Practical Fragments

Last week we highlighted an example of adding a warhead to a fragment-derived, non-covalent protein binder to generate a covalent inhibitor...

Targeting proteins involved in DNA repair is a promising approach against cancer. However, finding effective small molecule inhibitors can b...

The list of technologies used to find and validate fragments is long, with more than a dozen in our 2024 poll . But it’s always fun to learn...

Cambridge Healthtech Institute held its annual Discovery on Target ( DoT ) meeting in Boston last week. Attendance may have set a record, wi...

Without a good library, it is difficult to find a good hit, so library design is one of the most import aspects of a screening campaign. The...

The goal of lead optimization is to improve the properties of a molecule such that it can become a drug or a chemical probe . Early in a pro...

NLRP3 has received considerable attention as an inflammatory disease target. The protein normally exists in an auto-inhibited conformation, ...

Last week we highlighted how NMR-based fragment screening was able to identify cryptic pockets on a small protein. Experimental methods are...

We’ve written previously about the concept of synthetic lethality, in which changes to one protein make cancer cells more dependent on anot...

RNA helicases present an intriguing but challenging opportunity for drug discovery. Their importance for cell growth makes them attractive c...

Most methods to characterize protein-ligand binding interactions have drawbacks. Crystallography, obviously, requires your protein to crysta...

Protein tyrosine phosphatase 1B (PTP1B) is a long-standing target for diabetes and other diseases. But as we’ve written previously, it is c...

Back in 2009 we highlighted a paper, “Escape from flatland,” suggesting that molecules with higher fractions of sp 3 -hybridized (ie, non-a...

Earlier this year we highlighted a study that compared the affinities of kinase inhibitors for isolated proteins vs those same proteins in ...

Differential scanning fluorimetry (DSF), also known as a thermal shift assay, is one of the most common techniques for fragment screening ac...

Last month Practical Fragments wrote about make-on-demand libraries, such as those offered by Enamine. We’ve also written about fluorine-...