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:...

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Detalles Bibliográficos
Autores principales: Chessari, Gianni, Grainger, Rachel, Holvey, Rhian S., Ludlow, R. Frederick, Mortenson, Paul N., Rees, David C.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2021
Materias:
Chemistry
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

Internet

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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