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pmid: 19674898
A novel series of CCR5 antagonists has been identified, utilizing leads from high-throughput screening which were further modified based on insights from competitor molecules. Lead optimization was pursued by balancing opposing trends of metabolic stability and potency. Selective and potent analogs with good pharmacokinetic properties were successfully developed.
Receptors, CCR5, Haplorhini, Rats, Structure-Activity Relationship, Dogs, Piperidines, CCR5 Receptor Antagonists, Animals, Humans, Spiro Compounds, Caco-2 Cells
Receptors, CCR5, Haplorhini, Rats, Structure-Activity Relationship, Dogs, Piperidines, CCR5 Receptor Antagonists, Animals, Humans, Spiro Compounds, Caco-2 Cells
citations This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically). | 22 | |
popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network. | Average | |
influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically). | Top 10% | |
impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network. | Top 10% |