Practical Fragments

The twin rise of make-on-demand libraries and speedy in silico docking has supercharged fragment screening and optimization: we’ve written p...

Glioblastoma multiforme (GBM) is a particularly nasty type of brain tumor with few drug options aside from the DNA alkylating agent temozolo...

In 2009 we highlighted a paper reporting that approved drugs have a higher fraction of sp 3 -hybridized carbon atoms than discovery-phase c...

As we noted just last week, crystallography has unleashed a torrent of protein-ligand complexes, especially fragments. Historically a singl...

As the title states, this is the 1000 th post at Practical Fragments . This blog was conceived in 2008 over drinks at the Third Annual CHI ...

E3 ligase proteins conjugate ubiquitin to other proteins, changing their function or targeting them for degradation. Hijacking E3 ligases us...

At the end of 2023 I mentioned that a paper by Dean Brown listed berotralstat as a fragment-derived drug. Readers will notice this molecule...

After a bumper year for conferences in 2024, this year is also shaping up to be eventful.  April 14-17:  CHI’s Twentieth Annual  Fragment-Ba...

Long winter is here in the global north, with its dim days and gaping nights. As is tradition , Practical Fragments looks back on the year ...

Last week we highlighted the construction of a covalent fragment library at AstraZeneca. The first fruits of this library have recently bee...

Covalent fragment-based lead discovery is becoming ever more popular, driven by success against difficult targets such as KRAS G12C . These...

Practical Fragments has written repeatedly about various assay artifacts (vide infra). Different technologies are susceptible to different ...

Proteins can be remarkably dynamic, and, as we noted recently, different conformational states can reveal different pockets for small molec...

Perhaps because it sounds like “chicken,” when I first heard of chikungunya I thought it was a joke. But there’s nothing funny about a dise...