| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T61622 | ||||
| Target Name | Angiotensinogenase renin (REN) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | (H-261)Boc-His-Pro-Phe-His-Leu(OH)-Val-Ile-His-OH | Drug Info | IC50 = 0.7 nM | [5] | |
| CP-305202 | Drug Info | IC50 = 39 nM | [3] | ||
| Glu-Trp-Pro-Arg-Pro-Gln-Ile-Pro-Pro | Drug Info | Ki = 800 nM | [7] | ||
| Iva-His-Pro-Phe-His-ACHPA-Leu-Phe-NH2 | Drug Info | IC50 = 0.17 nM | [6] | ||
| Iva-His-Pro-Phe-His-AHPPA-Leu-Phe-NH2 | Drug Info | IC50 = 2.2 nM | [6] | ||
| Iva-His-Pro-Phe-His-Sta-Leu-Phe-NH2 | Drug Info | IC50 = 13 nM | [6] | ||
| PP1-Pro-Phe-N-MeHis-LVA-Ile-Amp-(O) | Drug Info | IC50 = 2.5 nM | [2] | ||
| PP2-Pro-Phe-N-MeHis-LVA-Ile-Amp-(O) | Drug Info | IC50 = 1.9 nM | [2] | ||
| Pro-His-Pro-His-Leu-Phe-Val-Tyr | Drug Info | Ki = 4000 nM | [7] | ||
| Pro-His-Pro-His-Phe-Phe-Val-Tyr | Drug Info | Ki = 1000 nM | [7] | ||
| Pro-His-Pro-His-Phe-Phe-Val-Tyr-Lys | Drug Info | Ki = 2000 nM | [7] | ||
| Pro-His-Pro-Phe-His-Leu(CH2NH)Val-Ile-His-Lys | Drug Info | IC50 = 10 nM | [4] | ||
| Sul-Pro-Phe-N-MeHis-LVA-Ile-Amp | Drug Info | IC50 = 1.8 nM | [2] | ||
| Sul-Pro-Phe-N-MeHis-LVA-Ile-Amp-(O) | Drug Info | IC50 = 0.31 nM | [2] | ||
| ZANKIREN | Drug Info | IC50 = 1.1 nM | [1] | ||
| References | |||||
| REF 1 | Design and preparation of potent, nonpeptidic, bioavailable renin inhibitors. J Med Chem. 2009 Jun 25;52(12):3689-702. | ||||
| REF 2 | Renin inhibitory peptides. Incorporation of polar, hydrophilic end groups into an active renin inhibitory peptide template and their evaluation in ... J Med Chem. 1991 Feb;34(2):633-42. | ||||
| REF 3 | Direct renin inhibitors as a new therapy for hypertension. J Med Chem. 2010 Nov 11;53(21):7490-520. | ||||
| REF 4 | Synthesis and biological activity of some transition-state inhibitors of human renin. J Med Chem. 1988 Sep;31(9):1839-46. | ||||
| REF 5 | Renin inhibitors. Dipeptide analogues of angiotensinogen incorporating transition-state, nonpeptidic replacements at the scissile bond. J Med Chem. 1987 Oct;30(10):1729-37. | ||||
| REF 6 | Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analogue inhibitors containing a novel analogue of statine. J Med Chem. 1985 Dec;28(12):1779-90. | ||||
| REF 7 | Inhibition of the renin-angiotensin system. A new approach to the therapy of hypertension. J Med Chem. 1981 Apr;24(4):355-61. | ||||
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