title: Integrating biophysics with HTS-driven drug discovery projects.
abstract: Over the past decade biophysics has become an established discipline in HTS hit triaging, owing to its high fidelity in detecting protein-ligand interactions. Many pharma companies are using biophysical techniques to filter HTS output for false positives, as will be discussed in this review. Moreover, I will demonstrate how the earlier application of biophysics, already at the HTS assay development stage, is potentially even more impactful. Two key areas here are early mode-of-action studies and ensuring that the HTS assay and subsequent cascade are fit for purpose. Top-level results from 20 in-house projects are shown to underpin the impact of these studies.
authors.affiliation: Dept of Structure & Biophysics, Discovery Sciences, AstraZeneca R&D, Mölndal SE-431 83, Sweden. Electronic address: rutger.folmer@astrazeneca.com.
authors.forename: Rutger H A
authors.initials: RH
authors.lastname: Folmer
mesh_terms: D001681:Biological Assay; D055592:Biophysical Phenomena; D017046:Cost Savings; D055808:Drug Discovery / Q000191:economics; D057166:High-Throughput Screening Assays / Q000191:economics; D007202:Indicators and Reagents
chemical_list: D007202:Indicators and Reagents