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Methyl Effects on Protein–Ligand Binding

The effects of addition of a methyl group to a lead compound on biological activity are examined. A literature analysis of >2000 cases reveals that an activity boost of a factor of ten or more is found with an 8% frequency, and a 100-fold boost is a 1 in 200 event. Four cases in the latter catego...

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Autori principali: Leung, Cheryl S., Leung, Siegfried S. F., Tirado-Rives, Julian, Jorgensen, William L.
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2012
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Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC3353327/
https://ncbi.nlm.nih.gov/pubmed/22500930
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm3003697
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