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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Veröffentlicht in:	Journal of medicinal chemistry Jg. 66; H. 11; S. 7594
Hauptverfasser:	Whitehurst, Benjamin C, Bauer, Matthias R, Edfeldt, Fredrik, Gunnarsson, Anders, Margreitter, Christian, Rawlins, Philip B, Storer, R Ian
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	United States 08.06.2023
Schlagworte:	Administration, Oral Biological Availability Hydrogen Bonding Proteins - metabolism Proteolysis Proteolysis Targeting Chimera Ubiquitin-Protein Ligases - metabolism
ISSN:	1520-4804, 1520-4804
Online-Zugang:	Weitere Angaben
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