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 529174Bioorg 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 528393Bioorg 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 528393Bioorg 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 528393Bioorg 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 528393Bioorg 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 552371Investigation of the prostaglandin E (EP-) receptor subtype mediating relaxation of the rabbit jugular vein. Br J Pharmacol. 1992 Apr;105(4):817-24.
Ref 528672J 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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