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American Chemical Society, Journal of Medicinal Chemistry, 14(52), p. 4543-4547, 2009

DOI: 10.1021/jm9002582

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Allosteric Modulators of the Adenosine A(1) Receptor: Synthesis and Pharmacological Evaluation of 4-Substituted 2-Amino-3-benzoylthiophenes

Journal article published in 2009 by Luigi Aurelio, Celine Valant ORCID, Bernard Luke Flynn, Patrick M. Sexton, Arthur Christopoulos, Peter John Scammells ORCID
This paper is available in a repository.
This paper is available in a repository.

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Abstract

A series of 4-substituted 2-amino-3-benzoylthiophenes was screened using a functional assay of A(1)AR-mediated phosphorylation of ERK1/2 in intact CHO cells to identify both potential agonistic effects as well the ability to allosterically modulate the activity of the orthosteric agonist, R-PIA. More detailed concentration-response experiments were subsequently performed on two compounds (9a and 9o) utilizing both the ERK1/2 assay as well as a second assay of [(35)S]GTPgammaS binding to activated G proteins.