A linear combination of pharmacophore hypotheses as a new tool in search of new active compounds--an application for 5-HT1A receptor ligands

PLoS One. 2013 Dec 18;8(12):e84510. doi: 10.1371/journal.pone.0084510. eCollection 2013.

Abstract

This study explores a new approach to pharmacophore screening involving the use of an optimized linear combination of models instead of a single hypothesis. The implementation and evaluation of the developed methodology are performed for a complete known chemical space of 5-HT1AR ligands (3616 active compounds with K i < 100 nM) acquired from the ChEMBL database. Clusters generated from three different methods were the basis for the individual pharmacophore hypotheses, which were assembled into optimal combinations to maximize the different coefficients, namely, MCC, accuracy and recall, to measure the screening performance. Various factors that influence filtering efficiency, including clustering methods, the composition of test sets (random, the most diverse and cluster population-dependent) and hit mode (the compound must fit at least one or two models from a final combination) were investigated. This method outmatched both single hypothesis and random linear combination approaches.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cluster Analysis
  • Drug Evaluation, Preclinical / methods*
  • Ligands
  • Models, Molecular
  • Molecular Conformation
  • Receptor, Serotonin, 5-HT1A / metabolism*
  • Reproducibility of Results

Substances

  • Ligands
  • Receptor, Serotonin, 5-HT1A

Grants and funding

This study was supported by the project UDA-POIG.01.03.01-12-063/09-00 Prokog, which is co-financed by the European Union from the European Fund of Regional Development (EFRD) and by Norway Grants within the Polish-Norwegian Research Programme, grant no. Pol-Nor/198887/73/2013. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.