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Structure-guided optimization of a novel class of ASK1 inhibitors with increased sp<sup>3</sup> character and an exquisite selectivity profile.

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第一作者: Simone V,Bigi-Botterill
第一单位: Medicinal Chemistry & In Vitro Pharmacology, Gastroenterology Drug Discovery Unit, Takeda Research in California, 9625 Towne Centre Drive, San Diego, CA 92121, United States. Electronic address: simone.bigi@takeda.com.
作者单位: Medicinal Chemistry & In Vitro Pharmacology, Gastroenterology Drug Discovery Unit, Takeda Research in California, 9625 Towne Centre Drive, San Diego, CA 92121, United States. Electronic address: simone.bigi@takeda.com. [1] Mirati Therapeutics, 9393 Towne Centre Drive #200, San Diego, CA 92121, United States. [2] Quantitative Translational Sciences, Takeda Research in California, 9625 Towne Centre Drive, San Diego, CA 92121, United States. [3] Medicinal Chemistry & In Vitro Pharmacology, Gastroenterology Drug Discovery Unit, Takeda Research in California, 9625 Towne Centre Drive, San Diego, CA 92121, United States. [4] Structural Biology & Biophysics, Gastroenterology Drug Discovery Unit, Takeda Research in California, 9625 Towne Centre Drive, San Diego, CA 92121, United States. [5] Medicinal Chemistry, Neuroscience Drug Discovery Unit, Takeda Research in California, 9625 Towne Centre Drive, San Diego, CA 92121, United States. [6] 858 Therapeutics, 4757 Nexus Center Drive #150, San Diego, CA 92121, United States. [7] Chemistry & Design, Silicon Therapeutics, 451 D Street #205, Boston, MA 02210, United States. [8]
DOI 10.1016/j.bmcl.2020.127405
PMID 32738982
发布时间 2021-06-08
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