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

Biology

Thi-My-Nhung Hoang²  Hong-Lien Vu²  Ly-Thuy-Tram Le²  Chi-Hung Nguyen¹ 

[1] UMR 176 CNRS-Institut Curie, Bat 110 Centre Universitaire, Orsay 91405, France; E-Mail:;INSERM UJF U823 Institut Albert Bonniot, Team 4: Chromatin and Epigenetic, BP 170, 38 042 Grenoble Cedex 9, France; E-Mails:

关键词: aurora;    kinase;    kinase inhibitor;    Gck;    Nuak1;    Tak-1;   

DOI  :  10.3390/biology3010167

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.