Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy

[Image: see text] Herein we present the outcome of a high throughput screening (HTS) campaign-based strategy for the rapid identification and optimization of selective and general chemotypes for both kappa (κ) opioid receptor (KOR) activation and inhibition. In this program, we have developed potent...

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Main Authors: Frankowski, Kevin J., Hedrick, Michael P., Gosalia, Palak, Li, Kelin, Shi, Shenghua, Whipple, David, Ghosh, Partha, Prisinzano, Thomas E., Schoenen, Frank J., Su, Ying, Vasile, S., Sergienko, Eduard, Gray, Wilson, Hariharan, Santosh, Milan, Loribelle, Heynen-Genel, Susanne, Mangravita-Novo, Arianna, Vicchiarelli, Michael, Smith, Layton H., Streicher, John M., Caron, Marc G., Barak, Lawrence S., Bohn, Laura M., Chung, Thomas D. Y., Aubé, Jeffrey
Formato: Artigo
Idioma:Inglês
Publicado: American Chemical Society 2012
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC3378255/
https://ncbi.nlm.nih.gov/pubmed/22737280
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/cn200128x
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