Related Experiment Video
Updated: Apr 5, 2026

A Fluorescence-based Lymphocyte Assay Suitable for High-throughput Screening of Small Molecules
Published on: March 10, 2017
Identifying compound efficacy targets in phenotypic drug discovery
Markus Schirle1, Jeremy L Jenkins1
1Developmental & Molecular Pathways, Novartis Institutes for BioMedical Research, Cambridge, MA 02139, USA.
Identifying drug targets and understanding compound mechanisms are crucial for drug development. This review covers key technologies for characterizing compound targets after phenotypic screening, aiding in assessing efficacy and potential liabilities.
Area of Science:
- Pharmacology
- Medicinal Chemistry
- Drug Discovery
Background:
- Identifying efficacy targets for compounds from phenotypic screening is essential for drug development.
- Characterizing epistatic proteins and off-targets aids in elucidating mechanisms of action and assessing liabilities.
Purpose of the Study:
- To review current technologies for characterizing the direct and indirect target space of bioactive compounds.
- To present a comprehensive strategy using complementary approaches for target identification.
Main Methods:
- Review of key technologies for target identification post-phenotypic screening.
- Discussion of complementary approaches to address technology strengths and weaknesses.
Main Results:
- Phenotypic screening requires robust methods for target identification.
- A combination of technologies provides a balanced approach to target characterization.
Conclusions:
- Effective target identification strategies are vital for advancing compounds in drug development.
- Complementary technologies enhance the characterization of compound targets and mechanisms.
More Related Videos
10:21Author Spotlight: Streamlining Protein Target Prediction and Validation via Molecular Docking and CETSA
Published on: February 23, 2024
08:31Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
Published on: December 1, 2020
Related Concept Videos
Drug Discovery: Overview
Pharmacogenomics: Identification of New Drug Targets
Targets for Drug Action: Overview
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Pharmacogenetic Phenotypes: Alterations in Pharmacokinetics, Drug Targets and Biologic Milieu
Structure-Activity Relationships and Drug Design
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...
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase