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Related Concept Videos

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...
Patch Clamp01:18

Patch Clamp

Many fundamental cell functions such as muscle contraction and nerve transmission rely on the electrical signals produced by the movement of positively and negatively charged ions across the cell membrane. One competent method to record current flowing across the whole cell or single ion channel is the patch-clamp technique.
In this method, a glass micropipette containing electrolyte solution is tightly sealed against a small portion of the cell membrane. As a result, a patch of the cell...
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...
Pharmacogenomics: Identification of New Drug Targets01:29

Pharmacogenomics: Identification of New Drug Targets

Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...

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Updated: May 23, 2026

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
06:26

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Published on: May 16, 2021

Experiences in fragment-based drug discovery.

Christopher W Murray1, Marcel L Verdonk, David C Rees

  • 1Astex Pharmaceuticals, 436 Cambridge Science Park, Milton Road, Cambridge, CB4 0QA, UK. chris.murray@astx.com

Trends in Pharmacological Sciences
|March 31, 2012
PubMed
Summary

Fragment-based drug discovery (FBDD) offers a viable alternative to high-throughput screening for identifying drug leads. This approach yields high-quality compounds with favorable properties, promising future drug development.

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Last Updated: May 23, 2026

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Area of Science:

  • Medicinal Chemistry
  • Structural Biology
  • Drug Discovery

Background:

  • Fragment-based drug discovery (FBDD) is an established method in pharmaceutical research.
  • It serves as an alternative to high-throughput screening for generating chemical leads.
  • FBDD utilizes specialized detection methods to identify small molecules binding to drug targets.

Purpose of the Study:

  • To present recent successful case histories in FBDD.
  • To re-examine key concepts and challenges in FBDD.
  • To evaluate the effectiveness of FBDD in generating drug leads.

Main Methods:

  • Identification of small chemical compounds (fragments) that bind to drug targets.
  • Utilizing specialized detection methods for fragment screening.
  • Employing structural biology to determine fragment binding modes and guide optimization.

Main Results:

  • Presented three recent and successful case histories in FBDD.
  • Re-examined FBDD concepts and challenges based on literature and practical experience.
  • Demonstrated that FBDD delivers high-quality leads with good physical properties.

Conclusions:

  • Fragment-based drug discovery (FBDD) is a promising approach for developing new medicines.
  • Careful application of FBDD fulfills its potential in generating effective drug leads.
  • Future drug molecules are likely to be derived from fragment-based strategies.