Designing Soluble PROTACs: Strategies and Preliminary Guidelines

[Image: see text] Solubility optimization is a crucial step to obtaining oral PROTACs. Here we measured the thermodynamic solubilities (log S) of 21 commercial PROTACs. Next, we measured BRlogD and log k(w)(IAM) (lipophilicity), EPSA, and Δ log k(w)(IAM) (polarity) and showed that lipophilicity play...

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Detalles Bibliográficos
Autores principales: García Jiménez, Diego, Rossi Sebastiano, Matteo, Vallaro, Maura, Mileo, Valentina, Pizzirani, Daniela, Moretti, Elisa, Ermondi, Giuseppe, Caron, Giulia
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9574862/
https://www.ncbi.nlm.nih.gov/pubmed/35469399
http://dx.doi.org/10.1021/acs.jmedchem.2c00201

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9574862/
https://www.ncbi.nlm.nih.gov/pubmed/35469399
http://dx.doi.org/10.1021/acs.jmedchem.2c00201

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