Learned Conformational Space and Pharmacophore Into Molecular Foundational Model

The emergence of large-scale chemical pre-trained models has significantly advanced our ability to capture complex relationships between molecular structures and their functions. Despite the growing interest in molecular foundational model that provide versatile representations and support molecular optimization for downstream tasks, few efforts have integrated explicit chemical knowledge-such as conformational and pharmacophore information-into pre-training. Given the highly dynamic nature of small molecules in solution, their conformational changes upon target binding, and the critical role of pharmacophore complementarity, it is essential to incorporate these factors into molecular foundational modeling. Here, we present a molecular foundational model that integrates conformational-space and pharmacophore-similarity projections during pre-training to regularize the representation space. The model adopts an Ouroboros-like architecture, where the molecular graphs are encoded into 1D representation vectors via a graph neural network and subsequently reconstructed back into SMILES sequences through an autoregressive Transformer module. This dual-module design establishes a flexible and extensible framework for both representation learning and molecular generation within a unified latent space. Extensive experiments demonstrate that our model effectively addresses a variety of practical chemical challenges, including similarity-based virtual screening, targeted poly-pharmacology design, chemical property prediction, and directed molecular optimization.

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Publication Details

Journal
Advanced Science
Published
2026-01-04
DOI
https://doi.org/10.1002/advs.202513556
Primary Topic
Computational Drug Discovery Methods
Type
article
Field-Weighted Citation Impact
0.00

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article

Learned Conformational Space and Pharmacophore Into Molecular Foundational Model

Yifan Wu, C. J. Chen, J. L. Zhang, Y. Z. Zhou et al.
Advanced Science
Computational Drug Discovery Methods
article

Learned Conformational Space and Pharmacophore Into Molecular Foundational Model

Yifan Wu, C. J. Chen, J. L. Zhang, Y. Z. Zhou, Chris Liu, Minglong Liang, Yang Zhang, Hao Luo, Lin Wang
article en

Abstract

The emergence of large-scale chemical pre-trained models has significantly advanced our ability to capture complex relationships between molecular structures and their functions. Despite the growing interest in molecular foundational model that provide versatile representations and support molecular optimization for downstream tasks, few efforts have integrated explicit chemical knowledge-such as conformational and pharmacophore information-into pre-training. Given the highly dynamic nature of small molecules in solution, their conformational changes upon target binding, and the critical role of pharmacophore complementarity, it is essential to incorporate these factors into molecular foundational modeling. Here, we present a molecular foundational model that integrates conformational-space and pharmacophore-similarity projections during pre-training to regularize the representation space. The model adopts an Ouroboros-like architecture, where the molecular graphs are encoded into 1D representation vectors via a graph neural network and subsequently reconstructed back into SMILES sequences through an autoregressive Transformer module. This dual-module design establishes a flexible and extensible framework for both representation learning and molecular generation within a unified latent space. Extensive experiments demonstrate that our model effectively addresses a variety of practical chemical challenges, including similarity-based virtual screening, targeted poly-pharmacology design, chemical property prediction, and directed molecular optimization.

Advanced ScienceVol. 13(17)
National University of Singapore (SG), Chinese Academy of Medical Sciences & Peking Union Medical College (CN), Suzhou University of Science and Technology (CN), National University Cancer Institute, Singapore (SG), Suzhou Institute of Systems Medicine (CN)
Agency for Science, Technology and Research, Ministry of Education, India, Chinese Academy of Medical Sciences, Peking Union Medical College, Fundamental Research Funds for the Central Universities
Openalex Percentile: Top 95%
Computational Drug Discovery Methods
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