Machine‐learning scoring functions for structure‐based drug lead optimization

H Li, KH Sze, G Lu, PJ Ballester - Wiley Interdisciplinary …, 2020 - Wiley Online Library
Molecular docking can be used to predict how strongly small‐molecule binders and their
chemical derivatives bind to a macromolecular target using its available three‐dimensional …

OnionNet-2: a convolutional neural network model for predicting protein-ligand binding affinity based on residue-atom contacting shells

Z Wang, L Zheng, Y Liu, Y Qu, YQ Li, M Zhao… - Frontiers in …, 2021 - frontiersin.org
One key task in virtual screening is to accurately predict the binding affinity (△ G) of protein-
ligand complexes. Recently, deep learning (DL) has significantly increased the predicting …

A comprehensive survey of prospective structure-based virtual screening for early drug discovery in the past fifteen years

H Zhu, Y Zhang, W Li, N Huang - International Journal of Molecular …, 2022 - mdpi.com
Structure-based virtual screening (SBVS), also known as molecular docking, has been
increasingly applied to discover small-molecule ligands based on the protein structures in …

A review of mathematical representations of biomolecular data

DD Nguyen, Z Cang, GW Wei - Physical Chemistry Chemical Physics, 2020 - pubs.rsc.org
Recently, machine learning (ML) has established itself in various worldwide benchmarking
competitions in computational biology, including Critical Assessment of Structure Prediction …

Assessment of the generalization abilities of machine-learning scoring functions for structure-based virtual screening

H Zhu, J Yang, N Huang - Journal of Chemical Information and …, 2022 - ACS Publications
In structure-based virtual screening (SBVS), it is critical that scoring functions capture protein–
ligand atomic interactions. By focusing on the local domains of ligand binding pockets, a …

True accuracy of fast scoring functions to predict high-throughput screening data from docking poses: the simpler the better

VK Tran-Nguyen, G Bret, D Rognan - Journal of Chemical …, 2021 - ACS Publications
Hundreds of fast scoring functions have been developed over the last 20 years to predict
binding free energies from three-dimensional structures of protein-ligand complexes …

VAD-MM/GBSA: a variable atomic dielectric MM/GBSA model for improved accuracy in protein–ligand binding free energy calculations

E Wang, W Fu, D Jiang, H Sun, J Wang… - Journal of Chemical …, 2021 - ACS Publications
The molecular mechanics/generalized Born surface area (MM/GBSA) has been widely used
in end-point binding free energy prediction in structure-based drug design (SBDD) …

SMPLIP-Score: predicting ligand binding affinity from simple and interpretable on-the-fly interaction fingerprint pattern descriptors

S Kumar, M Kim - Journal of cheminformatics, 2021 - Springer
In drug discovery, rapid and accurate prediction of protein–ligand binding affinities is a
pivotal task for lead optimization with acceptable on-target potency as well as …

A consistent scheme for gradient-based optimization of protein–ligand poses

F Flachsenberg, A Meyder, K Sommer… - Journal of Chemical …, 2020 - ACS Publications
Scoring and numerical optimization of protein–ligand poses is an integral part of docking
tools. Although many scoring functions exist, many of them are not continuously …

Improving docking-based virtual screening ability by integrating multiple energy auxiliary terms from molecular docking scoring

WL Ye, C Shen, GL Xiong, JJ Ding, AP Lu… - Journal of Chemical …, 2020 - ACS Publications
Virtual Screening (VS) based on molecular docking is an efficient method used for retrieving
novel hit compounds in drug discovery. However, the accuracy of the current docking …