Project highlights: screened collection and identified several series of compounds that inhibited IDH1 R132H and were synthetically tractable. Inhibition of WT IDH1 and IDH1 R132C was also assessed as was 2-HG levels in cell-based assay format. Selected compounds were characterized further in mechanism of action and binding assays. During this period, the NCGC has fostered and maintained over 180 active collaborations with both NIH and extramural investigators, facilitating drug discovery efforts across the entire spectrum of human disease. These efforts have led to over 100 high-throughput screens and nearly 60 medicinal chemistry campaigns, providing our collaborators and the general research community a wealth of publications and promising small molecule leads. In addition, the NCGC has undertaken a number of informatic challenges to make better use of existing drug and disease target information and provide the general public with easily accessible resources, further catalyzing the development of new therapies for human disease.
