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Related Experiment Video

Updated: Mar 16, 2026

Extracellular Protein Microarray Technology for High Throughput Detection of Low Affinity Receptor-Ligand Interactions

Extracellular Protein Microarray Technology for High Throughput Detection of Low Affinity Receptor-Ligand Interactions

Published on: January 7, 2019

Selectivity Determination of a Small Molecule Chemical Probe Using Protein Microarray and Affinity Capture

Erik C Hett¹, Robert E Kyne², Ariamala Gopalsamy¹

¹Medicine Design, Pfizer , 610 Main Street, Cambridge, Massachusetts 02139, United States.

ACS Combinatorial Science

|August 6, 2016

Summary

This study demonstrates how a tritiated probe and protein microarray effectively assess drug selectivity for the DcpS enzyme. Diaminoquinazoline inhibitors show excellent selectivity, validating these methods for drug discovery.

Keywords:

affinity enrichment cap-binding protein chemical probe protein microarray

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Last Updated: Mar 16, 2026

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Published on: January 7, 2019

Identification of Small Molecule-binding Proteins in a Native Cellular Environment by Live-cell Photoaffinity Labeling

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Published on: September 20, 2016

Probing High-density Functional Protein Microarrays to Detect Protein-protein Interactions

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Published on: August 2, 2015

Area of Science:

Chemical biology
Drug discovery
Biochemistry

Background:

Small molecule selectivity is critical for drug development and target validation.
Understanding off-target effects requires advanced protein profiling technologies.

Purpose of the Study:

To evaluate the binding selectivity of a DcpS enzyme inhibitor.
To showcase the utility of protein microarrays and affinity enrichment in drug discovery.

Main Methods:

Utilized a tritiated chemical probe and a human protein microarray (9000 proteins).
Employed immobilized m7GTP resin for assessing selectivity against mRNA cap-associated proteins in cell extracts.

Main Results:

Confirmed the exquisite selectivity of diaminoquinazoline inhibitors for DcpS.
Demonstrated the effectiveness of protein microarrays for broad protein profiling.

Conclusions:

Protein microarray and affinity enrichment are valuable tools for assessing drug candidate selectivity.
These methods aid in understanding off-target effects and validating drug targets.