How many crystal structures do you need to trust your docking results?
Payne, A. M.; Kaminow, B.; MacDermott-Opeskin, H.; Pulido, I.; Scheen, J.; Castellanos, M. A.; Fearon, D.; Chodera, J. D.; Singh, S.
Show abstract
Structure-based drug discovery relies on the prediction of protein-bound poses of new molecule designs, the accuracy of which can impact downstream prioritization. While it is expected that crystal structures of similar molecules would provide the best template for predicting the poses of new designs, the time and cost required motivates identifying a point of diminishing returns for collecting new structures. Using 403 crystal structures of SARS-CoV-2 main protease from the open science COVID Moonshot project, we explore the tradeoff between the cost and utility of obtaining crystal structures for accurately predicting poses of designed molecules. We observe that similar reference ligands enable superior pose prediction and show that success plateaus after approximately five crystal structures per generic Bemis-Murcko scaffold, exceeding 95% for the campaign's lead series. This work provides practical recommendations for resource allocation in structure-enabled drug discovery campaigns.
Matching journals
The top 1 journal accounts for 50% of the predicted probability mass.
Similar papers in this journal
- QMAP: A Benchmark for Standardized Evaluation of Antimicrobial Peptide MIC and Hemolytic Activity Regression 94%
- Smart Distributed Data Factory: Volunteer Computing Platform for Active Learning-Driven Molecular Data Acquisition 93%
- Benchmarking Protein Language Models for Protein Crystallization 92%
Similar papers in this journal
Similar papers in this journal
"Similar papers" are the closest papers from that journal in the model's embedding space. They show what the match is built on, but the ranking comes mostly from a classifier over the whole training set, not from these examples alone.