| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T15556 | ||||
| Target Name | Endothelial plasminogen activator inhibitor (SERPINE1) | ||||
| Type of Target |
Clinical trial |
||||
| Drug Potency against Target | AR-HO29953XX | Drug Info | IC50 = 17800 nM | [3] | |
| SIDEROXYLONAL A | Drug Info | IC50 = 3300 nM | [1] | ||
| SIDEROXYLONAL B | Drug Info | IC50 = 5300 nM | [1] | ||
| Sideroxylonal C | Drug Info | IC50 = 4700 nM | [1] | ||
| XR-5118 | Drug Info | IC50 = 8000 nM | [2] | ||
| References | |||||
| REF 1 | Sideroxylonal C, a new inhibitor of human plasminogen activator inhibitor type-1, from the flowers of Eucalyptus albens. J Nat Prod. 1999 Feb;62(2):324-6. | ||||
| REF 2 | Tiplaxtinin, a novel, orally efficacious inhibitor of plasminogen activator inhibitor-1: design, synthesis, and preclinical characterization. J Med Chem. 2004 Jul 1;47(14):3491-4. | ||||
| REF 3 | Synthesis and SAR of 2-carboxylic acid indoles as inhibitors of plasminogen activator inhibitor-1. Bioorg Med Chem Lett. 2005 Aug 1;15(15):3514-8. | ||||
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