Fig. 1.

Testing scheme for CHD1Li drug discovery. CHD1Li are selected from either HTS hits or analogs developed from a previously identified hit. They are then subjected to different in vitro assays in the “testing funnel” to filter out the less promising hits or analogs. Highly promising compounds are advanced for further testing and the most promising (leads) are taken through in vivo testing or used as structural templates for lead optimization using medicinal chemistry. Results from all tests are analyzed for existing SAR to design new analogs and improve efficacy.