title: Designing novel building blocks is an overlooked strategy to improve compound quality.
abstract: One pragmatic way to improve compound quality, while enhancing and accelerating drug discovery projects, is the ability to access a high quality, novel, diverse building block collection. Here, we outline general principles that should be applied to ensure that a building block collection has the greatest impact on drug discovery projects, by discussing design principles for novel reagents and what types of reagents are popular with medicinal chemists in general. We initiated a program in 2009 to address this, which has already delivered three candidate drugs, and the success of that program provides evidence that focussing on building block design is a useful strategy for drug discovery.
authors.affiliation: AstraZeneca, Alderley Park, Macclesfield SK10 4TG, UK. Electronic address: frederick.goldberg@astrazeneca.com.
authors.forename: Frederick W
authors.initials: FW
authors.lastname: Goldberg
authors.affiliation: AstraZeneca, Alderley Park, Macclesfield SK10 4TG, UK.
authors.forename: Jason G
authors.initials: JG
authors.lastname: Kettle
authors.affiliation: AstraZeneca, SE-43183 Mölndal, Sweden.
authors.forename: Thierry
authors.initials: T
authors.lastname: Kogej
authors.affiliation: AstraZeneca, SE-43183 Mölndal, Sweden.
authors.forename: Matthew W D
authors.initials: MW
authors.lastname: Perry
authors.affiliation: AstraZeneca, Alderley Park, Macclesfield SK10 4TG, UK.
authors.forename: Nick P
authors.initials: NP
authors.lastname: Tomkinson
mesh_terms: D015195:Drug Design; D007202:Indicators and Reagents / Q000737:chemistry
chemical_list: D007202:Indicators and Reagents