PubMed · 12547014
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Stanley S Davis. 2002-12-01. Parenteral polymers.. https://doi.org/10.1016/s1359-6446(02)02517-5
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The synthesis and abl tyrosine kinase inhibitory activities of alkyltriazenes conjugated to phenylaminopyrimidines are described. Significant abl inhibitory activities were observed only when a benzamido spacer was inserted between the 1,2,3-triazene chain and the 2-phenyaminopyridopyrimidine moiety.
NMR-based ligand screening is now an established field in its own right. In recent years, advances in both methodology and hardware have broadened its range of applications and pushed back practical limitations, leading to the growing importance of NMR screening as a tool in industrial drug research. An overview of new screening methods and applications is presented here, and ways in which NMR-screening is being used in cooperation with other screening techniques are discussed.
The dominance of G protein-coupled receptors (GPCRs) as a drug target class, coupled with the increased pace of target identification and expansion of compound libraries, presents a compelling need to develop technologies to screen multiple GPCRs simultaneously. To address this need, GPCR microarrays that require the co-immobilization of lipid molecules and the probe receptors of interest have been fabricated, using conventional robotic printing technologies. Assays to screen compounds for their pharmacological properties (binding affinity, relative potency and selectivity) using GPCR microarrays are discussed.