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Drug discovery and development is a complex and costly process. Machine learning approaches are being investigated to help improve the effectiveness and speed of multiple stages of the drug discovery pipeline. Of these, those that use…

Artificial Intelligence · Computer Science 2022-09-27 Stephen Bonner , Ian P Barrett , Cheng Ye , Rowan Swiers , Ola Engkvist , Andreas Bender , Charles Tapley Hoyt , William L Hamilton

We introduce a graphical method originating from the computer graphics domain that is used for the arbitrary and intuitive placement of cells over a two-dimensional manifold. Using a bitmap image as input, where the color indicates the…

Neural and Evolutionary Computing · Computer Science 2018-03-23 Nicolas P. Rougier

Background: Identifying new indications for approved drugs is a complex and time-consuming process that requires extensive knowledge of pharmacology, clinical data, and advanced computational methods. Recently, deep learning (DL) methods…

Machine Learning · Computer Science 2025-11-13 Shuting Jin , Yi Jiang , Yimin Liu , Tengfei Ma , Dongsheng Cao , Leyi Wei , Xiangrong Liu , Xiangxiang Zeng

Fragment-based drug design is a promising strategy leveraging the binding of small chemical moieties that can efficiently guide drug discovery. The initial step of fragment identification remains challenging, as fragments often bind weakly…

Biomolecules · Quantitative Biology 2025-09-17 Rebecca Manuela Neeser , Ilia Igashov , Arne Schneuing , Michael Bronstein , Philippe Schwaller , Bruno Correia

Background Semantic Web Technology (SWT) makes it possible to integrate and search the large volume of life science datasets in the public domain, as demonstrated by well-known linked data projects such as LODD, Bio2RDF, and Chem2Bio2RDF.…

Quantitative Methods · Quantitative Biology 2011-06-27 Qian Zhu , Yuyin Sun , Sashikiran Challa , Ying Ding , Michael S. Lajiness , David J. Wild

How to produce expressive molecular representations is a fundamental challenge in AI-driven drug discovery. Graph neural network (GNN) has emerged as a powerful technique for modeling molecular data. However, previous supervised approaches…

Machine Learning · Computer Science 2020-12-22 Pengyong Li , Jun Wang , Yixuan Qiao , Hao Chen , Yihuan Yu , Xiaojun Yao , Peng Gao , Guotong Xie , Sen Song

The dynamic nature of proteins, influenced by ligand interactions, is essential for comprehending protein function and progressing drug discovery. Traditional structure-based drug design (SBDD) approaches typically target binding sites with…

Biomolecules · Quantitative Biology 2025-03-07 Xiangxin Zhou , Yi Xiao , Haowei Lin , Xinheng He , Jiaqi Guan , Yang Wang , Qiang Liu , Feng Zhou , Liang Wang , Jianzhu Ma

Learning accurate drug representation is essential for tasks such as computational drug repositioning and prediction of drug side-effects. A drug hierarchy is a valuable source that encodes human knowledge of drug relations in a tree-like…

Machine Learning · Computer Science 2020-06-02 Ke Yu , Shyam Visweswaran , Kayhan Batmanghelich

Several generative models with elaborate training and sampling procedures have been proposed to accelerate structure-based drug design (SBDD); however, their empirical performance turns out to be suboptimal. We seek to better understand…

Machine Learning · Computer Science 2025-03-04 Rafał Karczewski , Samuel Kaski , Markus Heinonen , Vikas Garg

A novel framework has recently been proposed for designing the molecular structure of chemical compounds with a desired chemical property, where design of novel drugs is an important topic in bioinformatics and chemo-informatics. The…

The Spatial Knowledge Graphs (SKG) are experiencing growing adoption as a means to model real-world entities, proving especially invaluable in domains like crisis management and urban planning. Considering that RDF specifications offer…

Artificial Intelligence · Computer Science 2024-11-05 Amin Anjomshoaa , Hannah Schuster , Axel Polleres

Modern drug discovery is often time-consuming, complex and cost-ineffective due to the large volume of molecular data and complicated molecular properties. Recently, machine learning algorithms have shown promising results in virtual…

Neural and Evolutionary Computing · Computer Science 2022-02-08 Dongning Ma , Rahul Thapa , Xun Jiao

Accurately predicting the binding affinity between drugs and proteins is an essential step for computational drug discovery. Since graph neural networks (GNNs) have demonstrated remarkable success in various graph-related tasks, GNNs have…

Quantitative Methods · Quantitative Biology 2020-12-18 Jingbo Zhou , Shuangli Li , Liang Huang , Haoyi Xiong , Fan Wang , Tong Xu , Hui Xiong , Dejing Dou

In this paper, we study a sequential decision-making problem, called Adaptive Sampling for Discovery (ASD). Starting with a large unlabeled dataset, algorithms for ASD adaptively label the points with the goal to maximize the sum of…

Machine Learning · Statistics 2023-01-04 Ziping Xu , Eunjae Shim , Ambuj Tewari , Paul Zimmerman

The rise of cost involved with drug discovery and current speed of which they are discover, underscore the need for more efficient structure-based drug design (SBDD) methods. We employ Generative Flow Networks (GFlowNets), to effectively…

Machine Learning · Computer Science 2024-06-18 Grayson Lee , Tony Shen , Martin Ester

Machine learning has the potential to automate molecular design and drastically accelerate the discovery of new functional compounds. Towards this goal, generative models and reinforcement learning (RL) using string and graph…

Machine Learning · Computer Science 2022-02-02 Daniel Flam-Shepherd , Alexander Zhigalin , Alán Aspuru-Guzik

Recent remarkable advancements in geometric deep generative models, coupled with accumulated structural data, enable structure-based drug design (SBDD) using only target protein information. However, existing models often struggle to…

Biomolecules · Quantitative Biology 2026-03-09 Joongwon Lee , Wonho Zhung , Jisu Seo , Woo Youn Kim

In therapeutic design, balancing various physiochemical properties is crucial for molecule development, similar to how Multiparameter Optimization (MPO) evaluates multiple variables to meet a primary goal. While many molecular features can…

Biomolecules · Quantitative Biology 2024-01-03 Agustin Kruel , Andrew D. McNaughton , Neeraj Kumar

Drug synergy arises when the combined impact of two drugs exceeds the sum of their individual effects. While single-drug effects on cell lines are well-documented, the scarcity of data on drug synergy, considering the vast array of…

Quantitative Methods · Quantitative Biology 2024-04-29 Kyriakos Schwarz , Alicia Pliego-Mendieta , Amina Mollaysa , Lara Planas-Paz , Chantal Pauli , Ahmed Allam , Michael Krauthammer

Recent advances in generative deep learning have transformed small molecule design, but most methods lack biological systems context, focusing narrowly on specific protein pockets. We introduce a non-differentiable diffusion guidance method…

Biomolecules · Quantitative Biology 2024-10-15 Vincent D. Zaballa , Elliot E. Hui