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Drug development is an expensive and time-consuming process where thousands of chemical compounds are being tested in order to find those possessing drug-like properties while being safe and effective. One of key parts of the early drug…

Quantitative Methods · Quantitative Biology 2022-02-15 Josip Mesarić

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

Drug discovery through virtual screening (VS) has become a popular strategy for identifying hits against protein targets. Alongside VS, molecular design further expands accessible chemical space. Together, these approaches have the…

Biomolecules · Quantitative Biology 2025-10-15 Shanzhuo Zhang , Xianbin Ye , Donglong He , Yueyang Huang , Xiaonan Zhang , Xiaomin Fang

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

Due to their excellent drug-like and pharmacokinetic properties, small molecule drugs are widely used to treat various diseases, making them a critical component of drug discovery. In recent years, with the rapid development of deep…

Machine Learning · Computer Science 2025-05-15 Kun Li , Yida Xiong , Hongzhi Zhang , Xiantao Cai , Jia Wu , Bo Du , Wenbin Hu

Drug discovery is the most expensive, time demanding and challenging project in biopharmaceutical companies which aims at the identification and optimization of lead compounds from large-sized chemical libraries. The lead compounds should…

Distributed, Parallel, and Cluster Computing · Computer Science 2021-12-02 Natarajan Arul Murugan , Artur Podobas , Davide Gadioli , Emanuele Vitali , Gianluca Palermo , Stefano Markidis

Virtual screening of small molecules against protein targets can accelerate drug discovery and development by predicting drug-target interactions (DTIs). However, structure-based methods like molecular docking are too slow to allow for…

Artificial intelligence (AI) in the form of deep learning bears promise for drug discovery and chemical biology, $\textit{e.g.}$, to predict protein structure and molecular bioactivity, plan organic synthesis, and design molecules…

Biomolecules · Quantitative Biology 2022-12-29 Rıza Özçelik , Derek van Tilborg , José Jiménez-Luna , Francesca Grisoni

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

Machine learning shows great potential in virtual screening for drug discovery. Current efforts on accelerating docking-based virtual screening do not consider using existing data of other previously developed targets. To make use of the…

Machine Learning · Computer Science 2021-12-14 Zijing Liu , Xianbin Ye , Xiaomin Fang , Fan Wang , Hua Wu , Haifeng Wang

Structure-based drug design uses three-dimensional geometric information of macromolecules, such as proteins or nucleic acids, to identify suitable ligands. Geometric deep learning, an emerging concept of neural-network-based machine…

Chemical Physics · Physics 2022-10-21 Clemens Isert , Kenneth Atz , Gisbert Schneider

Machine learning approaches to Structure-Based Drug Design (SBDD) have proven quite fertile over the last few years. In particular, diffusion-based approaches to SBDD have shown great promise. We present a technique which expands on this…

Machine Learning · Computer Science 2024-07-01 Matan Halfon , Eyal Rozenberg , Ehud Rivlin , Daniel Freedman

With the development of computer-assisted techniques, research communities including biochemistry and deep learning have been devoted into the drug discovery field for over a decade. Various applications of deep learning have drawn great…

Machine Learning · Computer Science 2023-03-07 Wenhao Hu , Yingying Liu , Xuanyu Chen , Wenhao Chai , Hangyue Chen , Hongwei Wang , Gaoang Wang

Support vector machines and kernel methods have recently gained considerable attention in chemoinformatics. They offer generally good performance for problems of supervised classification or regression, and provide a flexible and…

Quantitative Methods · Quantitative Biology 2007-08-02 Pierre Mahé , Jean-Philippe Vert

The ability to precisely visualize the atomic geometry of the interactions between a drug and its protein target in structural models is critical in predicting the correct modifications in previously identified inhibitors to create more…

Biomolecules · Quantitative Biology 2018-08-14 Erick Martins Ratamero , Dom Bellini , Christopher G. Dowson , Rudolf A. Roemer

Virtual screening (VS) is a critical component of modern drug discovery, yet most existing methods--whether physics-based or deep learning-based--are developed around holo protein structures with known ligand-bound pockets. Consequently,…

Machine Learning · Computer Science 2025-10-31 Wenyu Zhu , Jianhui Wang , Bowen Gao , Yinjun Jia , Haichuan Tan , Ya-Qin Zhang , Wei-Ying Ma , Yanyan Lan

The potential of virtual reality (VR) to contribute to drug design and development has been recognised for many years. Hardware and software developments now mean that this potential is beginning to be realised, and VR methods are being…

Biomolecules · Quantitative Biology 2022-02-09 Rebecca K. Walters , Ella M. Gale , Jonathan Barnoud , David R. Glowacki , Adrian J. Mulholland

Structure-based drug design (SBDD) leverages the three-dimensional geometry of proteins to identify potential drug candidates. Traditional approaches, rooted in physicochemical modeling and domain expertise, are often resource-intensive.…

Quantitative Methods · Quantitative Biology 2024-11-19 Zaixi Zhang , Jiaxian Yan , Yining Huang , Qi Liu , Enhong Chen , Mengdi Wang , Marinka Zitnik

Molecular docking is a crucial step in drug development, which enables the virtual screening of compound libraries to identify potential ligands that target proteins of interest. However, the computational complexity of traditional docking…

Machine Learning · Computer Science 2024-12-06 Zhangfan Yang , Junkai Ji , Shan He , Jianqiang Li , Tiantian He , Ruibin Bai , Zexuan Zhu , Yew Soon Ong

Despite the great popularity of virtual screening of existing compound libraries, the search for new potential drug candidates also takes advantage of generative protocols, where new compound suggestions are enumerated using various…

Biomolecules · Quantitative Biology 2023-12-22 Tomasz Danel , Jan Łęski , Sabina Podlewska , Igor T. Podolak
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