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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...
Uloženo v:
| Vydáno v: | Sci Rep |
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| Hlavní autoři: | , , , , , , , , , , , |
| Médium: | Artigo |
| Jazyk: | Inglês |
| Vydáno: |
Nature Publishing Group
2016
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| Témata: | |
| On-line přístup: | https://ncbi.nlm.nih.gov/pmc/articles/PMC4837355/ https://ncbi.nlm.nih.gov/pubmed/27094554 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/srep24575 |
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