Andy Zaayenga
Forum Admin
USA
293 Posts |
 Posted - 11/21/2002 : 1:52:57 PM
Presentation: Count the Ways: Automated Biochemical Counter-Screening for Kinase Drug Discovery
Gordon Alton, Department of Biochemistry, Pfizer Global R and D, La Jolla Labs
[email protected]One of the most critical issues for protein kinase drug discovery is selectivity. Since most kinase inhibitors are targeted to the ATP-binding site and there are more than 500 kinases in the Human genome off-target inhibition is a significant problem. As the potency of lead compounds increase through iterative cycles of medicinal chemistry and structure based drug design it is important to identify off-target inhibition. To facilitate counter-screening by individual project biochemists routine robust automation of dose response curve kinase assays are required. In contrast to an HTS assay these automated assays are designed to provide high precision data for a small number of compounds for multiple kinases. This presentation will outline some of the robotic assay development solutions that have been implemented in the Biochemistry Group at Pfizer La Jolla.
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Biochemical Counter-Screening for Kinase
