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Drug Design

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The SAR Matrix Method and an Artificially Intelligent Variant for the Identification and Structural Organization of Analog Series, SAR Analysis, and Compound Design.

Molecular informatics
The SAR Matrix (SARM) approach was originally conceived for the systematic identification of analog series, their structural organization, and graphical structure-activity relationship (SAR) analysis. For structurally related series, SARMs also produ...

The Synthesizability of Molecules Proposed by Generative Models.

Journal of chemical information and modeling
The discovery of functional molecules is an expensive and time-consuming process, exemplified by the rising costs of small molecule therapeutic discovery. One class of techniques of growing interest for early stage drug discovery is molecular genera...

Revealing cytotoxic substructures in molecules using deep learning.

Journal of computer-aided molecular design
In drug development, late stage toxicity issues of a compound are the main cause of failure in clinical trials. In silico methods are therefore of high importance to guide the early design process to reduce time, costs and animal testing. Technical a...

Cov_FB3D: A De Novo Covalent Drug Design Protocol Integrating the BA-SAMP Strategy and Machine-Learning-Based Synthetic Tractability Evaluation.

Journal of chemical information and modeling
drug design actively seeks to use sets of chemical rules for the fast and efficient identification of structurally new chemotypes with the desired set of biological properties. Fragment-based design tools have been successfully applied in the disco...

The power of deep learning to ligand-based novel drug discovery.

Expert opinion on drug discovery
INTRODUCTION: Deep discriminative and generative neural-network models are becoming an integral part of the modern approach to ligand-based novel drug discovery. The variety of different architectures of neural networks, the methods of their training...

Big data and artificial intelligence discover novel drugs targeting proteins without 3D structure and overcome the undruggable targets.

Stroke and vascular neurology
The discovery of targeted drugs heavily relies on three-dimensional (3D) structures of target proteins. When the 3D structure of a protein target is unknown, it is very difficult to design its corresponding targeted drugs. Although the 3D structures ...

How Sure Can We Be about ML Methods-Based Evaluation of Compound Activity: Incorporation of Information about Prediction Uncertainty Using Deep Learning Techniques.

Molecules (Basel, Switzerland)
A great variety of computational approaches support drug design processes, helping in selection of new potentially active compounds, and optimization of their physicochemical and ADMET properties. Machine learning is a group of methods that are able ...

Automated De Novo Design in Medicinal Chemistry: Which Types of Chemistry Does a Generative Neural Network Learn?

Journal of medicinal chemistry
Artificial intelligence offers promising solutions for property prediction, compound design, and retrosynthetic planning, which are expected to significantly accelerate the search for pharmacologically relevant molecules. Here, we investigate aspects...

Improving detection of protein-ligand binding sites with 3D segmentation.

Scientific reports
In recent years machine learning (ML) took bio- and cheminformatics fields by storm, providing new solutions for a vast repertoire of problems related to protein sequence, structure, and interactions analysis. ML techniques, deep neural networks espe...

A Review on Applications of Computational Methods in Drug Screening and Design.

Molecules (Basel, Switzerland)
Drug development is one of the most significant processes in the pharmaceutical industry. Various computational methods have dramatically reduced the time and cost of drug discovery. In this review, we firstly discussed roles of multiscale biomolecul...