Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 14, Pages 4543-4547Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm9002582
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A series of 4-substituted 2-amino-3-benzoylthiophenes was screened using a functional assay of A A(1)AR-mediated phosphorylation of ERK 1/2 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 ERK 1/2 assay as well as a second assay of [S-35]GTP gamma S binding to activated G proteins.
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