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Virtual screening can accelerate drug discovery by identifying promising candidates for experimental evaluation. Machine learning is a powerful method for screening, as it can learn complex structure-property relationships from experimental…

Machine Learning · Computer Science 2021-02-22 Simon Axelrod , Rafael Gomez-Bombarelli

Sampling physically valid ligand-binding poses remains a major challenge in molecular docking, particularly for unseen or structurally diverse targets. We introduce PocketVina, a fast and memory-efficient, search-based docking framework…

Quantitative Methods · Quantitative Biology 2025-06-26 Ahmet Sarigun , Bora Uyar , Vedran Franke , Altuna Akalin

Molecular docking is a structure-based computational drug design technique for predicting the interaction between a small molecule (ligand) and a macromolecule (receptor). Over the past three decades various docking software programs have…

Quantitative Methods · Quantitative Biology 2023-10-18 Katherine Ge , Dayna Olson , Michel F. Sanner

The diffusion learning method, DiffDock, for docking small-molecule ligands into protein binding sites was recently introduced. Results included comparisons to more conventional docking approaches, with DiffDock showing superior…

Artificial Intelligence · Computer Science 2024-12-10 Ajay N. Jain , Ann E. Cleves , W. Patrick Walters

The drug discovery process involves several tasks to be performed in vivo, in vitro and in silico. Molecular docking is a task typically performed in silico. It aims at finding the three-dimensional pose of a given molecule when it…

Distributed, Parallel, and Cluster Computing · Computer Science 2019-01-21 Davide Gadioli , Gianluca Palermo , Stefano Cherubin , Emanuele Vitali , Giovanni Agosta , Candida Manelfi , Andrea R. Beccari , Carlo Cavazzoni , Nico Sanna , Cristina Silvano

Black-box optimization methods play an important role in many fields of computational simulation. In particular, such methods are often used in the design and modelling of biological systems, including proteins and their complexes with…

Biomolecules · Quantitative Biology 2023-02-08 Dmitry Morozov , Artem Melnikov , Vishal Shete , Michael Perelshtein

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…

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

Energy evaluation using fast Fourier transforms enables sampling billions of putative complex structures and hence revolutionized rigid protein-protein docking. However, in current methods efficient acceleration is achieved only in either…

De novo ligand design is a fundamental task that seeks to generate protein or molecule candidates that can effectively dock with protein receptors and achieve strong binding affinity entirely from scratch. It holds paramount significance…

Machine Learning · Computer Science 2025-10-13 Zekai Chen , Xunkai Li , Sirui Zhang , Henan Sun , Jia Li , Zhenjun Li , Bing Zhou , Rong-Hua Li , Guoren Wang

Molecular docking is a critical computational strategy in drug design and discovery, but the complex diversity of biomolecular structures and flexible binding conformations create an enormous search space that challenges conventional…

Computational Physics · Physics 2025-03-27 Yihan He , Ming-Chun Hong , Qiming Ding , Chih-Sheng Lin , Chih-Ming Lai , Chao Fang , Xiao Gong , Tuo-Hung Hou , Gengchiau Liang

Understanding how proteins structurally interact is crucial to modern biology, with applications in drug discovery and protein design. Recent machine learning methods have formulated protein-small molecule docking as a generative problem…

Protein interactions and assembly formation are fundamental to most biological processes. Predicting the assembly structure from constituent proteins -- referred to as the protein docking task -- is thus a crucial step in protein design…

Machine Learning · Computer Science 2023-10-11 Vignesh Ram Somnath , Pier Giuseppe Sessa , Maria Rodriguez Martinez , Andreas Krause

Accurate prediction of protein-ligand binding structures, a task known as molecular docking is crucial for drug design but remains challenging. While deep learning has shown promise, existing methods often depend on holo-protein structures…

Biomolecules · Quantitative Biology 2024-02-22 Yufei Huang , Odin Zhang , Lirong Wu , Cheng Tan , Haitao Lin , Zhangyang Gao , Siyuan Li , Stan. Z. Li

The knowledge of potentially druggable binding sites on proteins is an important preliminary step towards the discovery of novel drugs. The computational prediction of such areas can be boosted by following the recent major advances in the…

Biomolecules · Quantitative Biology 2021-02-17 Stelios K. Mylonas , Apostolos Axenopoulos , Petros Daras

Deep learning promises to dramatically improve scoring functions for molecular docking, leading to substantial advances in binding pose prediction and virtual screening. To train scoring functions-and to perform molecular docking-one must…

Biomolecules · Quantitative Biology 2023-12-04 Patricia Suriana , Ron O. Dror

Molecular docking is a core tool in drug discovery for predicting ligand-target interactions. Despite the availability of diverse search-based and machine learning approaches, no single docking algorithm consistently dominates, as…

Artificial Intelligence · Computer Science 2025-10-01 Siyuan Cao , Hongxuan Wu , Jiabao Brad Wang , Yiliang Yuan , Mustafa Misir

Molecular docking aims to predict the 3D pose of a small molecule in a protein binding site. Traditional docking methods predict ligand poses by minimizing a physics-inspired scoring function. Recently, a diffusion model has been proposed…

Quantitative Methods · Quantitative Biology 2023-07-27 Michael Brocidiacono , Konstantin I. Popov , David Ryan Koes , Alexander Tropsha

Molecular docking is an essential tool for drug design. It helps the scientist to rapidly know if two molecules, respectively called ligand and receptor, can be combined together to obtain a stable complex. We propose a new multi-objective…

Quantitative Methods · Quantitative Biology 2008-11-05 Jean-Charles Boisson , Laetitia Jourdan , El-Ghazali Talbi , Dragos Horvath

Understanding the structure of the protein-ligand complex is crucial to drug development. Existing virtual structure measurement and screening methods are dominated by docking and its derived methods combined with deep learning. However,…

Artificial Intelligence · Computer Science 2024-08-22 Kelei He , Tiejun Dong , Jinhui Wu , Junfeng Zhang