AIMC Topic: Drug Evaluation, Preclinical

Clear Filters Showing 21 to 30 of 213 articles

In Silico Screening of Small Molecule Inhibitors for Amyloid-β Aggregation.

Journal of chemical information and modeling
The self-aggregation of amyloid-β (Aβ) into fibrils is a hallmark of Alzheimer's disease (AD). Inhibition of Aβ aggregation with small molecule compounds represents a promising therapeutic strategy for AD. However, designing effective ligands is chal...

On the Difficulty to Rescore Hits from Ultralarge Docking Screens.

Journal of chemical information and modeling
Docking-based virtual screening tools customized to mine ultralarge chemical spaces are consistently reported to yield both higher hit rates and more potent ligands than that achieved by conventional docking of smaller million-sized compound librarie...

Artificial intelligence in preclinical research: enhancing digital twins and organ-on-chip to reduce animal testing.

Drug discovery today
Artificial intelligence (AI) is reshaping preclinical drug research offering innovative alternatives to traditional animal testing. Advanced techniques, including machine learning (ML), deep learning (DL), AI-powered digital twins (DTs), and AI-enhan...

Discovery and Characterization of Novel Receptor-Interacting Protein Kinase 1 Inhibitors Using Deep Learning and Virtual Screening.

ACS chemical neuroscience
Receptor-interacting protein kinase 1 (RIPK1) serves as a critical mediator of cell necroptosis and represents a promising therapeutic target for various human neurodegenerative diseases and inflammatory diseases. Nonetheless, the RIPK1 inhibitors cu...

Unveiling CNS cell morphology with deep learning: A gateway to anti-inflammatory compound screening.

PloS one
Deciphering the complex relationships between cellular morphology and phenotypic manifestations is crucial for understanding cell behavior, particularly in the context of neuropathological states. Despite its importance, the application of advanced i...

Fine-Tuned Deep Transfer Learning Models for Large Screenings of Safer Drugs Targeting Class A GPCRs.

Biochemistry
G protein-coupled receptors (GPCRs) remain a focal point of research due to their critical roles in cell signaling and their prominence as drug targets. However, directly linking drug efficacy to the receptor-mediated activation of specific intracell...

CPHNet: a novel pipeline for anti-HAPE drug screening via deep learning-based Cell Painting scoring.

Respiratory research
BACKGROUND: High altitude pulmonary edema (HAPE) poses a significant medical challenge to individuals ascending rapidly to high altitudes. Hypoxia-induced cellular morphological changes in the alveolar-capillary barrier such as mitochondrial structur...

Machine learning enables high-throughput, low-replicate screening for novel anti-seizure targets and compounds using combined movement and calcium fluorescence in larval zebrafish.

European journal of pharmacology
Identifying new anti-seizure medications (ASMs) is difficult due to limitations in animal-based assays. Zebrafish (Danio rerio) serve as a model for chemical and genetic seizures, but current methods for detecting anti-seizure responses are limited b...