Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T38529 | ||||
Target Name | Prostaglandin E2 receptor EP2 (PTGER2) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Iloprost | Drug Info | IC50 = 12.6 nM | [4] | |
3-(2-((E)-3-phenylprop-1-enyl)phenyl)acrylic acid | Drug Info | Ki = 1400 nM | [1] | ||
3-(2-(4-methoxycinnamyl)phenyl)acrylic acid | Drug Info | Ki = 2500 nM | [1] | ||
3-(2-(naphthalen-2-ylmethyl)phenyl)acrylic acid | Drug Info | Ki = 12000 nM | [1] | ||
3-(2-cinnamylphenyl)acrylic acid | Drug Info | Ki = 1400 nM | [1] | ||
BUTAPROST | Drug Info | Ki = 110 nM | [3] | ||
LAROPIPRANT | Drug Info | Ki = 136 nM | [2] | ||
References | |||||
REF 1 | Comparison between two classes of selective EP(3) antagonists and their biological activities. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5639-42. | ||||
REF 2 | Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydroc... J Med Chem. 2007 Feb 22;50(4):794-806. | ||||
REF 3 | Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist. Bioorg Med Chem Lett. 2008 Jan 15;18(2):821-4. | ||||
REF 4 | Investigation of the prostaglandin E (EP-) receptor subtype mediating relaxation of the rabbit jugular vein. Br J Pharmacol. 1992 Apr;105(4):817-24. | ||||
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