Design and Evaluation of a Low Hydrogen Bond Donor Count Fragment Screening Set to Aid Hit Generation of PROTACs Intended for Oral Delivery

The development of orally bioavailable PROTACs presents a significant challenge due to the inflated physicochemical properties of such heterobifunctional molecules. Molecules occupying this "beyond rule of five" space often demonstrate limited oral bioavailability due to the compounding ef...

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Vydané v:	Journal of medicinal chemistry Ročník 66; číslo 11; s. 7594
Hlavní autori:	Whitehurst, Benjamin C, Bauer, Matthias R, Edfeldt, Fredrik, Gunnarsson, Anders, Margreitter, Christian, Rawlins, Philip B, Storer, R Ian
Médium:	Journal Article
Jazyk:	English
Vydavateľské údaje:	United States 08.06.2023
Predmet:	Administration, Oral Biological Availability Hydrogen Bonding Proteins - metabolism Proteolysis Proteolysis Targeting Chimera Ubiquitin-Protein Ligases - metabolism
ISSN:	1520-4804, 1520-4804
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