| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T38529 | ||||
| Target Name | Prostaglandin E2receptor, EP2 subtype | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | BUTAPROST | Drug Info | Ki = 110 nM | [529174] | |
| 3-(2-((E)-3-phenylprop-1-enyl)phenyl)acrylic acid | Drug Info | Ki = 1400 nM | [528393] | ||
| 3-(2-(naphthalen-2-ylmethyl)phenyl)acrylic acid | Drug Info | Ki = 12000 nM | [528393] | ||
| 3-(2-cinnamylphenyl)acrylic acid | Drug Info | Ki = 1400 nM | [528393] | ||
| 3-(2-(4-methoxycinnamyl)phenyl)acrylic acid | Drug Info | Ki = 2500 nM | [528393] | ||
| Iloprost | Drug Info | IC50 = 12.6 nM | [552371] | ||
| LAROPIPRANT | Drug Info | Ki = 136 nM | [528672] | ||
| References | |||||
| Ref 529174 | Bioorg Med Chem Lett. 2008 Jan 15;18(2):821-4. Epub 2007 Nov 13.Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist. | ||||
| Ref 528393 | Bioorg Med Chem Lett. 2006 Nov 1;16(21):5639-42. Epub 2006 Aug 22.Comparison between two classes of selective EP(3) antagonists and their biological activities. | ||||
| Ref 528393 | Bioorg Med Chem Lett. 2006 Nov 1;16(21):5639-42. Epub 2006 Aug 22.Comparison between two classes of selective EP(3) antagonists and their biological activities. | ||||
| Ref 528393 | Bioorg Med Chem Lett. 2006 Nov 1;16(21):5639-42. Epub 2006 Aug 22.Comparison between two classes of selective EP(3) antagonists and their biological activities. | ||||
| Ref 528393 | Bioorg Med Chem Lett. 2006 Nov 1;16(21):5639-42. Epub 2006 Aug 22.Comparison between two classes of selective EP(3) antagonists and their biological activities. | ||||
| Ref 552371 | Investigation of the prostaglandin E (EP-) receptor subtype mediating relaxation of the rabbit jugular vein. Br J Pharmacol. 1992 Apr;105(4):817-24. | ||||
| Ref 528672 | J Med Chem. 2007 Feb 22;50(4):794-806.Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524). | ||||
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