| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T99954 | ||||
| Target Name | Prostacyclin receptor | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | FR-193262 | Drug Info | Ki = 12 nM | [527580] | |
| FR-181157 | Drug Info | IC50 = 1200 nM | [528308] | ||
| Misoprostol | Drug Info | IC50 = 6.17 nM | [552371] | ||
| LAROPIPRANT | Drug Info | Ki = 6628 nM | [528672] | ||
| AP-227 | Drug Info | IC50 = 150 nM | |||
| Epoprostenol | Drug Info | Kd = 16 nM | [553165] | ||
| Treprostinil | Drug Info | EC50 = 8.2 nM | [552969] | ||
| References | |||||
| Ref 527580 | Bioorg Med Chem Lett. 2005 Jul 1;15(13):3279-83.Discovery of new diphenyloxazole derivatives containing a pyrrolidine ring: orally active prostacyclin mimetics. Part 2. | ||||
| Ref 528308 | Bioorg Med Chem Lett. 2006 Sep 15;16(18):4861-4. Epub 2006 Jul 11.Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6. | ||||
| 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). | ||||
| Ref 553165 | 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. | ||||
| Ref 552969 | A review of prostaglandin analogs in the management of patients with pulmonary arterial hypertension. Respir Med. 2010 Jan;104(1):9-21. doi: 10.1016/j.rmed.2009.07.015. Epub 2009 Aug 15. | ||||
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