title: Ion channel screening plates: design, construction, and maintenance.
abstract: Ion channels have provided a diverse set of therapeutic targets across all areas of the pharmaceutical industry. Many companies are pursuing this unique class of targets for areas of unmet medical need such as neuropathic and inflammatory pains. In the past, focused library screening sets had been designed for CNS and kinase targets. Our investigations were aimed at creating a similar dynamic screening set enriched for compounds targeting ion channels to aid screening efforts of this important class of targets. The key advantages of this approach for ion channel targets would be: (1) to identify tool compounds for novel targets and assist in assay validation, (2) to serve as a focused screen for non-384-well adaptable targets, and (3) to jump start a particular program, that is, catch-up to competition for validated, well-known targets.
authors.affiliation: Chemical Sciences, Pfizer Global Research and Development, Princeton, New Jersey 08543, USA. ssammayer@optonline.net
authors.forename: Scott C
authors.initials: SC
authors.lastname: Mayer
authors.forename: John A
authors.initials: JA
authors.lastname: Butera
authors.forename: David J
authors.initials: DJ
authors.lastname: Diller
authors.forename: John
authors.initials: J
authors.lastname: Dunlop
authors.forename: John
authors.initials: J
authors.lastname: Ellingboe
authors.forename: Kristi Yi
authors.initials: KY
authors.lastname: Fan
authors.forename: Edward
authors.initials: E
authors.lastname: Kaftan
authors.forename: Belew
authors.initials: B
authors.lastname: Mekonnen
authors.forename: Dominick
authors.initials: D
authors.lastname: Mobilio
authors.forename: Jeff
authors.initials: J
authors.lastname: Paslay
authors.forename: Gregory
authors.initials: G
authors.lastname: Tawa
authors.forename: Dmitry
authors.initials: D
authors.lastname: Vasilyev
authors.forename: Mark R
authors.initials: MR
authors.lastname: Bowlby
mesh_terms: D015195:Drug Design; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D015640:Ion Channel Gating; D007473:Ion Channels / Q000032:analysis / Q000378:metabolism*; D008958:Models, Molecular; D058990:Molecular Targeted Therapy; D054852:Small Molecule Libraries
chemical_list: D007473:Ion Channels; D054852:Small Molecule Libraries