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Related Experiment Videos

Development of a high throughput equilibrium dialysis method.

I Kariv1, H Cao, K R Oldenburg

  • 1Leads Discovery Department, Dupont Pharmaceuticals Company, Rt. 141 & Henry Clay Road, Wilmington, Delaware 19880, USA. ilona.kariv@dupontpharma.com

Journal of Pharmaceutical Sciences
|April 5, 2001
PubMed
Summary
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A new 96-well equilibrium dialysis plate enables high throughput screening (HTS) of plasma protein binding for drug candidates. This method accurately assesses drug-like properties early in development, improving lead prioritization.

Area of Science:

  • Pharmacology
  • Drug Discovery
  • Analytical Chemistry

Background:

  • High throughput screening (HTS) identifies numerous biologically active compounds.
  • Early assessment of drug-like properties, including plasma protein binding, is crucial for lead prioritization.
  • Traditional equilibrium dialysis is not suitable for HTS formats.

Purpose of the Study:

  • To develop a high throughput equilibrium dialysis device for assessing plasma protein binding.
  • To validate the 96-well format equilibrium dialysis plate for drug development.

Main Methods:

  • Development of a 96-well format equilibrium dialysis plate.
  • Assay validation using three drugs (propranolol, paroxetine, losartan) with varying binding properties.
  • Comparison of results with traditional equilibrium dialysis techniques.

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Main Results:

  • Successful development of a 96-well equilibrium dialysis plate.
  • Plasma protein binding data obtained using the new method correlated well with published data.
  • The assay is suitable for HTS drug development.

Conclusions:

  • The 96-well equilibrium dialysis plate is a viable tool for high throughput assessment of plasma protein binding.
  • This method facilitates early identification of compounds with favorable drug-like properties.
  • The developed device supports efficient lead prioritization in drug discovery processes.