Document Detail


Tautomers and reference 3D-structures: the orphans of in silico drug design.
MedLine Citation:
PMID:  20349114     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The importance of calculating not only the correct tautomer, but also the correct protonation state and conformation in 3D modeling applications is emphasized. Above all, identifying and characterizing the most stable form of a ligand under physiological conditions is seen to be the key to successful 3D modeling. Modeling strategies that make use of the performance of modern hardware can employ physically more appropriate models than most currently in use and still be easily applicable to large numbers of compounds. Because the performance of quantitative structure-property relationships is likely to be limited by the available training and validation data, we must either find new sources of such data or resort to explicit modeling, which can partly be parameterized using definitive ab initio calculations for reference data such as gas-phase proton affinities.
Authors:
Timothy Clark
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Publication Detail:
Type:  Journal Article     Date:  2010-03-27
Journal Detail:
Title:  Journal of computer-aided molecular design     Volume:  24     ISSN:  1573-4951     ISO Abbreviation:  J. Comput. Aided Mol. Des.     Publication Date:  2010 Jun 
Date Detail:
Created Date:  2010-06-17     Completed Date:  2010-09-27     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8710425     Medline TA:  J Comput Aided Mol Des     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  605-11     Citation Subset:  IM    
Affiliation:
Computer-Chemie-Centrum, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nägelsbachstrasse 25, 91052, Erlangen, Germany. Tim.Clark@chemie.uni-erlangen.de
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MeSH Terms
Descriptor/Qualifier:
Drug Design*
Isomerism
Models, Chemical
Molecular Conformation*
Protons*
Chemical
Reg. No./Substance:
0/Protons

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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