In vitro high throughput screening, what next? Lessons from the screening for aurora kinase inhibitors.
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.
INSERM UJF U823 Institut Albert Bonniot, Team 4: Chromatin and Epigenetic, BP 170, 38 042 Grenoble Cedex 9, France. hoangthimynhung@hus.edu.vn.
Thi-My-Nhung
TM
Hoang
INSERM UJF U823 Institut Albert Bonniot, Team 4: Chromatin and Epigenetic, BP 170, 38 042 Grenoble Cedex 9, France. honglien162@yahoo.com.
Hong-Lien
HL
Vu
INSERM UJF U823 Institut Albert Bonniot, Team 4: Chromatin and Epigenetic, BP 170, 38 042 Grenoble Cedex 9, France. llttram@gmail.com.
Ly-Thuy-Tram
LT
Le
UMR 176 CNRS-Institut Curie, Bat 110 Centre Universitaire, Orsay 91405, France. Chi.Hung@curie.fr.
Chi-Hung
CH
Nguyen
INSERM UJF U823 Institut Albert Bonniot, Team 4: Chromatin and Epigenetic, BP 170, 38 042 Grenoble Cedex 9, France. annie.molla@ujf-grenoble.fr.
Annie
A
Molla