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Inspired by recent progress in dynamic programming approaches for weighted model counting, we investigate a dynamic-programming approach in the context of boolean realizability and synthesis, which takes a conjunctive-normal-form boolean…

Formal Languages and Automata Theory · Computer Science 2024-06-21 Yi Lin , Lucas M. Tabajara , Moshe Y. Vardi

Accurate blind docking has the potential to lead to new biological breakthroughs, but for this promise to be realized, docking methods must generalize well across the proteome. Existing benchmarks, however, fail to rigorously assess…

Biomolecules · Quantitative Biology 2024-02-29 Gabriele Corso , Arthur Deng , Benjamin Fry , Nicholas Polizzi , Regina Barzilay , Tommi Jaakkola

Searching the vast chemical space for drug-like molecules that bind with a protein pocket is a challenging task in drug discovery. Recently, structure-based generative models have been introduced which promise to be more efficient by…

Machine Learning · Computer Science 2024-09-09 Tony Shen , Seonghwan Seo , Grayson Lee , Mohit Pandey , Jason R Smith , Artem Cherkasov , Woo Youn Kim , Martin Ester

Structure-based drug design aims at generating high affinity ligands with prior knowledge of 3D target structures. Existing methods either use conditional generative model to learn the distribution of 3D ligands given target binding sites,…

Biomolecules · Quantitative Biology 2024-03-18 Yuwei Yang , Siqi Ouyang , Xueyu Hu , Mingyue Zheng , Hao Zhou , Lei Li

Protein-ligand structure prediction is an essential task in drug discovery, predicting the binding interactions between small molecules (ligands) and target proteins (receptors). Recent advances have incorporated deep learning techniques to…

Binding affinity optimization is crucial in early-stage drug discovery. While numerous machine learning methods exist for predicting ligand potency, their comparative efficacy remains unclear. This study evaluates the performance of…

Biomolecules · Quantitative Biology 2024-07-30 Nikolai Schapin , Carles Navarro , Albert Bou , Gianni De Fabritiis

Accurately predicting the binding conformation of small-molecule ligands to protein targets is a critical step in rational drug design. Although recent deep learning-based docking surpasses traditional methods in speed and accuracy, many…

Computer Vision and Pattern Recognition · Computer Science 2025-08-14 Liyan Jia , Chuan-Xian Ren , Hong Yan

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

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

Due to the contribution of drug-target binding kinetics to drug efficacy, there is a high level of interest in developing methods to predict drug-target binding kinetic parameters. During the review period, a wide range of enhanced sampling…

Quantitative Methods · Quantitative Biology 2020-08-10 Ariane Nunes-Alves , Daria B. Kokh , Rebecca C. Wade

Deductive verification is an effective method to ensure that a given system exposes the intended behavior. In spite of its proven usefulness and feasibility in selected projects, deductive verification is still not a mainstream technique.…

Software Engineering · Computer Science 2026-01-26 Lea Salome Brugger , Xavier Denis , Peter Müller

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

The widespread application of Artificial Intelligence (AI) techniques has significantly influenced the development of new therapeutic agents. These computational methods can be used to design and predict the properties of generated…

Neural and Evolutionary Computing · Computer Science 2024-08-21 Arthur Cerveira , Frederico Kremer , Darling de Andrade Lourenço , Ulisses B Corrêa

We explored the Protein DataBank (PDB) to collect protein-ssDNA structures and create a multiconformational docking benchmark including both bound and unbound protein structures. Due to ssDNA high flexibility when not bound, no ssDNA…

Quantitative Methods · Quantitative Biology 2022-10-21 Dominique Mias-Lucquin , Isaure Chauvot de Beauchene

Navigating the vast chemical space of druggable compounds is a formidable challenge in drug discovery, where generative models are increasingly employed to identify viable candidates. Conditional 3D structure-based drug design (3D-SBDD)…

Machine Learning · Computer Science 2025-02-04 Kiwoong Yoo , Owen Oertell , Junhyun Lee , Sanghoon Lee , Jaewoo Kang

Molecular docking is a cornerstone of drug discovery to unveil the mechanism of ligand-receptor interactions. With the recent development of deep learning in the field of artificial intelligence, innovative methods were developed for…

Chemical Physics · Physics 2025-10-29 Xuhan Liu , Baohua Zhang , Hong Zhang , Yi Qin Gao

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

The first step in drug discovery is finding drug molecule moieties with medicinal activity against specific targets. Therefore, it is crucial to investigate the interaction between drug-target proteins and small chemical molecules. However,…

Biomolecules · Quantitative Biology 2022-11-15 Boyuan Liu

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

Scaffold based drug discovery (SBDD) is a technique for drug discovery which pins chemical scaffolds as the framework of design. Scaffolds, or molecular frameworks, organize the design of compounds into local neighborhoods. We formalize…

Quantitative Methods · Quantitative Biology 2021-09-13 Austin Clyde , Ashka Shah , Max Zvyagin , Arvind Ramanathan , Rick Stevens
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