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Drug Design

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Deep Learning in Drug Design: Protein-Ligand Binding Affinity Prediction.

IEEE/ACM transactions on computational biology and bioinformatics
Computational drug design relies on the calculation of binding strength between two biological counterparts especially a chemical compound, i.e., a ligand, and a protein. Predicting the affinity of protein-ligand binding with reasonable accuracy is c...

AI in 3D compound design.

Current opinion in structural biology
The success of Artificial Intelligence (AI) across a wide range of domains has fuelled significant interest in its application to designing novel compounds and screening compounds against a specific target. However, many existing AI methods either do...

Interpretation of Structure-Activity Relationships in Real-World Drug Design Data Sets Using Explainable Artificial Intelligence.

Journal of chemical information and modeling
In silico models based on Deep Neural Networks (DNNs) are promising for predicting activities and properties of new molecules. Unfortunately, their inherent black-box character hinders our understanding, as to which structural features are important ...

Chemical Reactivity Prediction: Current Methods and Different Application Areas.

Molecular informatics
The ability to predict chemical reactivity of a molecule is highly desirable in drug discovery, both ex vivo (synthetic route planning, formulation, stability) and in vivo: metabolic reactions determine pharmacodynamics, pharmacokinetics and potentia...

Can Generative-Model-Based Drug Design Become a New Normal in Drug Discovery?

Journal of medicinal chemistry
It is still rare that AI application examples with full DMTA (Design, Make, Test, Analysis) outcomes are reported. A recent study highlights that a generative model could be applied in the drug discovery process through an example in which ideas gene...

Discovery of Pyrazolo[3,4-]pyridazinone Derivatives as Selective DDR1 Inhibitors via Deep Learning Based Design, Synthesis, and Biological Evaluation.

Journal of medicinal chemistry
Alterations of discoidin domain receptor1 (DDR1) may lead to increased production of inflammatory cytokines, making DDR1 an attractive target for inflammatory bowel disease (IBD) therapy. A scaffold-based molecular design workflow was established and...

Deep learning approaches for de novo drug design: An overview.

Current opinion in structural biology
De novo drug design is the process of generating novel lead compounds with desirable pharmacological and physiochemical properties. The application of deep learning (DL) in de novo drug design has become a hot topic, and many DL-based approaches have...

Drug Design: Where We Are and Future Prospects.

Molecules (Basel, Switzerland)
Medicinal chemistry is facing new challenges in approaching precision medicine. Several powerful new tools or improvements of already used tools are now available to medicinal chemists to help in the process of drug discovery, from a hit molecule to ...

Structure-Based Drug Design Using Deep Learning.

Journal of chemical information and modeling
In recent years, deep learning-based methods have emerged as promising tools for drug design. Most of these methods are ligand-based, where an initial target-specific ligand data set is necessary to design potent molecules with optimized properties....