| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T50970 | ||||
| Target Name | Endothelin-converting enzyme 1 (ECE1) | ||||
| Type of Target |
Literature-reported |
||||
| Drug Potency against Target | LY-292223 | Drug Info | IC50 = 67 nM | [1] | |
| PO3 2-Ile-Trp-O-3K | Drug Info | IC50 = 2800 nM | |||
| PO3 2-Leu-Nal-O-3K | Drug Info | IC50 = 7400 nM | |||
| PO3 2-Leu-Trp-O-3K | Drug Info | IC50 = 960 nM | |||
| PO3 2-Nle-Trp-O-3K | Drug Info | IC50 = 1500 nM | |||
| SCH-54470 | Drug Info | IC50 = 80 nM | [2] | ||
| References | |||||
| REF 1 | Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells. J Med Chem. 2005 Jan 27;48(2):483-98. | ||||
| REF 2 | Phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1 inhibitors. J Med Chem. 2010 Jan 14;53(1):208-20. | ||||
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