High-Throughput Screening

High-Throughput Screening

1. Definition & overview

• High-throughput screening (HTS) is an automated, microprocessor-controlled robotic process that evolved from the older manual, low-speed screening of compounds against a biological target; it is a synergy of chemistry, biology, engineering and informatics (SK Gupta Ch.2, p.20).
• HTS allows over 50,000–100,000 compounds to be screened per week against a validated biological target; further advances allow 10,000–100,000 compounds to be screened within 24 h, a process termed ultra-high-throughput screening (uHTS) (SK Gupta Ch.2, p.20).
• High-throughput synthesis of large numbers of test compounds in a shorter time is now a reality, feeding the compound libraries that HTS consumes (SK Gupta Ch.2, p.20).
• Parallel advances in drug synthesis, toxicity screening, and drug metabolism and pharmacokinetics (DMPK) studies help the overall process reach its ultimate speed in new drug development (NDD) (SK Gupta Ch.2, p.20).
• In the drug-research workflow, target identification, purification, and assay development constitute the initial step; potential compounds are then screened against the identified target (SK Gupta Ch.2, p.20).
• Over the last quarter-century the pharmaceutical industry has shifted to fast-track, target-oriented drug discovery; market estimates project a new molecule's journey from laboratory to market takes well over seven years at an average cost of over $600 million (SK Gupta Ch.1, p.1).
• The revolutionary technological advances that cumulatively increased the speed of lead generation are: combinatorial chemistry, biochemical assays, genomics, proteomics, miniaturization, automation, robotic systems, and computerization (SK Gupta Ch.1, p.1).