Lead optimization in the nondrug-like space

Drug-like space might be more densely populated with orally available compounds than the remaining chemical space, but lead optimization can still occur outside this space. Oral drug space is more dynamic than the relatively static drug-like space. As new targets emerge and optimization tools advanc...

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Bibliographic Details
Published inDrug discovery today Vol. 16; no. 3; pp. 158 - 163
Main Author Zhao, Hongyu
Format Journal Article
LanguageEnglish
Published Kidlington Elsevier Ltd 01.02.2011
Elsevier
Subjects
Administration, Oral
Biological and medical sciences
Combinatorial Chemistry Techniques - methods
Combinatorial Chemistry Techniques - trends
Drug Design
General pharmacology
Humans
Ligands
Medical sciences
Molecular Structure
Molecular Weight
Pharmaceutical Preparations - administration & dosage
Pharmaceutical Preparations - chemistry
Pharmaceutical technology. Pharmaceutical industry
Pharmacokinetics
Pharmacology. Drug treatments
Technology, Pharmaceutical - methods
Technology, Pharmaceutical - trends
Pharmaceutical technology
Pharmaceutical industry
Optimization
Research and development
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Summary:Drug-like space might be more densely populated with orally available compounds than the remaining chemical space, but lead optimization can still occur outside this space. Oral drug space is more dynamic than the relatively static drug-like space. As new targets emerge and optimization tools advance the oral drug space might expand. Lead optimization protocols are becoming more complex with greater optimization needs to be satisfied, which consequently could change the role of drug-likeness in the process. Whereas drug-like space should usually be explored preferentially, it can be easier to find oral drugs for certain targets in the nondrug-like space.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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ISSN:1359-6446
1878-5832
DOI:10.1016/j.drudis.2010.12.002