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  3. The Polypharmacology Browser PPB2: Target Prediction Combining Nearest Neighbors with Machine Learning

The Polypharmacology Browser PPB2: Target Prediction Combining Nearest Neighbors with Machine Learning

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DOI
10.7892/boris.122954
Publisher DOI
10.1021/acs.jcim.8b00524
Abstract
Here we report PPB2 as a target prediction tool assigning targets to a query molecule based on ChEMBL data. PPB2 computes ligand similarities using molecular fingerprints encoding composition (MQN), molecular shape and pharmacophores (Xfp), and substructures (ECfp4), and features an unprecedented combination of nearest neighbor (NN) searches and Naïve Bayes (NB) machine learning, together with simple NN searches, NB and Deep Neural Network (DNN) machine learning models as further options. Although NN(ECfp4) gives the best results in terms of recall in a 10-fold cross-validation study, combining NN searches with NB machine learning provides superior precision statistics, as well as better results in a case study predicting off-targets of a recently reported TRPV6 calcium channel inhibitor, illustrating the value of this combined approach. PPB2 is available to assess possible off-targets of small molecule drug-like compounds by public access at ppb2.gdb.tools.
Date Issued
2019
Publication Type
Article
Subject(s)
500 Science > 570 Life sciences; biology
500 Science > 540 Chemistry
Language(s)
en
Author(s)
Awale, Mahendra  
Departement für Chemie und Biochemie (DCB)  
Reymond, Jean-Louis  orcid-logo
Departement für Chemie und Biochemie (DCB)  
Additional Credits
Departement für Chemie und Biochemie (DCB)  
Journal
Journal of chemical information and modeling
Publisher
American Chemical Society
ISSN
1549-9596
Access(Rights)
open.access
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