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Drug Discovery: Overview01:26

Drug Discovery: Overview

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...
Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...

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Related Experiment Video

Updated: May 8, 2026

A Fluorescence-based Lymphocyte Assay Suitable for High-throughput Screening of Small Molecules
08:43

A Fluorescence-based Lymphocyte Assay Suitable for High-throughput Screening of Small Molecules

Published on: March 10, 2017

Strategies for small molecule library design.

David W Sheppard, Michael J Lipkin, C John Harris

  • 1Galapagos NV, Generaal De Wittelaan L11 A3, 2800 Mechelen, Belgium. pieter.stouten@glpg.com.

Current Pharmaceutical Design
|August 17, 2013
PubMed
Summary
This summary is machine-generated.

Designing focused compound libraries is key for successful small molecule screening. BioFocus

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Area of Science:

  • Drug discovery and medicinal chemistry
  • Chemical biology and screening technologies

Background:

  • Small molecule screening requires carefully curated compound sets for success.
  • Diverse compound libraries are used when target information is limited.
  • Focused libraries, biased towards known ligands or target structures, improve efficiency.

Purpose of the Study:

  • To outline principles for designing focused compound libraries (SoftFocus®).
  • To showcase client successes using BioFocus's compound libraries.
  • To demonstrate the effectiveness of SoftFocus libraries against kinase targets.

Main Methods:

  • Design and synthesis of focused compound libraries.
  • Application of ligand- and target-focused strategies.
  • Screening of BioFocus's kinase libraries against 20 kinase targets.

Main Results:

  • BioFocus has successfully produced SoftFocus® libraries for diverse targets, including kinases, GPCRs, ion channels, epigenetics, and protein-protein interactions (PPI).
  • Screening results against 20 kinase targets demonstrated the SoftFocus approach's ability to yield both selective and less-selective compounds and libraries.
  • The article highlights client successes attributed to BioFocus's library design principles.

Conclusions:

  • Focused library design is crucial for efficient drug discovery, especially for challenging targets.
  • The SoftFocus® approach effectively delivers targeted compound libraries for various therapeutic areas.
  • BioFocus's libraries have a proven track record of success in client drug discovery programs.