Practical Fragments

Exactly 17 years ago, I  highlighted a paper from Brian Shoichet’s lab in which he hypothesized that only tiny regions of chemical space ar...

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 week we wrote about NMR, one of the most popular fragment-finding methods. This week we turn to a less common technique: weak affinit...

Virtual screening is continuing to make impressive strides. The latest example , in Nature , comes from William Wetsel (Duke), John Irwin (...

Last week we highlighted the use of surface plasmon resonance ( SPR ) to find ligands against RNA. Although RNA is not a typical protein ta...

Of the 50+ fragment-derived drugs that have entered the clinic , only two (both from Sosei Heptares) target transmembrane proteins, reflecti...

Earlier this year we highlighted a fragment optimization success story against a G protein-coupled receptor (GPCR) which made no use of str...

Last week we described a fragment library built with the aid of machine learning and designed to contain privileged fragments that should ...

Last week’s post highlighted how biophysical methods, and in particular structural insights, can be critical for advancing fragments to lea...

Last week NovAliX  held its biophysics meeting  outside of Strasbourg for the first time. Naturally they chose Boston, one of the most Euro...

Membrane-bound proteins such as GPCRs are often ignored by practitioners of FBLD in part because – Heptares notwithstanding – they are us...

G protein-coupled receptors (GPCRs) are common drug targets that present challenges for fragment-based approaches. Biophysical studies of t...

There are certain movies that when they are on TV, I can't not watch.  I call these Broken Leg Movies (as in if I were laid up with a b...

This is the straight-to-the-point title of a new book published by the Royal Society of Chemistry, edited by Steven Howard ( Astex ) and C...

Yesterday brought news that Heptares was purchased by Sosei.  The deal is for 180$MM upfront and 220$MM in royalties.  Similar to the Astex...

The year is spinning to an end, and as we did in 2013 and 2012 , Practical Fragments is looking back on notable events as well as reviews...

The latest issue of Prog. Biophys. Mol. Biol. includes five articles on fragment-related topics. We already discussed one from Astex; bri...