Practical Fragments

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

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...

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

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

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

Fragment linking is a compelling approach to advancing fragments, but, as our poll from several years ago showed, it often works better in ...

Last week we highlighted a study in which an attempt to optimize a covalent fragment led to a non-covalent fragment that bound in a differe...

The seven members of the 14-3-3 family act as “hub proteins” that bind to other proteins, bringing them together or affecting their subcellu...

Just over two years ago we highlighted a new clinical candidate targeting WRN, a covalent inhibitor then called VVD-133214. An open-access ...

Last week we described the discovery and early optimization of noncovalent inhibitors against the the DNA helicase WRN, an interesting onco...

Last week some 875 people attended the CHI Drug Discovery Chemistry ( DDC ) meeting in San Diego. I can’t do justice to the 40 or so present...

The most successful drug against COVID-19, nirmatrelvir, targets the main protease of SARS-CoV-2. As we discussed just last year, this prot...

As covalent drug discovery continues to rise, the demand for metrics to help guide lead optimization is increasing. Last year we discussed c...

As covalent drug discovery becomes increasingly common , researchers are becoming more rigorous in how they characterize their molecules. Th...

Turning and turning in the widening gyre The falcon cannot hear the falconer…   In our small, annual counterweight to Yeats’ “ mere a...