Ninety percent of clinical drug development fails despite implementation of many successful
strategies, which raised the question whether certain aspects in target validation and drug …

Background Monitoring target engagement at various stages of drug development is
essential for natural product (NP)-based drug discovery and development. The cellular …

Assessment of the interactions between a drug and its protein target in a physiologically
relevant cellular environment constitutes a major challenge in the pre-clinical drug discovery …

Small molecule chemical probes are valuable tools for interrogating protein biological
functions and relevance as a therapeutic target. Rigorous validation of chemical probe …

Measuring and quantifying the binding of a drug to a protein target inside living cells and
thereby correlating biochemical or biophysical activity with target engagement in cells or …

Small-molecule (SM) leads in the early drug discovery pipeline are progressed primarily
based on potency against the intended target (s) and selectivity against a very narrow slice …

The binding affinity and kinetics of target engagement are fundamental to establishing
structure–activity relationships (SARs) for prospective therapeutic agents. Enhancing these …

Thermal shift assays (TSAs) can reveal changes in protein structure, due to a resultant
change in protein thermal stability. Since proteins are often stabilized upon binding of ligand …

Determining a molecule's mechanism of action is paramount during chemical probe
development and drug discovery. The cellular thermal shift assay (CETSA) is a valuable tool …

The cellular thermal shift assay (CETSA) was introduced in 2013 to investigate drug–target
engagement inside live cells and tissues. As with all thermal shift assays, the response …