Practical Fragments

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

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

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

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...

Ligand efficiency ( LE ) was proposed more than two decades ago as “a useful metric for lead selection.” The concept is simple: divide the b...

As we noted in our thousandth post , covalent drugs are becoming increasingly popular, particularly for tackling tough targets. But finding ...

Last week’s CHI Drug Discovery Chemistry (DDC) meeting was held as usual in San Diego. More than 850 people attended, 96% in person, with 7...