ Inhibitor

[Image: see text] A novel series of RORγ inhibitors was identified starting with the HTS hit 1. After SAR investigation based on a prospective consideration of two drug-likeness metrics, ligand efficiency (LE) and fraction of sp(3) carbon atoms (Fsp(3)), significant improvement of metabolic stabilit...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Hirata, Kazuyuki, Kotoku, Masayuki, Seki, Noriyoshi, Maeba, Takaki, Maeda, Katsuya, Hirashima, Shintaro, Sakai, Takayuki, Obika, Shingo, Hori, Akimi, Hase, Yasunori, Yamaguchi, Takayuki, Katsuda, Yoshiaki, Hata, Takahiro, Miyagawa, Naoki, Arita, Kojo, Nomura, Yukihiro, Asahina, Kota, Aratsu, Yusuke, Kamada, Masafumi, Adachi, Tsuyoshi, Noguchi, Masato, Doi, Satoki, Crowe, Paul, Bradley, Erin, Steensma, Ruo, Tao, Haiyan, Fenn, Morgan, Babine, Robert, Li, Xiaolin, Thacher, Scott, Hashimoto, Hiromasa, Shiozaki, Makoto
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2015
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4716592/
https://ncbi.nlm.nih.gov/pubmed/26819660
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00253
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