In Vitro High Throughput Screening, What Next? Lessons from the Screening for Aurora Kinase Inhibitors

Abstract

Based on in vitro assays, we performed a High Throughput Screening (HTS) to identify kinase inhibitors among 10,000 small chemical compounds. In this didactic paper, we describe step-by-step the approach to validate the hits as well as the major pitfalls encountered in the development of active molecules. We propose a decision tree that could be adapted to most in vitro HTS.

Keywords

• aurora
• kinase
• kinase inhibitor
• Gck
• Nuak1
• Tak-1