CONTEXT

Discovery of new medicaments involves developing methods for high-throughput screening of libraries of molecules which are effective, i.e. which make it possible to isolate, from a restricted number of selected molecules (hits), molecules which are active in vivo on the pathology intended to be treated (leads).
In fact, functional tests (in vitro in cell culture or in vivo in an appropriate animal model) which make it possible to verify the activity of the hits selected during the screening are not generally adaptable to high-throughput. Since most eukaryotic proteins are multifunctional and involved in several functional cascades, the molecules isolated must be capable of specifically modulating the property of interest of the target without affecting its other activities, the modulation of which could have detrimental effects for the cell. Consequently, the screening must be highly specific in order to restrict to a maximum the number of hits identified, so that only a small number of them have to be tested in functional tests in vivo.