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Stepwise Dosing Protocol for Increased Throughput in Label-Free Impedance-Based GPCR Assays
Published on: February 21, 2020
Enhanced selectivity screening of GPCR ligands using a label-free cell based assay technology
R P McGuinness1, J M Proctor, D L Gallant
1MDS Analytical Technologies, Sunnyvale, CA 94089, USA. ryan.mcguinness@moldev.com
Combinatorial Chemistry & High Throughput Screening
|June 18, 2009
Summary
This study demonstrates how the impedance-based CellKey System, a label-free live cell assay, effectively screens compounds for G-protein coupled receptor (GPCR) selectivity. This technology aids in better decision-making during drug discovery by analyzing drug-target interactions.
Area of Science:
- Biotechnology
- Pharmacology
- Assay Development
Background:
- Advancements in assay technologies enhance drug discovery by improving the understanding of drug-target interactions.
- Label-free technologies offer significant advantages in drug discovery workflows.
- The CellKey System is a novel impedance-based, label-free live cell assay platform.
Purpose of the Study:
- To evaluate the CellKey System's utility for functional measurement of G-protein coupled receptors (GPCRs).
- To perform an enhanced selectivity screen of compounds against two unrelated GPCR targets using impedance technology.
- To demonstrate the application of impedance-based technology for selectivity analyses and lead compound triage.
Main Methods:
- Utilized the CellKey System, an impedance-based label-free live cell assay platform.
- Performed kinetic measurements on endogenously expressed and transfected GPCRs across various cell types.
- Conducted a simultaneous selectivity screen of a compound panel against two distinct GPCR targets.
Main Results:
- The CellKey System provided quantitative measures of cellular activation and qualitative interaction data.
- Successfully determined the relative selectivity of compounds across both GPCR targets.
- Gained insights into the character of compound-target interactions.
Conclusions:
- Impedance-based technology, exemplified by the CellKey System, is effective for performing selectivity analyses in drug discovery.
- The CellKey System offers a simplified format for triaging lead compounds.
- This label-free approach enhances decision-making in the drug discovery process.
