Fragment-based approaches to finding novel small molecules that bind to proteins are now
firmly established in drug discovery and chemical biology. Initially developed primarily in a …

The pharmaceutical industry's ability to produce new medicines is directly tied to its success
in identifying druglike molecules that target clinically relevant pathways. As a consequence …

▪ Abstract The genomics revolution has provided a deluge of new targets for drug discovery.
To facilitate the drug discovery process, many researchers are turning to fragment-based …

Since the first report appeared in 19961 describing the use of NMR spectroscopy to screen
for potential drug molecules, the field of NMR-based screening has evolved rapidly. Over the …

According to Hann's model of molecular complexity an increased probability of detection
binding to a target protein can be expected when small, low complex molecular fragments …

Natural products have historically been a rich source of lead molecules in drug discovery.
However, natural products have been de-emphasized as high throughput screening …

We have designed four generations of a low molecular weight fragment library for use in
NMR-based screening against protein targets. The library initially contained 723 fragments …

Our current understanding of the structure, mechanism of action and modes of regulation of
the protein tyrosine kinase family owes a great deal to structural biology. Structures are now …

The two subunits of core binding factor (Runx1 and CBFβ) play critical roles in
hematopoiesis and are frequent targets of chromosomal translocations found in leukemia …

Many of today's drug discovery programs use high-throughput screening methods that rely
on quick evaluations of protein activity to rank potential chemical leads. By monitoring …