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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