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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...
| Autores principales: | , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
Nature Publishing Group
2016
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| Materias: | |
| 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 |