Ligand biological activity predictions using fingerprint-based artificial neural networks (FANN-QSAR).

Journal: Methods in molecular biology (Clifton, N.J.)
PMID:

Abstract

This chapter focuses on the fingerprint-based artificial neural networks QSAR (FANN-QSAR) approach to predict biological activities of structurally diverse compounds. Three types of fingerprints, namely ECFP6, FP2, and MACCS, were used as inputs to train the FANN-QSAR models. The results were benchmarked against known 2D and 3D QSAR methods, and the derived models were used to predict cannabinoid (CB) ligand binding activities as a case study. In addition, the FANN-QSAR model was used as a virtual screening tool to search a large NCI compound database for lead cannabinoid compounds. We discovered several compounds with good CB2 binding affinities ranging from 6.70 nM to 3.75 μM. The studies proved that the FANN-QSAR method is a useful approach to predict bioactivities or properties of ligands and to find novel lead compounds for drug discovery research.

Authors

  • Kyaw Z Myint
    NIDA Center of Excellence for Computational Chemogenomics Drug Abuse Research, Computational Chemical Genomics Screening Center, Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pittsburgh, Pennsylvania, USA, kyawzeyarmyint@gmail.com.
  • Xiang-Qun Xie