Deep learning for molecular design - a review of the state of the art
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Abstract (arXiv)
In the space of only a few years, deep generative modeling has revolutionized how we think of artificial creativity, yielding autonomous systems which produce original images, music, and text. Inspired by these successes, researchers are now applying deep generative modeling techniques to the generation and optimization of molecules - in our review we found 45 papers on the subject published in the past two years. These works point to a future where such systems will be used to generate lead molecules, greatly reducing resources spent downstream synthesizing and characterizing bad leads in the lab. In this review we survey the increasingly complex landscape of models and representation schemes that have been proposed. The four classes of techniques we describe are recursive neural networks, autoencoders, generative adversarial networks, and reinforcement learning. After first discussing some of the mathematical fundamentals of each technique, we draw high level connections and comparisons with other techniques and expose the pros and cons of each. Several important high level themes emerge as a result of this work, including the shift away from the SMILES string representation of molecules towards more sophisticated representations such as graph grammars and 3D representations, the importance of reward function design, the need for better standards for benchmarking and testing, and the benefits of adversarial training and reinforcement learning over maximum likelihood based training.
Key facts. Cited by 38 papers in the map (data through 7 Oct 2026). First posted on arXiv 11 Mar 2019.
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Citing papers per year: 2021: 10; 2022: 16; 2023: 7; 2024: 1; 2025: 2; 2026: 2.
38 papers.
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- 2021Inverse design of 3d molecular structures with conditional generative neural networkscited by 93
- 2022MolGenSurvey: A Systematic Survey in Machine Learning Models for Molecule Designcited by 66
- 2022Regression Transformer: Concurrent sequence regression and generation for molecular language modelingcited by 49
- 2021Amortized Tree Generation for Bottom-up Synthesis Planning and Synthesizable Molecular Designcited by 44
- 2023A Survey on Graph Diffusion Models: Generative AI in Science for Molecule, Protein and Materialcited by 34
- 2021Learning 3D Representations of Molecular Chirality with Invariance to Bond Rotationscited by 29
- 2021Artificial Intelligence in Drug Discovery: Applications and Techniquescited by 28
- 2022Graph Neural Networks for Moleculescited by 21
- 2022Controllable Data Generation by Deep Learning: A Reviewcited by 20
- 2022Molecule Generation for Drug Design: a Graph Learning Perspectivecited by 13
- 2022Graph neural networks for the prediction of molecular structure-property relationshipscited by 12
- 2023PubChemQC B3LYP/6-31G*//PM6 dataset: the Electronic Structures of 86 Million Molecules using B3LYP/6-31G* calculationscited by 12
26 more
- 2021AugLiChem: Data Augmentation Library of Chemical Structures for Machine Learningcited by 10
- 2023Deep Learning Methods for Small Molecule Drug Discovery: A Surveycited by 10
- 2022Self-focusing virtual screening with active design space pruningcited by 8
- 2021IMG2SMI: Translating Molecular Structure Images to Simplified Molecular-input Line-entry Systemcited by 6
- 2022Graph Machine Learning for Design of High-Octane Fuelscited by 6
- 2022Faster and more diverse de novo molecular optimization with double-loop reinforcement learning using augmented SMILEScited by 5
- 2025Molecular Machine Learning in Chemical Process Designcited by 5
- 2023Automated patent extraction powers generative modeling in focused chemical spacescited by 4
- 2022An Unpooling Layer for Graph Generationcited by 3
- 2022De novo PROTAC design using graph-based deep generative modelscited by 3
- 2021Artificial Intelligence based Autonomous Molecular Design for Medical Therapeutic: A Perspectivecited by 2
- 2022PGMG: A Pharmacophore-Guided Deep Learning Approach for Bioactive Molecular Generationcited by 2
- 2023Modeling and design of heterogeneous hierarchical bioinspired spider web structures using generative deep learning and additive manufacturingcited by 2
- 2021Evaluating the progress of Deep Reinforcement Learning in the real world: aligning domain-agnostic and domain-specific researchcited by 1
- 2021An In-depth Summary of Recent Artificial Intelligence Applications in Drug Designcited by 1
- 2022Molecular Dipole Moment Learning via Rotationally Equivariant Gaussian Process Regression with Derivatives in Molecular-orbital-based Machine Learningcited by 1
- 2022Molecular-orbital-based Machine Learning for Open-shell and Multi-reference Systems with Kernel Addition Gaussian Process Regressioncited by 1
- 2023ChemVise: Maximizing Out-of-Distribution Chemical Detection with the Novel Application of Zero-Shot Learningcited by 1
- 2021ES-ENAS: Efficient Evolutionary Optimization for Large Hybrid Search Spacescited by 0
- 2022Transferring Chemical and Energetic Knowledge Between Molecular Systems with Machine Learningcited by 0
- 2022Topology-Driven Generative Completion of Lacunae in Molecular Datacited by 0
- 2023Neural Embeddings for Protein Graphscited by 0
- 2024Virtual Reality for Understanding Artificial-Intelligence-driven Scientific Discovery with an Application in Quantum Opticscited by 0
- 2025Learning Continuous Solvent Effects from Transient Flow Data: A Graph Neural Network Benchmark on Catechol Rearrangementcited by 0
- 2026Reasoning-Driven Design of Single Atom Catalysts via a Multi-Agent Large Language Model Frameworkcited by 0
- 2026A Systematic Evaluation of Molecule Generation Models for De Novo Drug Design: From Benchmarks to Practical Insightscited by 0
- 2026A Systematic Evaluation of Molecule Generation Models for De Novo Drug Design: From Benchmarks to Practical Insights9 Sep 2026
- 2026Reasoning-Driven Design of Single Atom Catalysts via a Multi-Agent Large Language Model Framework25 Feb 2026
- 2025Learning Continuous Solvent Effects from Transient Flow Data: A Graph Neural Network Benchmark on Catechol Rearrangement22 Dec 2025
- 2025Molecular Machine Learning in Chemical Process Design28 Aug 2025
- 2024Virtual Reality for Understanding Artificial-Intelligence-driven Scientific Discovery with an Application in Quantum Optics20 Feb 2024
- 2023Neural Embeddings for Protein Graphs7 Jun 2023
- 2023PubChemQC B3LYP/6-31G*//PM6 dataset: the Electronic Structures of 86 Million Molecules using B3LYP/6-31G* calculations29 May 2023
- 2023Modeling and design of heterogeneous hierarchical bioinspired spider web structures using generative deep learning and additive manufacturing11 Apr 2023
- 2023A Survey on Graph Diffusion Models: Generative AI in Science for Molecule, Protein and Material4 Apr 2023
- 2023Automated patent extraction powers generative modeling in focused chemical spaces14 Mar 2023
- 2023Deep Learning Methods for Small Molecule Drug Discovery: A Survey1 Mar 2023
- 2023ChemVise: Maximizing Out-of-Distribution Chemical Detection with the Novel Application of Zero-Shot Learning9 Feb 2023
26 more
- 2022De novo PROTAC design using graph-based deep generative models4 Nov 2022
- 2022Faster and more diverse de novo molecular optimization with double-loop reinforcement learning using augmented SMILES22 Oct 2022
- 2022Graph Neural Networks for Molecules12 Sep 2022
- 2022Topology-Driven Generative Completion of Lacunae in Molecular Data29 Jul 2022
- 2022Graph neural networks for the prediction of molecular structure-property relationships25 Jul 2022
- 2022Controllable Data Generation by Deep Learning: A Review19 Jul 2022
- 2022Molecular-orbital-based Machine Learning for Open-shell and Multi-reference Systems with Kernel Addition Gaussian Process Regression17 Jul 2022
- 2022PGMG: A Pharmacophore-Guided Deep Learning Approach for Bioactive Molecular Generation2 Jul 2022
- 2022An Unpooling Layer for Graph Generation4 Jun 2022
- 2022Graph Machine Learning for Design of High-Octane Fuels1 Jun 2022
- 2022Molecular Dipole Moment Learning via Rotationally Equivariant Gaussian Process Regression with Derivatives in Molecular-orbital-based Machine Learning31 May 2022
- 2022Transferring Chemical and Energetic Knowledge Between Molecular Systems with Machine Learning6 May 2022
- 2022Self-focusing virtual screening with active design space pruning3 May 2022
- 2022MolGenSurvey: A Systematic Survey in Machine Learning Models for Molecule Design28 Mar 2022
- 2022Molecule Generation for Drug Design: a Graph Learning Perspective18 Feb 2022
- 2022Regression Transformer: Concurrent sequence regression and generation for molecular language modeling1 Feb 2022
- 2021AugLiChem: Data Augmentation Library of Chemical Structures for Machine Learning30 Nov 2021
- 2021Amortized Tree Generation for Bottom-up Synthesis Planning and Synthesizable Molecular Design12 Oct 2021
- 2021An In-depth Summary of Recent Artificial Intelligence Applications in Drug Design10 Oct 2021
- 2021Learning 3D Representations of Molecular Chirality with Invariance to Bond Rotations8 Oct 2021
- 2021Inverse design of 3d molecular structures with conditional generative neural networks10 Sep 2021
- 2021IMG2SMI: Translating Molecular Structure Images to Simplified Molecular-input Line-entry System3 Sep 2021
- 2021Evaluating the progress of Deep Reinforcement Learning in the real world: aligning domain-agnostic and domain-specific research7 Jul 2021
- 2021Artificial Intelligence in Drug Discovery: Applications and Techniques9 Jun 2021
- 2021Artificial Intelligence based Autonomous Molecular Design for Medical Therapeutic: A Perspective10 Feb 2021
- 2021ES-ENAS: Efficient Evolutionary Optimization for Large Hybrid Search Spaces19 Jan 2021
- 2021Inverse design of 3d molecular structures with conditional generative neural networkscited by 93
- 2022MolGenSurvey: A Systematic Survey in Machine Learning Models for Molecule Designcited by 66
- 2022Regression Transformer: Concurrent sequence regression and generation for molecular language modelingcited by 49
- 2021Amortized Tree Generation for Bottom-up Synthesis Planning and Synthesizable Molecular Designcited by 44
- 2021Learning 3D Representations of Molecular Chirality with Invariance to Bond Rotationscited by 29
- 2021Artificial Intelligence in Drug Discovery: Applications and Techniquescited by 28
- 2022Graph Neural Networks for Moleculescited by 21
- 2022Controllable Data Generation by Deep Learning: A Reviewcited by 20
- 2022Molecule Generation for Drug Design: a Graph Learning Perspectivecited by 13
- 2022Graph neural networks for the prediction of molecular structure-property relationshipscited by 12
- 2023PubChemQC B3LYP/6-31G*//PM6 dataset: the Electronic Structures of 86 Million Molecules using B3LYP/6-31G* calculationscited by 12
- 2021AugLiChem: Data Augmentation Library of Chemical Structures for Machine Learningcited by 10
12 most cited of 35 All 35 (JSON)
- 2026A Systematic Evaluation of Molecule Generation Models for De Novo Drug Design: From Benchmarks to Practical Insights9 Sep 2026
- 2025Learning Continuous Solvent Effects from Transient Flow Data: A Graph Neural Network Benchmark on Catechol Rearrangement22 Dec 2025
- 2025Molecular Machine Learning in Chemical Process Design28 Aug 2025
- 2024Virtual Reality for Understanding Artificial-Intelligence-driven Scientific Discovery with an Application in Quantum Optics20 Feb 2024
- 2023Neural Embeddings for Protein Graphs7 Jun 2023
- 2023PubChemQC B3LYP/6-31G*//PM6 dataset: the Electronic Structures of 86 Million Molecules using B3LYP/6-31G* calculations29 May 2023
- 2023Automated patent extraction powers generative modeling in focused chemical spaces14 Mar 2023
- 2023Deep Learning Methods for Small Molecule Drug Discovery: A Survey1 Mar 2023
- 2023ChemVise: Maximizing Out-of-Distribution Chemical Detection with the Novel Application of Zero-Shot Learning9 Feb 2023
- 2022De novo PROTAC design using graph-based deep generative models4 Nov 2022
- 2022Faster and more diverse de novo molecular optimization with double-loop reinforcement learning using augmented SMILES22 Oct 2022
- 2022Graph Neural Networks for Molecules12 Sep 2022
12 newest of 35 All 35 (JSON)