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Quantitative Structure-Activity Relationship

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De Novo Design of Bioactive Small Molecules by Artificial Intelligence.

Molecular informatics
Generative artificial intelligence offers a fresh view on molecular design. We present the first-time prospective application of a deep learning model for designing new druglike compounds with desired activities. For this purpose, we trained a recurr...

Application of Generative Autoencoder in De Novo Molecular Design.

Molecular informatics
A major challenge in computational chemistry is the generation of novel molecular structures with desirable pharmacological and physiochemical properties. In this work, we investigate the potential use of autoencoder, a deep learning methodology, for...

Development of Predictive QSAR Models of 4-Thiazolidinones Antitrypanosomal Activity Using Modern Machine Learning Algorithms.

Molecular informatics
This paper presents novel QSAR models for the prediction of antitrypanosomal activity among thiazolidines and related heterocycles. The performance of four machine learning algorithms: Random Forest regression, Stochastic gradient boosting, Multivari...

Obituary: Toshio Fujita, QSAR pioneer.

Journal of computer-aided molecular design
This is the obituary for Toshio Fujita, pioneer of the quantitative structure activity relationship (QSAR) paradigm.

Transductive Ridge Regression in Structure-activity Modeling.

Molecular informatics
In this article we consider the application of the Transductive Ridge Regression (TRR) approach to structure-activity modeling. An original procedure of the TRR parameters optimization is suggested. Calculations performed on 3 different datasets invo...

Generative Recurrent Networks for De Novo Drug Design.

Molecular informatics
Generative artificial intelligence models present a fresh approach to chemogenomics and de novo drug design, as they provide researchers with the ability to narrow down their search of the chemical space and focus on regions of interest. We present a...

ADMET Evaluation in Drug Discovery. 18. Reliable Prediction of Chemical-Induced Urinary Tract Toxicity by Boosting Machine Learning Approaches.

Molecular pharmaceutics
Xenobiotic chemicals and their metabolites are mainly excreted out of our bodies by the urinary tract through the urine. Chemical-induced urinary tract toxicity is one of the main reasons that cause failure during drug development, and it is a common...

Predicting Organ Toxicity Using in Vitro Bioactivity Data and Chemical Structure.

Chemical research in toxicology
Animal testing alone cannot practically evaluate the health hazard posed by tens of thousands of environmental chemicals. Computational approaches making use of high-throughput experimental data may provide more efficient means to predict chemical to...

Demystifying Multitask Deep Neural Networks for Quantitative Structure-Activity Relationships.

Journal of chemical information and modeling
Deep neural networks (DNNs) are complex computational models that have found great success in many artificial intelligence applications, such as computer vision1,2 and natural language processing.3,4 In the past four years, DNNs have also generated p...

Probing the toxicity of nanoparticles: a unified in silico machine learning model based on perturbation theory.

Nanotoxicology
Nanoparticles (NPs) are part of our daily life, having a wide range of applications in engineering, physics, chemistry, and biomedicine. However, there are serious concerns regarding the harmful effects that NPs can cause to the different biological ...