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Drug Design

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Improving the binding affinity estimations of protein-ligand complexes using machine-learning facilitated force field method.

Journal of computer-aided molecular design
Scoring functions are routinely deployed in structure-based drug design to quantify the potential for protein-ligand (PL) complex formation. Here, we present a new scoring function Bappl+ that is designed to predict the binding affinities of non-meta...

Exploring chemical space using natural language processing methodologies for drug discovery.

Drug discovery today
Text-based representations of chemicals and proteins can be thought of as unstructured languages codified by humans to describe domain-specific knowledge. Advances in natural language processing (NLP) methodologies in the processing of spoken languag...

Design of (quinolin-4-ylthio)carboxylic acids as new Escherichia coli DNA gyrase B inhibitors: machine learning studies, molecular docking, synthesis and biological testing.

Computational biology and chemistry
Spread of multidrug-resistant Escherichia coli clinical isolates is a main problem in the treatment of infectious diseases. Therefore, the modern scientific approaches in decision this problem require not only a prevention strategy, but also the deve...

Deep neural network affinity model for BACE inhibitors in D3R Grand Challenge 4.

Journal of computer-aided molecular design
Drug Design Data Resource (D3R) Grand Challenge 4 (GC4) offered a unique opportunity for designing and testing novel methodology for accurate docking and affinity prediction of ligands in an open and blinded manner. We participated in the beta-secret...

De novo generation of hit-like molecules from gene expression signatures using artificial intelligence.

Nature communications
Finding new molecules with a desired biological activity is an extremely difficult task. In this context, artificial intelligence and generative models have been used for molecular de novo design and compound optimization. Herein, we report a generat...

Latest trends in structure based drug design with protein targets.

Advances in protein chemistry and structural biology
Structure based drug designing is an important endeavor in the field of structural bioinformatics. Previously the entire process was dependent on the wet-lab experiments to build libraries of ligand molecules. And the molecules used to be tested to d...

Rethinking drug design in the artificial intelligence era.

Nature reviews. Drug discovery
Artificial intelligence (AI) tools are increasingly being applied in drug discovery. While some protagonists point to vast opportunities potentially offered by such tools, others remain sceptical, waiting for a clear impact to be shown in drug discov...

Convolutional Neural Networks for the Design and Analysis of Non-Fullerene Acceptors.

Journal of chemical information and modeling
Convolutional neural network (CNN) is employed to construct generative and prediction models for the design and analysis of non-fullerene acceptors (NFAs) in organic solar cells. It is demonstrated that the dilated causal CNN can be trained as a good...

MathDL: mathematical deep learning for D3R Grand Challenge 4.

Journal of computer-aided molecular design
We present the performances of our mathematical deep learning (MathDL) models for D3R Grand Challenge 4 (GC4). This challenge involves pose prediction, affinity ranking, and free energy estimation for beta secretase 1 (BACE) as well as affinity ranki...

Identification of Synthetic Activators of Cancer Cell Migration by Hybrid Deep Learning.

Chembiochem : a European journal of chemical biology
Deep convolutional neural networks (CNNs) are a method of choice for image recognition. Herein a hybrid CNN approach is presented for molecular pattern recognition in drug discovery. Using self-organizing map images of molecular pharmacophores as inp...