Ion channel screening plates: design, construction, and maintenance.
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.
Mayer
Scott C
SC
Chemical Sciences, Pfizer Global Research and Development, Princeton, New Jersey 08543, USA. ssammayer@optonline.net
Butera
John A
JA
Diller
David J
DJ
Dunlop
John
J
Ellingboe
John
J
Fan
Kristi Yi
KY
Kaftan
Edward
E
Mekonnen
Belew
B
Mobilio
Dominick
D
Paslay
Jeff
J
Tawa
Gregory
G
Vasilyev
Dmitry
D
Bowlby
Mark R
MR
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
D007473:Ion Channels; D054852:Small Molecule Libraries