title: Increasing the delivery of next generation therapeutics from high throughput screening libraries.
abstract: The pharmaceutical industry has historically relied on high throughput screening as a cornerstone to identify chemical equity for drug discovery projects. However, with pharmaceutical companies moving through a phase of diminished returns and alternative hit identification strategies proving successful, it is more important than ever to understand how this approach can be used more effectively to increase the delivery of next generation therapeutics from high throughput screening libraries. There is a wide literature that describes HTS and fragment based screening approaches which offer clear direction on the process for these two distinct activities. However, few people have considered how best to identify medium to low molecular weight compounds from large diversity screening sets and increase downstream success.
authors.affiliation: Global High Throughput Screening, Discovery Sciences, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK. Electronic address: Mark.Wigglesworth@astrazeneca.com.
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Wigglesworth
authors.affiliation: Global High Throughput Screening, Discovery Sciences, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK.
authors.forename: David C
authors.initials: DC
authors.lastname: Murray
authors.affiliation: Global High Throughput Screening, Discovery Sciences, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK.
authors.forename: Carolyn J
authors.initials: CJ
authors.lastname: Blackett
authors.affiliation: Compound Collection Enhancement, Discovery Sciences, AstraZeneca, Pepparedsleden 1, 43183 Mölndal, Sweden.
authors.forename: Michael
authors.initials: M
authors.lastname: Kossenjans
authors.affiliation: Oncology iMed, AstraZeneca, Unit 310, Darwin Building, Cambridge Science Park, Milton Road, Cambridge CB4 0WG, UK.
authors.forename: J Willem M
authors.initials: JW
authors.lastname: Nissink
mesh_terms: D015195:Drug Design; D055808:Drug Discovery / Q000191:economics / Q000379:methods; D015723:Gene Library; D057166:High-Throughput Screening Assays / Q000191:economics* / Q000379:methods; D006801:Humans; D057786:Peptidomimetics / Q000138:chemical synthesis* / Q000494:pharmacology; D054852:Small Molecule Libraries / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D057786:Peptidomimetics; D054852:Small Molecule Libraries