AIMC Topic: Drug Design

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Pharmacophore features for machine learning in pharmaceutical virtual screening.

Molecular diversity
Methods of three-dimensional molecular alignment generally treat all pharmacophore features equally when superimposing. However, some pharmacophore features can be more important in a specific system. In this work, we derived the overlap volume of ph...

Design of Natural-Product-Inspired Multitarget Ligands by Machine Learning.

ChemMedChem
A virtual screening protocol based on machine learning models was used to identify mimetics of the natural product (-)-galantamine. This fully automated approach identified eight compounds with bioactivities on at least one of the macromolecular targ...

The significance of artificial intelligence in drug delivery system design.

Advanced drug delivery reviews
Over the last decade, increasing interest has been attracted towards the application of artificial intelligence (AI) technology for analyzing and interpreting the biological or genetic information, accelerated drug discovery, and identification of th...

Exploiting machine learning for end-to-end drug discovery and development.

Nature materials
A variety of machine learning methods such as naive Bayesian, support vector machines and more recently deep neural networks are demonstrating their utility for drug discovery and development. These leverage the generally bigger datasets created from...

Applications of machine learning in GPCR bioactive ligand discovery.

Current opinion in structural biology
GPCRs constitute the largest druggable family having targets for 475 Food and Drug Administration (FDA) approved drugs. As GPCRs are of great interest to pharmaceutical industry, enormous efforts are being expended to find relevant and potent GPCR li...

Autonomous Molecular Design: Then and Now.

ACS applied materials & interfaces
The success of deep machine learning in processing of large amounts of data, for example, in image or voice recognition and generation, raises the possibilities that these tools can also be applied for solving complex problems in materials science. I...

Automated discovery of GPCR bioactive ligands.

Current opinion in structural biology
While G-protein-coupled receptors (GPCRs) constitute the largest class of membrane proteins, structures and endogenous ligands of a large portion of GPCRs remain unknown. Because of the involvement of GPCRs in various signaling pathways and physiolog...

Elucidating the druggability of the human proteome with eFindSite.

Journal of computer-aided molecular design
Identifying the viability of protein targets is one of the preliminary steps of drug discovery. Determining the ability of a protein to bind drugs in order to modulate its function, termed the druggability, requires a non-trivial amount of time and r...

GuacaMol: Benchmarking Models for de Novo Molecular Design.

Journal of chemical information and modeling
De novo design seeks to generate molecules with required property profiles by virtual design-make-test cycles. With the emergence of deep learning and neural generative models in many application areas, models for molecular design based on neural net...