Re-evaluating sample efficiency in de novo molecule generation
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Abstract (arXiv)
De novo molecule generation can suffer from data inefficiency; requiring large amounts of training data or many sampled data points to conduct objective optimization. The latter is a particular disadvantage when combining deep generative models with computationally expensive molecule scoring functions (a.k.a. oracles) commonly used in computer-aided drug design. Recent works have therefore focused on methods to improve sample efficiency in the context of de novo molecule drug design, or to benchmark it. In this work, we discuss and adapt a recent sample efficiency benchmark to better reflect realistic goals also with respect to the quality of chemistry generated, which must always be considered in the context of small-molecule drug design; we then re-evaluate all benchmarked generative models. We find that accounting for molecular weight and LogP with respect to the training data, and the diversity of chemistry proposed, re-orders the ranking of generative models. In addition, we benchmark a recently proposed method to improve sample efficiency (Augmented Hill-Climb) and found it ranked top when considering both the sample efficiency and chemistry of molecules generated. Continual improvements in sample efficiency and chemical desirability enable more routine integration of computationally expensive scoring functions on a more realistic timescale.
Key facts. Cited by 8 papers in the map (data through 7 Oct 2026). Builds on 9 of its 30 references that are in the map. First posted on arXiv 1 Dec 2022.
Builds on
9 of 30 references.
References · 9
- 2014Learning Phrase Representations using RNN Encoder-Decoder for Statistical Machine Translationcited by 4,016
- 2016Automatic chemical design using a data-driven continuous representation of moleculescited by 762
- 2018GuacaMol: Benchmarking Models for De Novo Molecular Designcited by 294
- 2018Molecular Sets (MOSES): A Benchmarking Platform for Molecular Generation Modelscited by 270
- 2017Molecular De Novo Design through Deep Reinforcement Learningcited by 264
- 2018Optimization of Molecules via Deep Reinforcement Learningcited by 199
- 2017Deep Reinforcement Learning for De-Novo Drug Designcited by 161
- 2022Sample Efficiency Matters: A Benchmark for Practical Molecular Optimizationcited by 151
- 2021DOCKSTRING: easy molecular docking yields better benchmarks for ligand designcited by 33
Built on by
Citing papers per year: 2023: 2; 2024: 2; 2025: 3; 2026: 1.
8 papers.
- 2023Utilizing Reinforcement Learning for de novo Drug Designcited by 7
- 2023Augmented Memory: Capitalizing on Experience Replay to Accelerate De Novo Molecular Designcited by 7
- 2024GraphXForm: Graph transformer for computer-aided molecular designcited by 6
- 2024Diversity-Aware Reinforcement Learning for de novo Drug Designcited by 3
- 2025REINFORCE-ING Chemical Language Models for Drug Discoverycited by 3
- 2025Test-Time Training Scaling Laws for Chemical Exploration in Drug Designcited by 1
- 2025Diverse Mini-Batch Selection in Reinforcement Learning for Efficient Chemical Exploration in de novo Drug Designcited by 1
- 2026Multi-objective fluorescent molecule design with a data-physics dual-driven generative frameworkcited by 0
- 2026Multi-objective fluorescent molecule design with a data-physics dual-driven generative framework20 Jan 2026
- 2025Diverse Mini-Batch Selection in Reinforcement Learning for Efficient Chemical Exploration in de novo Drug Design26 Jun 2025
- 2025Test-Time Training Scaling Laws for Chemical Exploration in Drug Design31 Jan 2025
- 2025REINFORCE-ING Chemical Language Models for Drug Discovery27 Jan 2025
- 2024GraphXForm: Graph transformer for computer-aided molecular design3 Nov 2024
- 2024Diversity-Aware Reinforcement Learning for de novo Drug Design14 Oct 2024
- 2023Augmented Memory: Capitalizing on Experience Replay to Accelerate De Novo Molecular Design10 May 2023
- 2023Utilizing Reinforcement Learning for de novo Drug Design30 Mar 2023