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Quantitative Structure-Activity Relationship

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Deciphering Cathepsin K inhibitors: a combined QSAR, docking and MD simulation based machine learning approaches for drug design.

SAR and QSAR in environmental research
Cathepsin K (CatK), a lysosomal cysteine protease, contributes to skeletal abnormalities, heart diseases, lung inflammation, and central nervous system and immune disorders. Currently, CatK inhibitors are associated with severe adverse effects, there...

Molecular mechanism underlying effect of D93 and D289 protonation states on inhibitor-BACE1 binding: exploration from multiple independent Gaussian accelerated molecular dynamics and deep learning.

SAR and QSAR in environmental research
BACE1 has been regarded as an essential drug design target for treating Alzheimer's disease (AD). Multiple independent Gaussian accelerated molecular dynamics simulations (GaMD), deep learning (DL), and molecular mechanics general Born surface area (...

Synergizing Machine Learning, Conceptual Density Functional Theory, and Biochemistry: No-Code Explainable Predictive Models for Mutagenicity in Aromatic Amines.

Journal of chemical information and modeling
This study synergizes machine learning (ML) with conceptual density functional theory (CDFT) to develop OECD-compliant predictive models for the mutagenic activity of aromatic amines (AAs) with a fully No-Code methodology using a comprehensive data s...

Explainable machine learning models for predicting the acute toxicity of pesticides to sheepshead minnow (Cyprinodon variegatus).

The Science of the total environment
A quantitative structure-activity relationship (QSAR) study was conducted on 313 pesticides to predict their acute toxicity to Sheepshead minnow (Cyprinodon variegatus) by using DRAGON descriptors. Essentials accounting for a reliable model were all ...

Small molecule inhibitors of IL-1R1/IL-1β interaction identified via transfer machine learning QSAR modelling.

International journal of biological macromolecules
The human interleukin-1 receptor I (IL-1R1) is a cytokine receptor recognized by interleukin 1β (IL-1β), among other cytokines. Over activation of IL-1R1 has been implicated in various inflammatory conditions. This research aims to identify small-mol...

Machine Learning-Based Prediction of the Inhibitory Activity of Chemical Substances Against Rat and Human Cytochrome P450s.

Chemical research in toxicology
The prediction of cytochrome P450 inhibition by a computational (quantitative) structure-activity relationship approach using chemical structure information and machine learning would be useful for toxicity research as a simple and rapid tool. Howev...

Chemoinformatics for corrosion science: Data-driven modeling of corrosion inhibition by organic molecules.

Molecular informatics
This paper reviews the application of machine learning to the inhibition of corrosion by organic molecules. The methodologies considered include quantitative structure-property relationships (QSPR) and related data-driven approaches. The characterist...

Using the super-learner to predict the chemical acute toxicity on rats.

Journal of hazardous materials
With the rapid increase in the number of commercial chemicals, testing methods regarding on median lethal dose (LD) relying animal experiments face challenges such as high costs and ethical concerns. Classical quantitative structure-activity relation...

Integration of 3D-QSAR, molecular docking, and machine learning techniques for rational design of nicotinamide-based SIRT2 inhibitors.

Computational biology and chemistry
Selective inhibitors of sirtuin-2 (SIRT2) are increasingly recognized as potential therapeutics for cancer and neurodegenerative diseases. Derivatives of 5-((3-amidobenzyl)oxy)nicotinamides have been identified as some of the most potent and selectiv...

QSPR modeling to predict surface tension of psychoanaleptic drugs using the hybrid DA-SVR algorithm.

Journal of molecular graphics & modelling
A robust Quantitative Structure-Property Relationship (QSPR) model was presented to predict the surface tension property of psychoanaleptic (psychostimulant and antidepressant) drugs. A dataset of 112 molecules was utilized, and three feature selecti...