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Updated: Jun 22, 2026

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

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

Published on: May 16, 2021

Recent progress in fragment-based lead discovery.

Michèle N Schulz¹, Roderick E Hubbard

¹YSBL, University of York, York YO10 5YW, United Kingdom.

Current Opinion in Pharmacology

|May 30, 2009

Summary

This summary is machine-generated.

Fragment-based lead discovery (FBLD) offers a powerful strategy for identifying drug leads from small compound libraries. This approach is effective for targets where traditional high-throughput screening (HTS) fails, with ongoing advancements integrating FBLD with HTS.

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Last Updated: Jun 22, 2026

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

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Published on: May 16, 2021

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Workflow and Tools for Crystallographic Fragment Screening at the Helmholtz-Zentrum Berlin

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Published on: March 3, 2021

Area of Science:

Drug discovery and medicinal chemistry
Biochemistry and structural biology
Computational chemistry

Background:

Fragment-based lead discovery (FBLD) is an emerging strategy in drug development.
It utilizes small molecule fragments to identify starting points for drug candidates.
FBLD is particularly advantageous for targets intractable by conventional high-throughput screening (HTS).

Purpose of the Study:

To summarize the key elements of fragment-based lead discovery (FBLD).
To review recent advancements and progress in the field.
To provide a perspective on the remaining challenges in FBLD.

Main Methods:

Utilizing small libraries of low molecular weight compounds (typically ~1000 members).
Employing sensitive biophysical or structural methods to detect weak fragment binding.
Developing strategies for fragment evolution into larger, potent lead compounds.

Main Results:

FBLD has been validated, with multiple fragment-derived compounds entering clinical trials.
The approach is being applied to challenging targets where HTS is less effective.
Integration of FBLD with HTS is enhancing drug discovery for more targets.

Conclusions:

FBLD is a validated and increasingly important drug discovery strategy.
Key challenges include sensitive detection of weak binding and effective fragment evolution.
Future directions involve applying FBLD to difficult targets and integrating it with HTS.