Practical Fragments

Last week we highlighted work out of Steve Fesik’s lab at Vanderbilt University about PLPro. This week we’ll highlight another paper just p...

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

Since the invention of ligand efficiency ( LE ) more than two decades ago, scholars have been debating its strengths and weaknesses. And alt...

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

Despite the effectiveness of vaccines against SARS-CoV-2, COVID-19 continues to plague us. The handful of approved small molecule drugs targ...

Last year we celebrated the ten-year anniversary of the Chemical Probes Portal. One of the key requirements for a chemical probe is selecti...

Among the many biophysical techniques presented at the recent Novalix meeting , hydrogen/deuterium exchange mass spectrometry ( HDX-MS ) was...

Last week the Twelfth Novalix Biophysics in Drug Discovery Conference was held for the first time in La Jolla, California. It’s been severa...

Last month we highlighted a paper from Iwan de Esch and colleagues at Vrije Universiteit Amsterdam about assessing molecular shapeliness....

It’s been a couple years since Practical Fragments last updated our “fragments in the clinic” list . Before doing so it makes sense to high...

Last year we highlighted an example of crystallographic screening of crude reaction mixtures to find inhibitors against the oncology target...

Transcription factors can be difficult drug targets, particularly those whose primary structure is a “leucine zipper” in which two α -helice...