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Encoded chemical synthesis coupled to screening: "Pot Assay"
Z Parandoosh1, S K Knowles, X Y Xiao
1IRORI, La Jolla, CA 92037-1031, USA. parandoosh@aol.com
Combinatorial Chemistry & High Throughput Screening
|September 29, 1999
Summary
A novel Pot Assay enables direct screening of Radiofrequency Encoded Combinatorial chemistry libraries. This method rapidly identifies high-affinity binders using radiofrequency signals, streamlining lead compound discovery.
Area of Science:
- Medicinal Chemistry
- Biochemistry
- Analytical Chemistry
Background:
- Traditional screening methods for lead compound identification can be labor-intensive.
- Radiofrequency Encoded Combinatorial chemistry (RECC) generates large libraries of small molecules on individual encoded supports.
- Direct screening of RECC libraries can significantly reduce processing steps.
Purpose of the Study:
- To develop a direct screening method for RECC libraries.
- To introduce the Pot Assay, a multiplex assay for simultaneous binding measurements.
- To validate the Pot Assay's ability to decode high-affinity binders using radiofrequency signals.
Main Methods:
- Development of the Pot Assay, a multiplex binding assay.
- Utilizing specific radiofrequency signals for compound decoding.
- Validation using the biotin-streptavidin interaction with analogs.
Main Results:
- The Pot Assay was successfully developed and validated.
- It demonstrated rapid, simple, sensitive, and accurate identification of active compounds.
- The assay effectively decoded high-affinity binders from RECC libraries.
Conclusions:
- The Pot Assay offers a streamlined approach for screening RECC libraries.
- This method integrates RECC with direct screening, enhancing efficiency.
- The Pot Assay is applicable to various binding-based screening applications, including ligand/receptor and inhibitor/enzyme interactions.