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C–H functionalisation tolerant to polar groups could transform fragment-based drug discovery (FBDD)
We have analysed 131 fragment-to-lead (F2L) examples targeting a wide variety of protein families published by academic and industrial laboratories between 2015–2019. Our assessment of X-ray structural data identifies the most common polar functional groups involved in fragment-protein binding are:...
Autores principales: | Chessari, Gianni, Grainger, Rachel, Holvey, Rhian S., Ludlow, R. Frederick, Mortenson, Paul N., Rees, David C. |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
The Royal Society of Chemistry
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8457390/ https://www.ncbi.nlm.nih.gov/pubmed/34667563 http://dx.doi.org/10.1039/d1sc03563k |
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