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Predicting protein-ligand binding affinity is an essential part of computer-aided drug design. However, generalisable and performant global binding affinity models remain elusive, particularly in low data regimes. Despite the evolution of…

Machine Learning · Computer Science 2024-09-23 Julia Buhmann , Ward Haddadin , Lukáš Pravda , Alan Bilsland , Hagen Triendl

In this work, we introduce Auxiliary Discriminator Sequence Generative Adversarial Networks (ADSeqGAN), a novel approach for molecular generation in small-sample datasets. Traditional generative models often struggle with limited training…

Machine Learning · Computer Science 2025-09-15 Haocheng Tang , Jing Long , Beihong Ji , Junmei Wang

De novo 3D molecule generation is a pivotal task in drug discovery. However, many recent geometric generative models struggle to produce high-quality 3D structures, even if they maintain 2D validity and topological stability. To tackle this…

Machine Learning · Computer Science 2025-05-27 Danny Reidenbach , Filipp Nikitin , Olexandr Isayev , Saee Paliwal

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

Drug discovery using deep learning has attracted a lot of attention of late as it has obvious advantages like higher efficiency, less manual guessing and faster process time. In this paper, we present a novel neural network for generating…

Biomolecules · Quantitative Biology 2021-10-08 Abhinav Sagar

Molecular generation and molecular property prediction are both crucial for drug discovery, but they are often developed independently. Inspired by recent studies, which demonstrate that diffusion model, a prominent generative approach, can…

Machine Learning · Computer Science 2025-04-07 Shikun Feng , Yuyan Ni , Yan Lu , Zhi-Ming Ma , Wei-Ying Ma , Yanyan Lan

Structure-based drug design, i.e., finding molecules with high affinities to the target protein pocket, is one of the most critical tasks in drug discovery. Traditional solutions, like virtual screening, require exhaustively searching on a…

Biomolecules · Quantitative Biology 2023-02-16 Shuqi Lu , Lin Yao , Xi Chen , Hang Zheng , Di He , Guolin Ke

We introduce MolMiner, a fragment-based, geometry-aware, and order-agnostic autoregressive model for molecular design. MolMiner supports conditional generation of molecules over twelve properties, enabling flexible control across…

Machine Learning · Computer Science 2025-05-27 Raul Ortega-Ochoa , Tejs Vegge , Jes Frellsen

Diffusion generative models have emerged as a powerful framework for addressing problems in structural biology and structure-based drug design. These models operate directly on 3D molecular structures. Due to the unfavorable scaling of…

Biomolecules · Quantitative Biology 2024-05-10 Ian Dunn , David Ryan Koes

With the recent advances in machine learning for quantum chemistry, it is now possible to predict the chemical properties of compounds and to generate novel molecules. Existing generative models mostly use a string- or graph-based…

Biomolecules · Quantitative Biology 2020-10-14 Vitali Nesterov , Mario Wieser , Volker Roth

Computational biology offers immense potential for reducing the high costs and protracted cycles of new drug development through adverse drug reaction (ADR) prediction. However, current methods remain impeded by drug data scarcity-induced…

Machine Learning · Computer Science 2026-01-06 Yuyan Pi , Min Jin , Wentao Xie , Xinhua Liu

The de novo design of molecular structures using deep learning generative models introduces an encouraging solution to drug discovery in the face of the continuously increased cost of new drug development. From the generation of original…

Biomolecules · Quantitative Biology 2021-02-08 Yuemin Bian , Xiang-Qun Xie

A fundamental problem in drug discovery is to design molecules that bind to specific proteins. To tackle this problem using machine learning methods, here we propose a novel and effective framework, known as GraphBP, to generate 3D…

Biomolecules · Quantitative Biology 2022-05-31 Meng Liu , Youzhi Luo , Kanji Uchino , Koji Maruhashi , Shuiwang Ji

Generating novel graph structures that optimize given objectives while obeying some given underlying rules is fundamental for chemistry, biology and social science research. This is especially important in the task of molecular graph…

Machine Learning · Computer Science 2019-02-26 Jiaxuan You , Bowen Liu , Rex Ying , Vijay Pande , Jure Leskovec

Generative AI has made rapid progress in text, image, and video synthesis, yet text-to-3D modeling for scientific design remains particularly challenging due to limited controllability and high computational cost. Most existing 3D…

Graphics · Computer Science 2026-04-01 Rachel K. Luu , Markus J. Buehler

Generating a novel and optimized molecule with desired chemical properties is an essential part of the drug discovery process. Failure to meet one of the required properties can frequently lead to failure in a clinical test which is costly.…

Machine Learning · Computer Science 2020-10-28 Bonggun Shin , Sungsoo Park , JinYeong Bak , Joyce C. Ho

Generative modeling has emerged as a powerful paradigm for representation learning, but its direct applicability to challenging fields like medical imaging remains limited: mere generation, without task alignment, fails to provide a robust…

Machine Learning · Computer Science 2025-10-28 Luca Caldera , Giacomo Bottacini , Lara Cavinato

Generative Adversarial Networks (GANs) are proficient at generating synthetic data but continue to suffer from mode collapse, where the generator produces a narrow range of outputs that fool the discriminator but fail to capture the full…

Machine Learning · Computer Science 2025-11-03 Mahsa Valizadeh , Rui Tuo , James Caverlee

Deep generative models provide state-of-the-art performance across a wide array of applications, with recent studies showing increasing applicability for science and engineering. Despite a growing corpus of literature focused on the…

Machine Learning · Computer Science 2026-05-14 Jacob K. Christopher , James E. Warner , Ferdinando Fioretto

The accurate screening of candidate drug ligands against target proteins through computational approaches is of prime interest to drug development efforts. Such virtual screening depends in part on methods to predict the binding affinity…

Machine Learning · Computer Science 2024-10-22 Ho-Joon Lee , Prashant S. Emani , Mark B. Gerstein
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