Wellaway, Christopher R. published the artcileDiscovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening, Related Products of amides-buliding-blocks, the publication is Journal of Medicinal Chemistry (2020), 63(2), 714-746, database is CAplus and MEDLINE.
The bromodomain and extraterminal (BET) family of bromodomain-containing proteins are important regulators of the epigenome through their ability to recognize N-acetyl lysine (KAc) post-translational modifications on histone tails. These interactions have been implicated in various disease states and, consequently, disruption of BET-KAc binding has emerged as an attractive therapeutic strategy with a number of small mol. inhibitors now under investigation in the clinic. However, until the utility of these advanced candidates is fully assessed by these trials, there remains scope for the discovery of inhibitors from new chemotypes with alternative physicochem., pharmacokinetic, and pharmacodynamic profiles. Herein, we describe the discovery of a candidate-quality dimethylpyridone benzimidazole compound which originated from the hybridization of a dimethylphenol benzimidazole series, identified using encoded library technol., with an N-Me pyridone series identified through fragment screening. Optimization via structure- and property-based design led to I-BET469, which possesses favorable oral pharmacokinetic properties, displays activity in vivo, and is projected to have a low human efficacious dose.
Journal of Medicinal Chemistry published new progress about 475216-25-2. 475216-25-2 belongs to amides-buliding-blocks, auxiliary class Fluoride,Nitro Compound,Amine,Benzene,Amide,Benzene Compounds, name is 4-Fluoro-N-methyl-3-nitrobenzamide, and the molecular formula is C3H9ClOS, Related Products of amides-buliding-blocks.
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