Significats de lead optimization en anglès

The pyrimidineamine series provides a novel starting point for an anti-HAT lead optimization.

Herein, we report JzTx-V lead optimization to identify a pharmacodynamically active peptide variant.

Mapping of amyloid peptides as a new approach for drug lead optimization will be presented.

A few derivatives with overall favorable developability characteristics were selected for further late lead optimization studies.

Significant progress has been made in HTS, lead optimization and determination of 3D structures of DNMTs.

This report highlights a systematic antibody engineering strategy for mitigating an Asp isomerization developability risk during lead optimization.

Structure-activity relationships (SAR) of compound databases play a key role in hit identification and lead optimization.

Hit-to- lead optimization led to a number of highly potent inhibitors, while maintaining the high ligand efficiency of the screening hit.

It is uniquely useful in analysis of small, focused selectivity panel data frequently encountered in medicinal chemistry hit-to- lead and lead optimization.

In this study, we performed a lead optimization of a small molecule Doxazosin that was identified as an EphA2 receptor agonist.

The present biochemical advancements will allow high throughput chemical screening of compound libraries and lead optimization to develop new lines of antimalarials.

The discovery of several new TbAdoMetDC inhibitor chemotypes provides new hits for lead optimization programs aimed to deliver a novel treatment for HAT.

It represents a new class of activity-dependent TRPV1 antagonists and may serve as the basis for lead optimization in the development of new analgesics.

The utility of screening for in vitro liver microsomal stability as part of the lead optimization process for compounds with metabolic liabilities was shown.

Our results also detail a novel dual-binding mechanism for this compound as well as substantial structure-activity relationships (SAR) that may help in lead optimization activities.

Hit-to- lead optimization to determine the structure-activity relationship (SAR) identified the more potent EboV inhibitor 2 and a photoaffinity labeling agent 3.