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The fundamental goal of generative drug design is to propose optimized molecules that meet predefined activity, selectivity, and pharmacokinetic criteria. Despite recent progress, we argue that existing generative methods are limited in…

Chemical Physics · Physics 2020-12-17 Julien Horwood , Emmanuel Noutahi

Denoising diffusion models have shown great potential in multiple research areas. Existing diffusion-based generative methods on de novo 3D molecule generation face two major challenges. Since majority heavy atoms in molecules allow…

Machine Learning · Computer Science 2024-04-23 Can Xu , Haosen Wang , Weigang Wang , Pengfei Zheng , Hongyang Chen

Designing molecules with specific properties is a long-lasting research problem and is central to advancing crucial domains such as drug discovery and material science. Recent advances in deep graph generative models treat molecule design…

Machine Learning · Computer Science 2022-03-02 Yuanqi Du , Xiaojie Guo , Amarda Shehu , Liang Zhao

Molecular generation with diffusion models has emerged as a promising direction for AI-driven drug discovery and materials science. While graph diffusion models have been widely adopted due to the discrete nature of 2D molecular graphs,…

Artificial Intelligence · Computer Science 2026-02-20 Hojung Jung , Rodrigo Hormazabal , Jaehyeong Jo , Youngrok Park , Kyunggeun Roh , Se-Young Yun , Sehui Han , Dae-Woong Jeong

Molecular generation, an essential method for identifying new drug structures, has been supported by advancements in machine learning and computational technology. However, challenges remain in multi-objective generation, model…

Biomolecules · Quantitative Biology 2024-04-11 Ningfeng Liu , Jie Yu , Siyu Xiu , Xinfang Zhao , Siyu Lin , Bo Qiang , Ruqiu Zheng , Hongwei Jin , Liangren Zhang , Zhenming Liu

Deep generative models are able to suggest new organic molecules by generating strings, trees, and graphs representing their structure. While such models allow one to generate molecules with desirable properties, they give no guarantees…

Machine Learning · Computer Science 2019-12-05 John Bradshaw , Brooks Paige , Matt J. Kusner , Marwin H. S. Segler , José Miguel Hernández-Lobato

Diffusion models, a powerful and universal generative AI technology, have achieved tremendous success in computer vision, audio, reinforcement learning, and computational biology. In these applications, diffusion models provide flexible…

Machine Learning · Computer Science 2024-04-12 Minshuo Chen , Song Mei , Jianqing Fan , Mengdi Wang

Molecule generation is a challenging open problem in cheminformatics. Currently, deep generative approaches addressing the challenge belong to two broad categories, differing in how molecules are represented. One approach encodes molecular…

Machine Learning · Statistics 2020-11-02 Marco Podda , Davide Bacciu , Alessio Micheli

Machine learning in drug discovery has been focused on virtual screening of molecular libraries using discriminative models. Generative models are an entirely different approach that learn to represent and optimize molecules in a continuous…

Quantitative Methods · Quantitative Biology 2020-11-17 Matthew Ragoza , Tomohide Masuda , David Ryan Koes

Designing new molecules with a set of predefined properties is a core problem in modern drug discovery and development. There is a growing need for de-novo design methods that would address this problem. We present MolecularRNN, the graph…

Machine Learning · Computer Science 2019-06-03 Mariya Popova , Mykhailo Shvets , Junier Oliva , Olexandr Isayev

Molecular conformation generation, a critical aspect of computational chemistry, involves producing the three-dimensional conformer geometry for a given molecule. Generating molecular conformation via diffusion requires learning to reverse…

Computational Physics · Physics 2023-10-10 Zihan Zhou , Ruiying Liu , Chaolong Ying , Ruimao Zhang , Tianshu Yu

Molecule generation is advancing rapidly in chemical discovery and drug design. Flow matching methods have recently set the state of the art (SOTA) in unconditional molecule generation, surpassing score-based diffusion models. However,…

In recent years, deep learning techniques have made significant strides in molecular generation for specific targets, driving advancements in drug discovery. However, existing molecular generation methods present significant limitations:…

Machine Learning · Computer Science 2025-03-12 Taojie Kuang , Qianli Ma , Athanasios V. Vasilakos , Yu Wang , Qiang , Cheng , Zhixiang Ren

Molecular representation learning has shown great success in advancing AI-based drug discovery. The core of many recent works is based on the fact that the 3D geometric structure of molecules provides essential information about their…

Machine Learning · Computer Science 2024-10-23 Jiying Zhang , Zijing Liu , Yu Wang , Yu Li

Molecular optimization is a key challenge in drug discovery and material science domain, involving the design of molecules with desired properties. Existing methods focus predominantly on single-property optimization, necessitating…

Machine Learning · Computer Science 2024-09-13 Aye Phyu Phyu Aung , Jay Chaudhary , Ji Wei Yoon , Senthilnath Jayavelu

The rational design of molecules with desired properties is a long-standing challenge in chemistry. Generative neural networks have emerged as a powerful approach to sample novel molecules from a learned distribution. Here, we propose a…

Small-molecule drug discovery requires simultaneous optimization of numerous properties of candidate molecules. These properties can be investigated through the analysis of high-dimensional biological signatures, such as cell morphology and…

Machine Learning · Computer Science 2026-05-28 Łukasz Janisiów , Sebastian Musiał , Bartosz Zieliński , Dawid Rymarczyk , Tomasz Danel

Molecular dynamics (MD) has long been the de facto choice for simulating complex atomistic systems from first principles. Recently deep learning models become a popular way to accelerate MD. Notwithstanding, existing models depend on…

Computational Engineering, Finance, and Science · Computer Science 2023-01-10 Fang Wu , Stan Z. Li

Generating desirable molecular structures in 3D is a fundamental problem for drug discovery. Despite the considerable progress we have achieved, existing methods usually generate molecules in atom resolution and ignore intrinsic local…

Biomolecules · Quantitative Biology 2023-05-29 Bo Qiang , Yuxuan Song , Minkai Xu , Jingjing Gong , Bowen Gao , Hao Zhou , Weiying Ma , Yanyan Lan

Generating novel drug molecules with desired biological properties is a time consuming and complex task. Conditional generative adversarial models have recently been proposed as promising approaches for de novo drug design. In this paper,…

Quantitative Methods · Quantitative Biology 2021-10-26 Yuansan Liu , James Bailey