IHL phase passes the thousand compounds mark for public programmes

News
23 March 2016

Public target programmes that have received a promising Qualified Hit List (QHL) have the possibility to continue their collaboration with the European Lead Factory with the aim of producing an Improved Hit List (IHL). 

The aim of the IHL phase is to validate the hits identified during the HTS triage. This includes re-synthesis of selected QHL compounds to provide an authentic solid sample for hit characterisation, evidence for mechanism of action and further biochemical and biophysical profiling. Hit expansion around promising chemotypes is then carried out to develop early structure activity relationships. Crystallography and computational modelling is used to guide the medicinal chemistry design process. To date, 17 programmes have entered this phase and more than 1000 compounds have been synthesised and tested by the scientists of the European Screening Centre, Newhouse.

The diversity of compounds arriving on QHLs is considerable and so far over 250 different Bemis-Murcko scaffolds have been prepared. The efforts of the contributing scientists has resulted in the delivery of potent, well validated and tractable Hit Series for programme owners to exploit and continue their research efforts. The people in the picture are members of the Newhouse group in Scotland.