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Drug-target affinity (DTA) prediction is a critical aspect of drug discovery. The meaningful representation of drugs and targets is crucial for accurate prediction. Using 1D string-based representations for drugs and targets is a common…

Quantitative Methods · Quantitative Biology 2024-11-05 Kusal Debnath , Pratip Rana , Preetam Ghosh

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

Accurate prediction of the binding affinity between drugs and target proteins is a core task in computer-aided drug design. Existing deep learning methods tend to ignore the information of internal sub-structural features of drug molecules…

Biomolecules · Quantitative Biology 2025-04-04 Jiannuo Li , Lan Yao

Machine learning (ML) is a promising approach for predicting small molecule properties in drug discovery. Here, we provide a comprehensive overview of various ML methods introduced for this purpose in recent years. We review a wide range of…

Biomolecules · Quantitative Biology 2023-08-25 Nikolai Schapin , Maciej Majewski , Alejandro Varela , Carlos Arroniz , Gianni De Fabritiis

In recent years, machine learning has been proposed as a promising strategy to build accurate scoring functions for computational docking finalized to numerically empowered drug discovery. However, the latest studies have suggested that…

Quantitative Methods · Quantitative Biology 2023-02-17 F. Pellicani , D. Dal Ben , A. Perali , S. Pilati

Drug combination therapy has become a increasingly promising method in the treatment of cancer. However, the number of possible drug combinations is so huge that it is hard to screen synergistic drug combinations through wet-lab…

Machine Learning · Computer Science 2021-07-07 J. Wang , X. Liu , S. Shen , L. Deng , H. Liu*

A fundamental problem in drug discovery is to design molecules that bind to specific proteins. To tackle this problem using machine learning methods, here we propose a novel and effective framework, known as GraphBP, to generate 3D…

Biomolecules · Quantitative Biology 2022-05-31 Meng Liu , Youzhi Luo , Kanji Uchino , Koji Maruhashi , Shuiwang Ji

Drug-Target binding Affinity (DTA) prediction is essential for drug discovery. Despite the application of deep learning methods to DTA prediction, the achieved accuracy remain suboptimal. In this work, inspired by the recent success of…

Biomolecules · Quantitative Biology 2024-07-23 Qizhi Pei , Lijun Wu , Zhenyu He , Jinhua Zhu , Yingce Xia , Shufang Xie , Rui Yan

Accurate prediction of drug-target interaction (DTI) is essential for in silico drug design. For the purpose, we propose a novel approach for predicting DTI using a GNN that directly incorporates the 3D structure of a protein-ligand…

Machine Learning · Computer Science 2019-04-18 Jaechang Lim , Seongok Ryu , Kyubyong Park , Yo Joong Choe , Jiyeon Ham , Woo Youn Kim

Accurately predicting drug-target interactions (DTIs) is pivotal for advancing drug discovery and target validation techniques. While machine learning approaches including those that are based on Graph Neural Networks (GNN) have achieved…

Machine Learning · Computer Science 2025-09-30 Yuehua Song , Yong Gao

Accurate prediction of protein-ligand binding affinities is an essential challenge in structure-based drug design. Despite recent advances in data-driven methods for affinity prediction, their accuracy is still limited, partially because…

Biomolecules · Quantitative Biology 2024-09-04 Yaosen Min , Ye Wei , Peizhuo Wang , Xiaoting Wang , Han Li , Nian Wu , Stefan Bauer , Shuxin Zheng , Yu Shi , Yingheng Wang , Ji Wu , Dan Zhao , Jianyang Zeng

Drug combination therapy is a well-established strategy for disease treatment with better effectiveness and less safety degradation. However, identifying novel drug combinations through wet-lab experiments is resource intensive due to the…

Machine Learning · Computer Science 2023-01-18 Zhihang Hu , Qinze Yu , Yucheng Guo , Taifeng Wang , Irwin King , Xin Gao , Le Song , Yu Li

The identification of active binding drugs for target proteins (termed as drug-target interaction prediction) is the key challenge in virtual screening, which plays an essential role in drug discovery. Although recent deep learning-based…

Machine Learning · Computer Science 2021-10-18 Siyuan Liu , Yusong Wang , Tong Wang , Yifan Deng , Liang He , Bin Shao , Jian Yin , Nanning Zheng , Tie-Yan Liu

Drug-target interaction (DTI) prediction plays a very important role in drug development and drug discovery. Biochemical experiments or \textit{in vitro} methods are very expensive, laborious and time-consuming. Therefore, \textit{in…

Machine Learning · Computer Science 2018-05-04 Ratha Pech , Dong Hao , Yan-Li Lee , Maryna Po , Tao Zhou

Prediction of protein-ligand (PL) binding affinity remains the key to drug discovery. Popular approaches in recent years involve graph neural networks (GNNs), which are used to learn the topology and geometry of PL complexes. However, GNNs…

Machine Learning · Computer Science 2022-05-17 Dmitrii Gavrilev , Nurlybek Amangeldiuly , Sergei Ivanov , Evgeny Burnaev

Personalized drug response has received public awareness in recent years. How to combine gene test result and drug sensitivity records is regarded as essential in the real-world implementation. Research articles are good sources to train…

Social and Information Networks · Computer Science 2019-06-20 Shiyin Wang

The cornerstone of computational drug design is the calculation of binding affinity between two biological counterparts, especially a chemical compound, i.e., a ligand, and a protein. Predicting the strength of protein-ligand binding with…

Biomolecules · Quantitative Biology 2019-12-04 Yanjun Li , Mohammad A. Rezaei , Chenglong Li , Xiaolin Li , Dapeng Wu

Predicting drug-target interactions (DTI) via reliable computational methods is an effective and efficient way to mitigate the enormous costs and time of the drug discovery process. Structure-based drug similarities and sequence-based…

Machine Learning · Computer Science 2021-07-12 Bin Liu , Konstantinos Pliakos , Celine Vens , Grigorios Tsoumakas

Is it feasible to create an analysis paradigm that can analyze and then accurately and quickly predict known drugs from experimental data? PharML.Bind is a machine learning toolkit which is able to accomplish this feat. Utilizing deep…

Biomolecules · Quantitative Biology 2019-11-15 Aaron D. Vose , Jacob Balma , Damon Farnsworth , Kaylie Anderson , Yuri K. Peterson

Traditional drug design faces significant challenges due to inherent chemical and biological complexities, often resulting in high failure rates in clinical trials. Deep learning advancements, particularly generative models, offer potential…

Quantitative Methods · Quantitative Biology 2025-08-27 Mahsa Sheikholeslami , Navid Mazrouei , Yousof Gheisari , Afshin Fasihi , Matin Irajpour , Ali Motahharynia