Quantitation of ERK1/2 inhibitor cellular target occupancies with a reversible slow off-rate probe

Target engagement is a key concept in drug discovery and its direct measurement can provide a quantitative understanding of drug efficacy and/or toxicity. Failure to demonstrate target occupancy in relevant cells and tissues has been recognised as a contributing factor to the low success rate of cli...

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Detalles Bibliográficos
Autores principales: Lebraud, Honorine, Surova, Olga, Courtin, Aurélie, O'Reilly, Marc, Valenzano, Chiara R., Nordlund, Pär, Heightman, Tom D.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Royal Society of Chemistry 2018
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6253716/
https://www.ncbi.nlm.nih.gov/pubmed/30568786
http://dx.doi.org/10.1039/c8sc02754d

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6253716/
https://www.ncbi.nlm.nih.gov/pubmed/30568786
http://dx.doi.org/10.1039/c8sc02754d

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