After 20 years of sometimes quiet growth, fragment-based drug discovery (FBDD) has
become mainstream. More than 30 drug candidates derived from fragments have entered …

Fragment-based approaches to finding novel small molecules that bind to proteins are now
firmly established in drug discovery and chemical biology. Initially developed primarily in a …

Fragment-based drug discovery (FBDD) is well suited for discovering both drug leads and
chemical probes of protein function; it can cover broad swaths of chemical space and allows …

It is over 20 years since the first fragment-based discovery projects were disclosed. The
methods are now mature for most 'conventional'targets in drug discovery such as enzymes …

Research into the chemical biology of bromodomains has been driven by the development
of acetyl-lysine mimetics. The ligands are typically anchored by binding to a highly …

Screening methods seek to sample a vast chemical space in order to identify starting points
for further chemical optimisation. Fragment based drug discovery exploits the superior …

This Review describes the increasing demand for organic synthesis to facilitate fragment-
based drug discovery (FBDD), focusing on polar, unprotected fragments. In FBDD, X-ray …

Computational conformational sampling underpins many aspects of small molecule
modeling and design in pharmaceutical work. This work examined in detail the widely …

Current fragment-based drug design relies on the efficient exploration of chemical space by
using structurally diverse libraries of small fragments. However, structurally dissimilar …

Fragment-based drug discovery is a validated approach for the discovery of drug
candidates. However, the weak affinity of fragment compounds requires highly sensitive …