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Molecular docking is a cornerstone of drug discovery, relying on high-resolution ligand-bound structures to achieve accurate predictions. However, obtaining these structures is often costly and time-intensive, limiting their availability.…

Biomolecules · Quantitative Biology 2025-09-09 Raúl Miñán , Carles Perez-Lopez , Javier Iglesias , Álvaro Ciudad , Alexis Molina

Massive molecular simulations of drug-target proteins have been used as a tool to understand disease mechanism and develop therapeutics. This work focuses on learning a generative neural network on a structural ensemble of a drug-target…

Machine Learning · Computer Science 2022-05-24 N. Joseph Tatro , Payel Das , Pin-Yu Chen , Vijil Chenthamarakshan , Rongjie Lai

Currently, the field of structure-based drug design is dominated by three main types of algorithms: search-based algorithms, deep generative models, and reinforcement learning. While existing works have typically focused on comparing models…

Machine Learning · Computer Science 2024-06-06 Kangyu Zheng , Yingzhou Lu , Zaixi Zhang , Zhongwei Wan , Yao Ma , Marinka Zitnik , Tianfan Fu

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

Predicting the 3D structure of a macromolecule, such as a protein or an RNA molecule, is ranked top among the most difficult and attractive problems in bioinformatics and computational biology. Its importance comes from the relationship…

Biomolecules · Quantitative Biology 2016-12-14 Zhiyong Wang

Designing 3D ligands within a target binding site is a fundamental task in drug discovery. Existing structured-based drug design methods treat all ligand atoms equally, which ignores different roles of atoms in the ligand for drug design…

Biomolecules · Quantitative Biology 2024-03-14 Jiaqi Guan , Xiangxin Zhou , Yuwei Yang , Yu Bao , Jian Peng , Jianzhu Ma , Qiang Liu , Liang Wang , Quanquan Gu

Computer-Aided Drug Discovery research has proven to be a promising direction in drug discovery. In recent years, Deep Learning approaches have been applied to problems in the domain such as Drug-Target Interaction Prediction and have shown…

Machine Learning · Computer Science 2020-04-28 Brighter Agyemang , Wei-Ping Wu , Michael Y. Kpiebaareh , Ebenezer Nanor

Currently, the field of structure-based drug design is dominated by three main types of algorithms: search-based algorithms, deep generative models, and reinforcement learning. While existing works have typically focused on comparing models…

Machine Learning · Computer Science 2026-01-22 Kangyu Zheng , Kai Zhang , Jiale Tan , Xuehan Chen , Yingzhou Lu , Zaixi Zhang , Lichao Sun , Marinka Zitnik , Tianfan Fu , Zhiding Liang

Prediction of ligand binding sites of proteins is a fundamental and important task for understanding the function of proteins and screening potential drugs. Most existing methods require experimentally determined protein holo-structures as…

Quantitative Methods · Quantitative Biology 2023-12-07 Shuo Zhang , Lei Xie

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

Virtual screening aims to efficiently identify active ligands from massive chemical libraries for a given target pocket. Recent CLIP-style models such as DrugCLIP enable scalable virtual screening by embedding pockets and ligands into a…

Machine Learning · Computer Science 2026-02-18 Anjie Qiao , Zhen Wang , Yaliang Li , Jiahua Rao , Yuedong Yang

Structure-based drug design (SBDD) is a critical task in drug discovery, requiring the generation of molecular information across two distinct modalities: discrete molecular graphs and continuous 3D coordinates. However, existing SBDD…

Computational Engineering, Finance, and Science · Computer Science 2025-03-28 Xiuyuan Hu , Guoqing Liu , Can Chen , Yang Zhao , Hao Zhang , Xue Liu

Synthesizability remains a critical bottleneck in generative molecular design. While recent advances have addressed synthesizability in 2D graphs, extending these constraints to 3D for geometry-based conditional generation remains largely…

In this work, we introduce AutoFragDiff, a fragment-based autoregressive diffusion model for generating 3D molecular structures conditioned on target protein structures. We employ geometric vector perceptrons to predict atom types and…

Biomolecules · Quantitative Biology 2024-01-12 Mahdi Ghorbani , Leo Gendelev , Paul Beroza , Michael J. Keiser

Estimating correspondences between pairs of non-rigid deformable 3D shapes remains a significant challenge in computer vision and graphics. While deep functional map methods have become the go-to solution for addressing this problem, they…

Computer Vision and Pattern Recognition · Computer Science 2026-03-20 Feifan Luo , Hongyang Chen

We consider the problem of antibody sequence design given 3D structural information. Building on previous work, we propose a fine-tuned inverse folding model that is specifically optimised for antibody structures and outperforms generic…

Biomolecules · Quantitative Biology 2023-10-31 Frédéric A. Dreyer , Daniel Cutting , Constantin Schneider , Henry Kenlay , Charlotte M. Deane

Optimizing molecular design and discovering novel chemical structures to meet certain objectives, such as quantitative estimates of the drug-likeness score (QEDs), is NP-hard due to the vast combinatorial design space of discrete molecular…

Machine Learning · Computer Science 2023-02-23 Mohammad Sajjad Ghaemi , Hang Hu , Anguang Hu , Hsu Kiang Ooi

Drug discovery is a time-consuming and expensive process, with traditional high-throughput and docking-based virtual screening hampered by low success rates and limited scalability. Recent advances in generative modelling, including…

Artificial Intelligence · Computer Science 2026-03-12 Junkai Ji , Zhangfan Yang , Dong Xu , Ruibin Bai , Jianqiang Li , Tingjun Hou , Zexuan Zhu

Neural networks that incorporate geometric relationships respecting SE(3) group transformations (e.g. rotations and translations) are increasingly important in molecular applications, such as molecular property prediction, protein structure…

Machine Learning · Computer Science 2025-10-21 Jose Siguenza , Bharath Ramsundar

This paper highlights a shift in how to approach material generation. Instead of material-to-material, we propose a language-to-material generation architecture that utilizes millions of untapped data points. Using a web scraper to collect…

Computation and Language · Computer Science 2023-11-15 Neel Redkar
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