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Ligands

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Machine Learning to Identify Flexibility Signatures of Class A GPCR Inhibition.

Biomolecules
We show that machine learning can pinpoint features distinguishing inactive from active states in proteins, in particular identifying key ligand binding site flexibility transitions in GPCRs that are triggered by biologically active ligands. Our anal...

Machine learning models for drug-target interactions: current knowledge and future directions.

Drug discovery today
Predicting the binding affinity between compounds and proteins with reasonable accuracy is crucial in drug discovery. Computational prediction of binding affinity between compounds and targets greatly enhances the probability of finding lead compound...

Combining Docking Pose Rank and Structure with Deep Learning Improves Protein-Ligand Binding Mode Prediction over a Baseline Docking Approach.

Journal of chemical information and modeling
We present a simple, modular graph-based convolutional neural network that takes structural information from protein-ligand complexes as input to generate models for activity and binding mode prediction. Complex structures are generated by a standard...

Tapping on the Black Box: How Is the Scoring Power of a Machine-Learning Scoring Function Dependent on the Training Set?

Journal of chemical information and modeling
In recent years, protein-ligand interaction scoring functions derived through machine-learning are repeatedly reported to outperform conventional scoring functions. However, several published studies have questioned that the superior performance of m...

A novel artificial intelligence protocol for finding potential inhibitors of acute myeloid leukemia.

Journal of materials chemistry. B
There is currently no effective treatment for acute myeloid leukemia, and surgery is also ineffective as an important treatment for most tumors. Rapidly developing artificial intelligence technology can be applied to different aspects of drug develop...

Machine learning and ligand binding predictions: A review of data, methods, and obstacles.

Biochimica et biophysica acta. General subjects
Computational predictions of ligand binding is a difficult problem, with more accurate methods being extremely computationally expensive. The use of machine learning for drug binding predictions could possibly leverage the use of biomedical big data ...

Characterizing Protein-Ligand Binding Using Atomistic Simulation and Machine Learning: Application to Drug Resistance in HIV-1 Protease.

Journal of chemical theory and computation
Over the past several decades, atomistic simulations of biomolecules, whether carried out using molecular dynamics or Monte Carlo techniques, have provided detailed insights into their function. Comparing the results of such simulations for a few clo...

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...

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...