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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...
Autores principales: | Lebraud, Honorine, Surova, Olga, Courtin, Aurélie, O'Reilly, Marc, Valenzano, Chiara R., Nordlund, Pär, Heightman, Tom D. |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Royal Society of Chemistry
2018
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Materias: | |
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 |
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