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The discovery of novel inhibitor molecules for emerging drug-target proteins is widely acknowledged as a challenging inverse design problem: Exhaustive exploration of the vast chemical search space is impractical, especially when the target…

Drug discovery is vitally important for protecting human against disease. Target-based screening is one of the most popular methods to develop new drugs in the past several decades. This method efficiently screens candidate drugs inhibiting…

Quantitative Methods · Quantitative Biology 2022-11-22 Fan Hu , Dongqi Wang , Huazhen Huang , Yishen Hu , Peng Yin

We examine a pair of graph generative models for the therapeutic design of novel drug candidates targeting SARS-CoV-2 viral proteins. Due to a sense of urgency, we chose well-validated models with unique strengths: an autoencoder that…

Biomolecules · Quantitative Biology 2021-05-24 Jenna Bilbrey , Logan Ward , Sutanay Choudhury , Neeraj Kumar , Ganesh Sivaraman

In the past several months, COVID-19 has spread over the globe and caused severe damage to the people and the society. In the context of this severe situation, an effective drug discovery method to generate potential drugs is extremely…

Machine Learning · Computer Science 2021-04-26 Tianyue Cheng , Tianchi Fan , Landi Wang

The outbreak of COVID-19 caused millions of deaths worldwide, and the number of total infections is still rising. It is necessary to identify some potentially effective drugs that can be used to prevent the development of severe symptoms or…

Molecular Networks · Quantitative Biology 2022-09-07 Fan Hu , Jiaxin Jiang , Peng Yin

Design of new drug compounds with target properties is a key area of research in generative modeling. We present a small drug molecule design pipeline based on graph-generative models and a comparison study of two state-of-the-art graph…

Machine Learning · Computer Science 2021-02-10 Logan Ward , Jenna A. Bilbrey , Sutanay Choudhury , Neeraj Kumar , Ganesh Sivaraman

With the fast development of COVID-19 into a global pandemic, scientists around the globe are desperately searching for effective antiviral therapeutic agents. Bridging systems biology and drug discovery, we propose a deep learning…

Quantitative Methods · Quantitative Biology 2020-11-24 Jannis Born , Matteo Manica , Joris Cadow , Greta Markert , Nil Adell Mill , Modestas Filipavicius , María Rodríguez Martínez

Structure-based Deep Fusion models were recently shown to outperform several physics- and machine learning-based protein-ligand binding affinity prediction methods. As part of a multi-institutional COVID-19 pandemic response, over 500…

Recent advances in generative models, particularly diffusion and auto-regressive models, have revolutionized fields like computer vision and natural language processing. However, their application to structure-based drug design (SBDD)…

Machine Learning · Computer Science 2025-07-29 Yi He , Ailun Wang , Zhi Wang , Yu Liu , Xingyuan Xu , Wen Yan

Computational drug design based on artificial intelligence is an emerging research area. At the time of writing this paper, the world suffers from an outbreak of the coronavirus SARS-CoV-2. A promising way to stop the virus replication is…

Neural and Evolutionary Computing · Computer Science 2020-09-11 Tim Cofala , Lars Elend , Philip Mirbach , Jonas Prellberg , Thomas Teusch , Oliver Kramer

With the goal of designing novel inhibitors for SARS-CoV-1 and SARS-CoV-2, we propose the general molecule optimization framework, Molecular Neural Assay Search (MONAS), consisting of three components: a property predictor which identifies…

Machine Learning · Computer Science 2021-02-01 Timothy Atkinson , Saeed Saremi , Faustino Gomez , Jonathan Masci

We report a fast-track computationally-driven discovery of new SARS-CoV2 Main Protease (M$^{pro}$) inhibitors whose potency range from mM for initial non-covalent ligands to sub-$\mu$M for the final covalent compound (IC50=830 +/- 50 nM).…

The ultimate goal of various fields is to directly generate molecules with desired properties, such as finding water-soluble molecules in drug development and finding molecules suitable for organic light-emitting diode (OLED) or…

Machine Learning · Computer Science 2022-02-16 Myeonghun Lee , Kyoungmin Min

Recently, deep generative models have revealed itself as a promising way of performing de novo molecule design. However, previous research has focused mainly on generating SMILES strings instead of molecular graphs. Although current graph…

Quantitative Methods · Quantitative Biology 2018-04-24 Yibo Li , Liangren Zhang , Zhenming Liu

Simultaneously optimizing molecules against multiple therapeutic targets remains a profound challenge in drug discovery, particularly due to sparse rewards and conflicting design constraints. We propose a structured active learning (AL)…

Machine Learning · Computer Science 2025-06-24 Júlia Vilalta-Mor , Alexis Molina , Laura Ortega Varga , Isaac Filella-Merce , Victor Guallar

Drug repurposing can accelerate the identification of effective compounds for clinical use against SARS-CoV-2, with the advantage of pre-existing clinical safety data and an established supply chain. RNA viruses such as SARS-CoV-2…

A molecular and cellular understanding of how SARS-CoV-2 variably infects and causes severe COVID-19 remains a bottleneck in developing interventions to end the pandemic. We sought to use deep learning to study the biology of SARS-CoV-2…

Machine Learning · Computer Science 2020-12-16 Arijit Sehanobish , Neal G. Ravindra , David van Dijk

The novel nature of SARS-CoV-2 calls for the development of efficient de novo drug design approaches. In this study, we propose an end-to-end framework, named CogMol (Controlled Generation of Molecules), for designing new drug-like small…

Designing molecules with desirable physiochemical properties and functionalities is a long-standing challenge in chemistry, material science, and drug discovery. Recently, machine learning-based generative models have emerged as promising…

Biomolecules · Quantitative Biology 2023-04-26 Zaixi Zhang , Qi Liu , Chee-Kong Lee , Chang-Yu Hsieh , Enhong Chen

The world has witnessed unprecedented human and economic loss from the COVID-19 disease, caused by the novel coronavirus SARS-CoV-2. Extensive research is being conducted across the globe to identify therapeutic agents against the…

Biomolecules · Quantitative Biology 2020-04-09 Rohit Batra , Henry Chan , Ganesh Kamath , Rampi Ramprasad , Mathew J. Cherukara , Subramanian Sankaranarayanan
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