Blind Pose Prediction, Scoring, and Affinity Ranking of the CSAR 2014 Dataset

J Chem Inf Model. 2016 Jun 27;56(6):996-1003. doi: 10.1021/acs.jcim.5b00337. Epub 2015 Oct 1.

Abstract

The 2014 CSAR Benchmark Exercise was focused on three protein targets: coagulation factor Xa, spleen tyrosine kinase, and bacterial tRNA methyltransferase. Our protocol involved a preliminary analysis of the structural information available in the Protein Data Bank for the protein targets, which allowed the identification of the most appropriate docking software and scoring functions to be used for the rescoring of several docking conformations datasets, as well as for pose prediction and affinity ranking. The two key points of this study were (i) the prior evaluation of molecular modeling tools that are most adapted for each target and (ii) the increased search efficiency during the docking process to better explore the conformational space of big and flexible ligands.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benchmarking
  • Databases, Protein
  • Factor Xa / chemistry
  • Factor Xa / metabolism
  • Molecular Docking Simulation*
  • Protein Conformation
  • Proteins / chemistry*
  • Proteins / metabolism*
  • Syk Kinase / chemistry
  • Syk Kinase / metabolism
  • tRNA Methyltransferases / chemistry
  • tRNA Methyltransferases / metabolism

Substances

  • Proteins
  • tRNA Methyltransferases
  • Syk Kinase
  • Factor Xa