Receptor residence time trumps drug-likeness and oral bioavailability in determining efficacy of complement C5a antagonists

Drug discovery and translation are normally based on optimizing efficacy by increasing receptor affinity, functional potency, drug-likeness (rule-of-five compliance) and oral bioavailability. Here we demonstrate that residence time of a compound on its receptor has an overriding influence on efficac...

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Detalles Bibliográficos
Autores principales: Seow, Vernon, Lim, Junxian, Cotterell, Adam J., Yau, Mei-Kwan, Xu, Weijun, Lohman, Rink-Jan, Kok, W. Mei, Stoermer, Martin J., Sweet, Matthew J., Reid, Robert C., Suen, Jacky Y., Fairlie, David P.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group 2016
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4837355/
https://www.ncbi.nlm.nih.gov/pubmed/27094554
http://dx.doi.org/10.1038/srep24575

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4837355/
https://www.ncbi.nlm.nih.gov/pubmed/27094554
http://dx.doi.org/10.1038/srep24575

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