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Related Experiment Video

Updated: Jul 6, 2026

High-throughput Screening for Chemical Modulators of Post-transcriptionally Regulated Genes

High-throughput Screening for Chemical Modulators of Post-transcriptionally Regulated Genes

Published on: March 3, 2015

Hit and lead generation: beyond high-throughput screening.

Konrad H Bleicher¹, Hans-Joachim Böhm, Klaus Müller

¹F. Hoffmann-La Roche Ltd, Grenzacherstrasse 124, CH-4070, Basel, Switzerland.

Nature Reviews. Drug Discovery

|May 17, 2003

Summary

Identifying small-molecule modulators and developing lead series are crucial in drug discovery. New integrated strategies are needed to improve success rates and reduce costs in clinical development.

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Area of Science:

Drug discovery and development
Medicinal chemistry
Chemical biology

Background:

Small-molecule modulators of protein function are vital in drug discovery.
Early-stage decisions significantly impact lead optimization and clinical success.
High clinical failure rates increase downstream costs, necessitating process improvements.

Purpose of the Study:

To highlight the importance of efficient small-molecule modulator identification and lead series development.
To advocate for integrated, parallel processes over traditional linear approaches.
To address the need for flexible, fast, and cost-effective strategies in drug discovery.

Main Methods:

Review of current practices in small-molecule drug discovery.
Analysis of the impact of early-stage decisions on downstream development.
Exploration of emerging opportunities in functional genomics and proteomics.

Main Results:

Current linear processes are insufficient to meet the demands of modern drug discovery.
Integrated and parallel strategies offer a more efficient approach.
Flexible, fast, and cost-effective methods are essential for producing high-content lead series.

Conclusions:

Rethinking the drug discovery process is critical for success.
Adopting integrated strategies can improve the prospects of clinical success.
Innovation in identification and lead development is key to reducing drug development costs.