Abstract
Physics-based docking methods have long been the cornerstone of structure-based virtual screening (VS). However, the emergence of machine learning (ML)-based docking approaches has opened new possibilities for enhancing VS technologies. In this study, we explore the integration of DiffDock-L, a leading ML-based pose sampling method, into VS workflows by combining it with the Vina, Gnina, and RTMScore scoring functions. We assess this integrated approach in terms of its VS effectiveness, pose sampling quality, and complementarity to traditional physics-based docking methods, such as AutoDock Vina. Our findings from the DUDE-Z benchmark dataset show that DiffDock-L performs competitively in both VS performance and pose sampling in cross-docking settings. In most cases, it generates physically plausible and biologically relevant poses, establishing itself as a viable alternative to physics-based docking algorithms. Additionally, we found that the choice of scoring function significantly influences VS success.
| Original language | English |
|---|---|
| Pages (from-to) | 4833-4843 |
| Number of pages | 11 |
| Journal | Journal of Chemical Information and Modeling |
| Volume | 65 |
| Issue number | 10 |
| Early online date | 9 May 2025 |
| DOIs | |
| Publication status | Published - 26 May 2025 |
Funding
We thank Klaus-Ju\u0308rgen Schleifer and Miriam Mathea from BASF SE, along with Andreas Bergner from Boehringer-Ingelheim RCV GmbH & Co KG for fruitful discussions. We thank William Schueller for technical support and the anonymous reviewers for their thoughtful comments and helpful advice. The financial support received for the Christian Doppler Laboratory for Molecular Informatics in the Biosciences from the Austrian Federal Ministry of Labour and Economy, the National Foundation for Research, Technology and Development, the Christian Doppler Research Association, Boehringer-Ingelheim RCV GmbH & Co KG, and BASF SE is gratefully acknowledged.
Austrian Fields of Science 2012
- 102001 Artificial intelligence
- 106005 Bioinformatics
- 301207 Pharmaceutical chemistry
Keywords
- Machine Learning
- Molecular Docking Simulation
- Proteins/chemistry
- Drug Evaluation, Preclinical/methods
- Protein Conformation
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