Target Validation Information
TTD ID T99954
Target Name Prostacyclin receptor (PTGIR)
Type of Target
Successful
Drug Potency against Target Epoprostenol Drug Info Kd = 16 nM [6]
Misoprostol Drug Info IC50 = 6.17 nM [4]
Treprostinil Drug Info EC50 = 8.2 nM [5]
AP-227 Drug Info IC50 = 150 nM
FR-181157 Drug Info IC50 = 1200 nM [2]
FR-193262 Drug Info Ki = 12 nM [1]
LAROPIPRANT Drug Info Ki = 6628 nM [3]
References
REF 1 Discovery of new diphenyloxazole derivatives containing a pyrrolidine ring: orally active prostacyclin mimetics. Part 2. Bioorg Med Chem Lett. 2005 Jul 1;15(13):3279-83.
REF 2 Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4861-4.
REF 3 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 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.
REF 5 A review of prostaglandin analogs in the management of patients with pulmonary arterial hypertension. Respir Med. 2010 Jan;104(1):9-21.
REF 6 Epoprostenol (prostacyclin, PGI2) binding and activation of adenylate cyclase in platelets of diabetic and control subjects. Br J Clin Pharmacol. 1983 Jan;15(1):77-81.

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