FoXSight: Facilitating Computational Hit Identification in Crystallographic Fragment Screening Experiments

X-ray crystallographic fragment screening reveals how small molecules bind to proteins, providing important starting points for drug design. Identifying these weak binding events remains difficult when electron density signals are noisy, partially occupied or obscured by solvent, and campaigns may comprise thousands of datasets. Here, we present FoXSight, a computational method for hit identification in crystallographic compound screening. FoXSight applies Difference-of-Gaussian (DoG) filtering to multi-reference subtraction maps to detect recurring, target-specific density features associated with bound ligands. Its output maps remain visually interpretable and support subsequent ligand modeling. We evaluated FoXSight on in-house and public datasets spanning seven protein targets, comparing its maps with PanDDA where suitable comparison data were available. FoXSight was successfully used as the primary hit identification tool in a challenging crystallographic fragment screening campaign for human Cathepsin L, where the output of established methods was impractical to inspect systematically.

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Publication Details

Journal
bioRxiv (Cold Spring Harbor Laboratory)
Published
2026-11-03
DOI
https://doi.org/10.64898/2026.11.01.763443
Primary Topic
Enzyme Structure and Function
Type
preprint
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preprint

FoXSight: Facilitating Computational Hit Identification in Crystallographic Fragment Screening Experiments

Alke Meents, Sebastian Guenther, Sven Falke, Matthias Rarey et al.
bioRxiv (Cold Spring Harbor Laboratory)
Enzyme Structure and Function
preprint

FoXSight: Facilitating Computational Hit Identification in Crystallographic Fragment Screening Experiments

Alke Meents, Sebastian Guenther, Sven Falke, Matthias Rarey, T.G. Schulze
preprint en

Abstract

X-ray crystallographic fragment screening reveals how small molecules bind to proteins, providing important starting points for drug design. Identifying these weak binding events remains difficult when electron density signals are noisy, partially occupied or obscured by solvent, and campaigns may comprise thousands of datasets. Here, we present FoXSight, a computational method for hit identification in crystallographic compound screening. FoXSight applies Difference-of-Gaussian (DoG) filtering to multi-reference subtraction maps to detect recurring, target-specific density features associated with bound ligands. Its output maps remain visually interpretable and support subsequent ligand modeling. We evaluated FoXSight on in-house and public datasets spanning seven protein targets, comparing its maps with PanDDA where suitable comparison data were available. FoXSight was successfully used as the primary hit identification tool in a challenging crystallographic fragment screening campaign for human Cathepsin L, where the output of established methods was impractical to inspect systematically.

bioRxiv (Cold Spring Harbor Laboratory)
Universität Hamburg (DE), Deutsches Elektronen-Synchrotron DESY (DE)
Enzyme Structure and Function
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FoXSight: Facilitating Computational Hit Identification in Crystallographic Fragment Screening Experiments — Alke Meents, Sebastian Guenther, et al. · bioRxiv (Cold Spring Harbor Laboratory) (2026) | TGRS Research Map | TGRS