Abstract
Potent and selective ligands for the human EP3 prostanoid receptor are described. Triaryl compounds bearing an ortho-substituted propionic acid moiety were identified as potent EP3 antagonists based on the SAR described herein. The binding affinities of key compound on all eight human prostanoid receptors is reported.
MeSH terms
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Animals
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Cell Line, Tumor
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Cyclic AMP / metabolism
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Humans
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Indicators and Reagents
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Kinetics
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Protein Conformation
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Rats
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Receptors, Prostaglandin E / drug effects*
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Receptors, Prostaglandin E, EP3 Subtype
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Structure-Activity Relationship
Substances
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Indicators and Reagents
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PTGER3 protein, human
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Receptors, Prostaglandin E
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Receptors, Prostaglandin E, EP3 Subtype
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Cyclic AMP