期刊
EXPERT OPINION ON DRUG DISCOVERY
卷 5, 期 7, 页码 609-618出版社
TAYLOR & FRANCIS LTD
DOI: 10.1517/17460441.2010.490553
关键词
ADMET; biophase; CNS; developability; drug discovery; ligand efficiency; pharmacodynamics; pharmacokinetics; physicochemical properties; volume of distribution
As a result of their wide acceptance and conceptual simplicity, drug-like concepts are having a major influence on the drug discovery process, particularly in the selection of the 'optimal' absorption, distribution, metabolism, excretion and toxicity and physicochemical parameters space. While they have an undisputable value when assessing the potential of lead series or in evaluating inherent risk of a portfolio of drug candidates, they result much less useful in weighing up compounds for the selection of the best potential clinical candidate. We introduce the concept of drug efficiency as a new tool both to guide the drug discovery program teams during the lead optimization phase and to better assess the developability potential of a drug candidate.
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