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Molecular Conformation

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Prediction of pharmacological activities from chemical structures with graph convolutional neural networks.

Scientific reports
Many therapeutic drugs are compounds that can be represented by simple chemical structures, which contain important determinants of affinity at the site of action. Recently, graph convolutional neural network (GCN) models have exhibited excellent res...

Combining Data with Predictions for Modeling Hepatic Steatosis by Using Stratified Bagging and Conformal Prediction.

Chemical research in toxicology
Hepatic steatosis (fatty liver) is a severe liver disease induced by the excessive accumulation of fatty acids in hepatocytes. In this study, we developed reliable models for predicting hepatic steatosis on the basis of an data set of 1041 compound...

Predicting With Confidence: Using Conformal Prediction in Drug Discovery.

Journal of pharmaceutical sciences
One of the challenges with predictive modeling is how to quantify the reliability of the models' predictions on new objects. In this work we give an introduction to conformal prediction, a framework that sits on top of traditional machine learning al...

Integrated Variational Approach to Conformational Dynamics: A Robust Strategy for Identifying Eigenfunctions of Dynamical Operators.

The journal of physical chemistry. B
One approach to analyzing the dynamics of a physical system is to search for long-lived patterns in its motions. This approach has been particularly successful for molecular dynamics data, where slowly decorrelating patterns can indicate large-scale ...

Reverse graph self-attention for target-directed atomic importance estimation.

Neural networks : the official journal of the International Neural Network Society
Estimating the importance of each atom in a molecule is one of the most appealing and challenging problems in chemistry, physics, and materials science. The most common way to estimate the atomic importance is to compute the electronic structure usin...

Can One Hear the Shape of a Molecule (from its Coulomb Matrix Eigenvalues)?

Journal of chemical information and modeling
Coulomb matrix eigenvalues (CMEs) are global 3D representations of molecular structure, which have been previously used to predict atomization energies, prioritize geometry searches, and interpret rotational spectra. The properties of the CME represe...

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...

Flexible Fitting of Small Molecules into Electron Microscopy Maps Using Molecular Dynamics Simulations with Neural Network Potentials.

Journal of chemical information and modeling
Despite significant advances in resolution, the potential for cryo-electron microscopy (EM) to be used in determining the structures of protein-drug complexes remains unrealized. Determination of accurate structures and coordination of bound ligands ...

Incorporating Explicit Water Molecules and Ligand Conformation Stability in Machine-Learning Scoring Functions.

Journal of chemical information and modeling
Structure-based drug design is critically dependent on accuracy of molecular docking scoring functions, and there is of significant interest to advance scoring functions with machine learning approaches. In this work, by judiciously expanding the tra...

From Target to Drug: Generative Modeling for the Multimodal Structure-Based Ligand Design.

Molecular pharmaceutics
Chemical space is impractically large, and conventional structure-based virtual screening techniques cannot be used to simply search through the entire space to discover effective bioactive molecules. To address this shortcoming, we propose a generat...