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Despite decades of advancements in automated ligand screening, large-scale drug discovery remains resource-intensive and requires post-processing hit selection, a step where chemists manually select a few promising molecules based on their…

Machine Learning · Computer Science 2025-03-24 Tai Dang , Long-Hung Pham , Sang T. Truong , Ari Glenn , Wendy Nguyen , Edward A. Pham , Jeffrey S. Glenn , Sanmi Koyejo , Thang Luong

Virtual screening (VS) is an essential task in drug discovery, focusing on the identification of small-molecule ligands that bind to specific protein pockets. Existing deep learning methods, from early regression models to recent…

Machine Learning · Computer Science 2025-11-11 Bowei He , Bowen Gao , Yankai Chen , Yanyan Lan , Chen Ma , Philip S. Yu , Ya-Qin Zhang , Wei-Ying Ma

Computational drug discovery strategies can be broadly placed in two categories: ligand-based methods which identify novel molecules by similarity with known ligands, and structure-based methods which predict molecules with high-affinity to…

Quantitative Methods · Quantitative Biology 2019-05-30 Vincent Mallet , Carlos G. Oliver , Nicolas Moitessier , Jerome Waldispuhl

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…

Biomolecules · Quantitative Biology 2020-03-31 Marta M. Stepniewska-Dziubinska , Piotr Zielenkiewicz , Pawel Siedlecki

Virtual Screening is an essential technique in the early phases of drug discovery, aimed at identifying promising drug candidates from vast molecular libraries. Recently, ligand-based virtual screening has garnered significant attention due…

Biomolecules · Quantitative Biology 2024-11-22 Gengmo Zhou , Zhen Wang , Feng Yu , Guolin Ke , Zhewei Wei , Zhifeng Gao

Measuring similarity between molecules is an important part of virtual screening (VS) experiments deployed during the early stages of drug discovery. Most widely used methods for evaluating the similarity of molecules use molecular…

Quantitative Methods · Quantitative Biology 2019-11-04 Maritza Hernandez , Guo Liang Gan , Kirby Linvill , Carl Dukatz , Jun Feng , Govinda Bhisetti

Virtual screening (VS) is an essential technique for understanding biomolecular interactions, particularly, drug design and discovery. The best-performing VS models depend vitally on three-dimensional (3D) structures, which are not…

Biomolecules · Quantitative Biology 2022-12-29 Li Shen , Hongsong Feng , Yuchi Qiu , Guo-Wei Wei

In drug discovery, structure-based virtual high-throughput screening (vHTS) campaigns aim to identify bioactive ligands or "hits" for therapeutic protein targets from docked poses at specific binding sites. However, while generally…

Quantitative Methods · Quantitative Biology 2021-12-03 Pawel Gniewek , Bradley Worley , Kate Stafford , Henry van den Bedem , Brandon Anderson

Docking-based virtual screening (VS process) selects ligands with potential pharmacological activities from millions of molecules using computational docking methods, which greatly could reduce the number of compounds for experimental…

Quantitative Methods · Quantitative Biology 2021-10-26 Wei Ma , Qin Xie , Jianhang Zhang , Shiliang Li , Youjun Xu , Xiaobing Deng , Weilin Zhang

Structure-based virtual screening aims to identify high-affinity ligands by estimating binding free energies between proteins and small molecules. However, the conformational flexibility of both proteins and ligands challenges conventional…

Biomolecules · Quantitative Biology 2025-07-15 Pei-Kun Yang

As the size of accessible compound libraries expands to over 10 billion, the need for more efficient structure-based virtual screening methods is emerging. Different pre-screening methods have been developed for rapid screening, but there…

Biomolecules · Quantitative Biology 2025-03-07 Seonghwan Seo , Woo Youn Kim

The accurate screening of candidate drug ligands against target proteins through computational approaches is of prime interest to drug development efforts. Such virtual screening depends in part on methods to predict the binding affinity…

Machine Learning · Computer Science 2024-10-22 Ho-Joon Lee , Prashant S. Emani , Mark B. Gerstein

Comprehensive discovery of structural variation (SV) in human genomes from DNA sequencing requires the integration of multiple alignment signals including read-pair, split-read and read-depth. However, owing to inherent technical…

Genomics · Quantitative Biology 2014-01-23 Ryan M. Layer , Ira M. Hall , Aaron R. Quinlan

Drug development is a wide scientific field that faces many challenges these days. Among them are extremely high development costs, long development times, as well as a low number of new drugs that are approved each year. To solve these…

Biomolecules · Quantitative Biology 2022-11-08 Christoph Gorgulla

Drug discovery seeks molecules (ligands) that bind strongly and selectively to a target protein. However, fewer than 5% of candidate ligands pass the bar for even the early stages of drug discovery. Furthermore, we want methods that work…

Machine Learning · Computer Science 2026-05-08 Rahul Nandakumar , Ben Fauber , Deepayan Chakrabarti

Prediction of protein-ligand interactions (PLI) plays a crucial role in drug discovery as it guides the identification and optimization of molecules that effectively bind to target proteins. Despite remarkable advances in deep…

Biomolecules · Quantitative Biology 2023-07-18 Seokhyun Moon , Sang-Yeon Hwang , Jaechang Lim , Woo Youn Kim

Drug discovery is a time-consuming and expensive process, with traditional high-throughput and docking-based virtual screening hampered by low success rates and limited scalability. Recent advances in generative modelling, including…

Artificial Intelligence · Computer Science 2026-03-12 Junkai Ji , Zhangfan Yang , Dong Xu , Ruibin Bai , Jianqiang Li , Tingjun Hou , Zexuan Zhu

The arc of drug discovery entails a multiparameter optimization problem spanning vast length scales. They key parameters range from solubility (angstroms) to protein-ligand binding (nanometers) to in vivo toxicity (meters). Through feature…

The knowledge of potentially druggable binding sites on proteins is an important preliminary step towards the discovery of novel drugs. The computational prediction of such areas can be boosted by following the recent major advances in the…

Biomolecules · Quantitative Biology 2021-02-17 Stelios K. Mylonas , Apostolos Axenopoulos , Petros Daras

Structure based ligand discovery is one of the most successful approaches for augmenting the drug discovery process. Currently, there is a notable shift towards machine learning (ML) methodologies to aid such procedures. Deep learning has…

Machine Learning · Statistics 2018-06-12 Marta M. Stepniewska-Dziubinska , Piotr Zielenkiewicz , Pawel Siedlecki
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