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THE PHARMA REVIEW (FEBRUARY - MARCH, 2008)

High Throughput Screening (HTS) Technique in Drug Discovery

Dipak L. Kale, Dr. S. C. Chaturvedi, Deepak Patil, Dr. R. B. Kakde

Abstract: High-throughput screening (HTS) is an approach to drug discovery that has gained widespread popularity over the last three or four years. HTS is the process of assaying a large number of potential effectors of biological activity against targets (a biological event). The methods of HTS are applied to the screening of combinatorial chemistry, genomics, protein and peptide libraries. The goal of HTS is to accelerate drug discovery by screening large libraries often composed of hundreds of thousands of compounds (drug candidates) at a rate that may exceed 20,000 compounds per week.

Introduction

High Throughput Screening (HTS) refers to a modern process whereby thousands of samples can be screened each day, against a given (known or unknown) target (disease). This process has led to a significant improvement in “Lead Identification”. Leads are those samples which may eventually become candidate drugs by-

  • Firstly improving the spectrum of sample structures believed to have some possible effect, and

  • Secondly by quickly eliminating those samples which have no effect.

HTS is usually involved in the first phase after a target has been identified and is currently one of the few areas in the whole drug discovery process where significant time savings can be made in finding candidate drugs. For this reason HTS has seen widespread adoption amongst all of the major pharmaceutical companies.

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