Related Experiment Video
Updated: May 7, 2026

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
Published on: May 16, 2021
Discovery of novel drugs for promising targets
Robert E Martell1, David G Brooks, Yan Wang
1TESARO Inc, Waltham, Massachusetts; Tufts Medical Center, Boston, Massachusetts.
Background:
Once a promising drug target is identified, the steps to actually discover and optimize a drug are diverse and challenging.
Objective:
The goal of this study was to provide a road map to navigate drug discovery.
Methods:
Review general steps for drug discovery and provide illustrating references.
Results:
A number of approaches are available to enhance and accelerate target identification and validation. Consideration of a variety of potential mechanisms of action of potential drugs can guide discovery efforts. The hit to lead stage may involve techniques such as high-throughput screening, fragment-based screening, and structure-based design, with informatics playing an ever-increasing role. Biologically relevant screening models are discussed, including cell lines, 3-dimensional culture, and in vivo screening. The process of enabling human studies for an investigational drug is also discussed.
Conclusions:
Drug discovery is a complex process that has significantly evolved in recent years.
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