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Structure-activity relationship of triaryl propionic acid analogues on the human EP3 prostanoid receptor |
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| Authors: | Gallant Michel Belley Michel Carrière Marie-Claude Chateauneuf Anne Denis Danielle Lachance Nicolas Lamontagne Sonia Metters Kathleen M Sawyer Nicole Slipetz Deborah Truchon Jean François Labelle Marc |
| Affiliation: | Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe Claire-Dorval, Québec, Canada H9R 4P8. michel_gallant@merck.com |
| 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. |
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