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Drug Discovery: Overview

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Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...

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Updated: Jun 19, 2026

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions

Published on: December 1, 2020

Review article: high-throughput affinity-based technologies for small-molecule drug discovery.

Zhengrong Zhu¹, John Cuozzo

¹GlaxoSmithKline, Waltham, Massachusetts 02451, USA. zhengrong.x.zhu@gsk.com

Journal of Biomolecular Screening

|October 14, 2009

Summary

High-throughput affinity-based technologies are revolutionizing drug discovery screening. These methods, focusing on protein changes or bound compounds, offer varying throughput and mechanistic insights for small molecule development.

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Area of Science:

Biochemistry
Pharmacology
Nanotechnology

Background:

High-throughput screening (HTS) is crucial in modern drug discovery.
Affinity-based technologies are increasingly adopted as primary screening tools.
Evaluating the impact of these technologies on small-molecule drug discovery is essential.

Purpose of the Study:

To review the principles and applications of high-throughput affinity-based technologies.
To evaluate their impact on small-molecule drug discovery.
To discuss the appropriate use and future trends, including nanotechnology.

Main Methods:

Categorization of technologies based on detection principle: protein-centric vs. compound-centric.
Analysis of throughput and information yielded by each category.
Discussion of practical applications and future technological integration.

Main Results:

Technologies are divided into two main groups: those monitoring protein targets and those detecting bound compounds.
Protein-centric methods offer mechanistic insights but have limited throughput.
Compound-centric methods provide very high throughput but limited binding interaction details.

Conclusions:

Affinity-based technologies offer diverse capabilities for drug discovery screening.
Choosing the appropriate technology depends on the balance between throughput and mechanistic information required.
Nanotechnology is poised to significantly influence the future development of these screening platforms.