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Ligands

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Protein-Ligand Docking in the Machine-Learning Era.

Molecules (Basel, Switzerland)
Molecular docking plays a significant role in early-stage drug discovery, from structure-based virtual screening (VS) to hit-to-lead optimization, and its capability and predictive power is critically dependent on the protein-ligand scoring function....

Informed Chemical Classification of Organophosphorus Compounds via Unsupervised Machine Learning of X-ray Absorption Spectroscopy and X-ray Emission Spectroscopy.

The journal of physical chemistry. A
We analyze an ensemble of organophosphorus compounds to form an unbiased characterization of the information encoded in their X-ray absorption near-edge structure (XANES) and valence-to-core X-ray emission spectra (VtC-XES). Data-driven emergence of ...

Artificial intelligence and machine-learning approaches in structure and ligand-based discovery of drugs affecting central nervous system.

Molecular diversity
CNS disorders are indications with a very high unmet medical needs, relatively smaller number of available drugs, and a subpar satisfaction level among patients and caregiver. Discovery of CNS drugs is extremely expensive affair with its own unique c...

Molecule Design Using Molecular Generative Models Constrained by Ligand-Protein Interactions.

Journal of chemical information and modeling
In recent years, molecular deep generative models have attracted much attention for its application in drug design. The data-driven molecular deep generative model approximates the high dimensional distribution of the chemical space through learning...

AI-based prediction of new binding site and virtual screening for the discovery of novel P2X3 receptor antagonists.

European journal of medicinal chemistry
Artificial intelligence (AI) has been recognized as a powerful technique that can accelerate drug discovery during the hit compound identification step. However, most simple deep learning models have been used for naive pre-filtering as the predictio...

A Physics-Guided Neural Network for Predicting Protein-Ligand Binding Free Energy: From Host-Guest Systems to the PDBbind Database.

Biomolecules
Calculation of protein-ligand binding affinity is a cornerstone of drug discovery. Classic implicit solvent models, which have been widely used to accomplish this task, lack accuracy compared to experimental references. Emerging data-driven models, o...

Predicting Protein-Ligand Docking Structure with Graph Neural Network.

Journal of chemical information and modeling
Modern day drug discovery is extremely expensive and time consuming. Although computational approaches help accelerate and decrease the cost of drug discovery, existing computational software packages for docking-based drug discovery suffer from both...

Sfcnn: a novel scoring function based on 3D convolutional neural network for accurate and stable protein-ligand affinity prediction.

BMC bioinformatics
BACKGROUND: Computer-aided drug design provides an effective method of identifying lead compounds. However, success rates are significantly bottlenecked by the lack of accurate and reliable scoring functions needed to evaluate binding affinities of p...

Translating from Proteins to Ribonucleic Acids for Ligand-binding Site Detection.

Molecular informatics
Identifying druggable ligand-binding sites on the surface of the macromolecular targets is an important process in structure-based drug discovery. Deep-learning models have been shown to successfully predict ligand-binding sites of proteins. As a ste...

TocoDecoy: A New Approach to Design Unbiased Datasets for Training and Benchmarking Machine-Learning Scoring Functions.

Journal of medicinal chemistry
Development of accurate machine-learning-based scoring functions (MLSFs) for structure-based virtual screening against a given target requires a large unbiased dataset with structurally diverse actives and decoys. However, most datasets for the devel...