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Deep generative models have achieved tremendous success in designing novel drug molecules in recent years. A new thread of works have shown the great potential in advancing the specificity and success rate of in silico drug design by…

Machine Learning · Computer Science 2025-07-14 Xingang Peng , Shitong Luo , Jiaqi Guan , Qi Xie , Jian Peng , Jianzhu Ma

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…

Generating novel active molecules for a given protein is an extremely challenging task for generative models that requires an understanding of the complex physical interactions between the molecule and its environment. In this paper, we…

We study a fundamental problem in computational chemistry known as molecular conformation generation, trying to predict stable 3D structures from 2D molecular graphs. Existing machine learning approaches usually first predict distances…

Machine Learning · Computer Science 2021-06-09 Chence Shi , Shitong Luo , Minkai Xu , Jian Tang

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

Proteins in complex with small molecule ligands represent the core of structure-based drug discovery. However, three-dimensional representations are absent from most deep-learning-based generative models. We here present a graph-based…

Biomolecules · Quantitative Biology 2022-04-07 Seung-gu Kang , Jeffrey K. Weber , Joseph A. Morrone , Leili Zhang , Tien Huynh , Wendy D. Cornell

Learning on 3D structures of large biomolecules is emerging as a distinct area in machine learning, but there has yet to emerge a unifying network architecture that simultaneously leverages the graph-structured and geometric aspects of the…

Biomolecules · Quantitative Biology 2021-05-18 Bowen Jing , Stephan Eismann , Patricia Suriana , Raphael J. L. Townshend , Ron Dror

Molecule generation, especially generating 3D molecular geometries from scratch (i.e., 3D \textit{de novo} generation), has become a fundamental task in drug designs. Existing diffusion-based 3D molecule generation methods could suffer from…

Machine Learning · Computer Science 2022-09-14 Lei Huang , Hengtong Zhang , Tingyang Xu , Ka-Chun Wong

Ground-state 3D geometries of molecules are essential for many molecular analysis tasks. Modern quantum mechanical methods can compute accurate 3D geometries but are computationally prohibitive. Currently, an efficient alternative to…

Chemical Physics · Physics 2023-05-24 Zhao Xu , Yaochen Xie , Youzhi Luo , Xuan Zhang , Xinyi Xu , Meng Liu , Kaleb Dickerson , Cheng Deng , Maho Nakata , Shuiwang Ji

A common starting point for drug design is to find small chemical groups or "fragments" that form interactions with distinct subregions in a protein binding pocket. The subsequent challenge is to assemble these fragments into a molecule…

Quantitative Methods · Quantitative Biology 2025-05-29 Rohan V. Koodli , Alexander S. Powers , Ayush Pandit , Chiho Im , Ron O. Dror

Inspired by generative paradigms in image and video, 3D shape generation has made notable progress, enabling the rapid synthesis of high-fidelity 3D assets from a single image. However, current methods still face challenges, including the…

Computer Vision and Pattern Recognition · Computer Science 2025-11-26 Yangguang Li , Xianglong He , Zi-Xin Zou , Zexiang Liu , Wanli Ouyang , Ding Liang , Yan-Pei Cao

Recently, deep generative models for molecular graphs are gaining more and more attention in the field of de novo drug design. A variety of models have been developed to generate topological structures of drug-like molecules, but…

Quantitative Methods · Quantitative Biology 2021-09-16 Yibo Li , Jianfeng Pei , Luhua Lai

We introduce SegviGen, a framework that repurposes native 3D generative models for 3D part segmentation. Existing pipelines either lift strong 2D priors into 3D via distillation or multi-view mask aggregation, often suffering from…

Computer Vision and Pattern Recognition · Computer Science 2026-05-12 Lin Li , Haoran Feng , Zehuan Huang , Haohua Chen , Wenbo Nie , Shaohua Hou , Keqing Fan , Pan Hu , Sheng Wang , Buyu Li , Lu Sheng

With the growing demand for high-fidelity 3D models from 2D images, existing methods still face significant challenges in accurately reproducing fine-grained geometric details due to limitations in domain gaps and inherent ambiguities in…

Graphics · Computer Science 2025-04-01 Chongjie Ye , Yushuang Wu , Ziteng Lu , Jiahao Chang , Xiaoyang Guo , Jiaqing Zhou , Hao Zhao , Xiaoguang Han

Learning powerful deep generative models for 3D shape synthesis is largely hindered by the difficulty in ensuring plausibility encompassing correct topology and reasonable geometry. Indeed, learning the distribution of plausible 3D shapes…

Computer Vision and Pattern Recognition · Computer Science 2020-01-28 Jun Li , Chengjie Niu , Kai Xu

Prediction of a molecule's 3D conformer ensemble from the molecular graph holds a key role in areas of cheminformatics and drug discovery. Existing generative models have several drawbacks including lack of modeling important molecular…

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

In recent years, AI-assisted drug design methods have been proposed to generate molecules given the pockets' structures of target proteins. Most of them are atom-level-based methods, which consider atoms as basic components and generate…

Biomolecules · Quantitative Biology 2024-03-19 Haitao Lin , Yufei Huang , Odin Zhang , Lirong Wu , Siyuan Li , Zhiyuan Chen , Stan Z. Li

Generative models for 2D images has recently seen tremendous progress in quality, resolution and speed as a result of the efficiency of 2D convolutional architectures. However it is difficult to extend this progress into the 3D domain since…

Computer Vision and Pattern Recognition · Computer Science 2022-10-07 Hassan Abu Alhaija , Alara Dirik , André Knörig , Sanja Fidler , Maria Shugrina

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