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In silico drug-target interaction (DTI) prediction is an important and challenging problem in biomedical research with a huge potential benefit to the pharmaceutical industry and patients. Most existing methods for DTI prediction including…

Machine Learning · Computer Science 2019-08-22 Qingyuan Feng , Evgenia Dueva , Artem Cherkasov , Martin Ester

Predicting drug-target binding affinity (DTA) is essential for identifying potential therapeutic candidates in drug discovery. However, most existing models rely heavily on static protein structures, often overlooking the dynamic nature of…

Robotics · Computer Science 2025-05-20 Dan Luo , Jinyu Zhou , Le Xu , Sisi Yuan , Xuan Lin

Predicting the interaction between a compound and a target is crucial for rapid drug repurposing. Deep learning has been successfully applied in drug-target affinity (DTA) problem. However, previous deep learning-based methods ignore…

Machine Learning · Computer Science 2020-09-29 Tri Minh Nguyen , Thin Nguyen , Thao Minh Le , Truyen Tran

The field of drug discovery hinges on the accurate prediction of binding affinity between prospective drug molecules and target proteins, especially when such proteins directly influence disease progression. However, estimating binding…

Empirical scoring functions based on either molecular force fields or cheminformatics descriptors are widely used, in conjunction with molecular docking, during the early stages of drug discovery to predict potency and binding affinity of a…

Machine Learning · Computer Science 2017-03-31 Joseph Gomes , Bharath Ramsundar , Evan N. Feinberg , Vijay S. Pande

Accurate prediction of protein-ligand binding affinity is critical for drug discovery. While recent deep learning approaches have demonstrated promising results, they often rely solely on structural features of proteins and ligands,…

Machine Learning · Computer Science 2026-01-23 Han Liu , Keyan Ding , Peilin Chen , Yinwei Wei , Liqiang Nie , Dapeng Wu , Shiqi Wang

We devise an approach for targeted molecular design, a problem of interest in computational drug discovery: given a target protein site, we wish to generate a chemical with both high binding affinity to the target and satisfactory…

Artificial Intelligence · Computer Science 2018-09-07 Tristan Aumentado-Armstrong

Drug-target interaction is fundamental in understanding how drugs affect biological systems, and accurately predicting drug-target affinity (DTA) is vital for drug discovery. Recently, deep learning methods have emerged as a significant…

Machine Learning · Computer Science 2024-12-30 Minghui Li , Zikang Guo , Yang Wu , Peijin Guo , Yao Shi , Shengshan Hu , Wei Wan , Shengqing Hu

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

Predicting a ligand's bound pose to a target protein is a key component of early-stage computational drug discovery. Recent developments in machine learning methods have focused on improving pose quality at the cost of model runtime. For…

Biomolecules · Quantitative Biology 2024-10-23 Wojtek Treyde , Seohyun Chris Kim , Nazim Bouatta , Mohammed AlQuraishi

The work for predicting drug and target affinity(DTA) is crucial for drug development and repurposing. In this work, we propose a novel method called GDGRU-DTA to predict the binding affinity between drugs and targets, which is based on…

Quantitative Methods · Quantitative Biology 2022-04-27 Lyu Zhijian , Jiang Shaohua , Liang Yigao , Gao Min

Motivation: Prediction of the interaction affinity between proteins and compounds is a major challenge in the drug discovery process. WideDTA is a deep-learning based prediction model that employs chemical and biological textual sequence…

Quantitative Methods · Quantitative Biology 2019-02-13 Hakime Öztürk , Elif Ozkirimli , Arzucan Özgür

Despite recent advances in protein-ligand structure prediction, deep learning methods remain limited in their ability to accurately predict binding affinities, particularly for novel protein targets dissimilar from the training set. In…

Quantitative Methods · Quantitative Biology 2025-12-04 Michael Brocidiacono , James Wellnitz , Konstantin I. Popov , Alexander Tropsha

Structure-based drug design (SBDD) aims to generate ligands that bind strongly and specifically to target protein pockets. Recent diffusion models have advanced SBDD by capturing the distributions of atomic positions and types, yet they…

Machine Learning · Computer Science 2026-02-11 Yue Jian , Curtis Wu , Danny Reidenbach , Aditi S. Krishnapriyan

Accurate prediction of compound-protein interactions (CPI) remains a cornerstone challenge in computational drug discovery. While existing sequence-based approaches leverage molecular fingerprints or graph representations, they critically…

Machine Learning · Computer Science 2025-04-08 Ngoc-Quang Nguyen

Deep Learning (DL) algorithms hold great promise for applications in the field of computational biophysics. In fact, the vast amount of available molecular structures, as well as their notable complexity, constitutes an ideal context in…

Soft Condensed Matter · Physics 2019-01-07 Marco Giulini , Raffaello Potestio

Predicting drug-target affinity is fundamental to virtual screening and lead optimization. However, existing deep models often suffer from representation collapse in stringent cold-start regimes, where the scarcity of labels and domain…

Machine Learning · Statistics 2026-03-13 Yining Qian , Pengjie Wang , Yixiao Li , An-Yang Lu , Cheng Tan , Shuang Li , Lijun Liu

The discovery of drug-target interactions (DTIs) is a very promising area of research with great potential. The accurate identification of reliable interactions among drugs and proteins via computational methods, which typically leverage…

Quantitative Methods · Quantitative Biology 2022-12-06 Bin Liu , Dimitrios Papadopoulos , Fragkiskos D. Malliaros , Grigorios Tsoumakas , Apostolos N. Papadopoulos

Accurate prediction of drug-target interactions (DTI) is crucial for drug discovery. Recently, deep learning (DL) models for show promising performance for DTI prediction. However, these models can be difficult to use for both computer…

Machine Learning · Computer Science 2020-12-11 Kexin Huang , Tianfan Fu , Lucas Glass , Marinka Zitnik , Cao Xiao , Jimeng Sun

Drug-Target Interaction (DTI) prediction is vital for drug discovery, yet challenges persist in achieving model interpretability and optimizing performance. We propose a novel transformer-based model, FragXsiteDTI, that aims to address…