Practical Fragments

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

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

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...

Native mass spectrometry ( nMS ) is one of the less commonly used fragment-finding methods . The approach entails mixing proteins and ligand...

Last week we highlighted a ligand-detected NMR method to measure affinities of protein-ligand interactions. That technique, R2KD, requires ...

Just over seven years ago Practical Fragments highlighted work out of Merck describing the discovery and optimization of potent, selective ...

Last week we highlighted work out of Vernalis and Servier in which fragment-based methods were used to identify potent and selective inhibi...

The dual-specificity tyrosine-phosphorylation-regulated kinases 1A and 1B (DYRK1A and DYRK1B) belong to a family of five serine/threonine ki...

Leucine-rich repeat kinase 2 (LRRK2) has been implicated in Parkinson’s disease and has thus long been targeted by drug hunters. Dozens of i...

RNA is hot. Hundreds of millions of dollars have gone to startups focused on finding small molecules that bind RNA, and plenty of large phar...

Four years ago we highlighted a paper from LEO Pharma describing inhibitors of the kinase JAK1, which is implicated in a host of inflammat...

A common approach in drug discovery is to improve a previously reported molecule. An example of such a “fast follower” approach has just be...

FBLD, of course, starts with small libraries of small fragments. DNA-encoded chemical libraries ( DEL ) usually start from the opposite ext...