Target Validation Information
Target ID T61622
Target Name Renin, renal
Target Type
Successful
Drug Potency against Target Pro-His-Pro-Phe-His-Leu(CH2NH)Val-Ile-His-Lys Drug Info IC50 = 10 nM [533426]
CP-305202 Drug Info IC50 = 39 nM [531120]
(H-261)Boc-His-Pro-Phe-His-Leu(OH)-Val-Ile-His-OH Drug Info IC50 = 0.7 nM [533442]
Iva-His-Pro-Phe-His-AHPPA-Leu-Phe-NH2 Drug Info IC50 = 2.2 nM [533493]
Pro-His-Pro-His-Leu-Phe-Val-Tyr Drug Info Ki = 4000 nM [533536]
PP2-Pro-Phe-N-MeHis-LVA-Ile-Amp-(O) Drug Info IC50 = 1.9 nM [530554]
PP1-Pro-Phe-N-MeHis-LVA-Ile-Amp-(O) Drug Info IC50 = 2.5 nM [530554]
Iva-His-Pro-Phe-His-ACHPA-Leu-Phe-NH2 Drug Info IC50 = 0.17 nM [533493]
Iva-His-Pro-Phe-His-Sta-Leu-Phe-NH2 Drug Info IC50 = 13 nM [533493]
Sul-Pro-Phe-N-MeHis-LVA-Ile-Amp-(O) Drug Info IC50 = 0.31 nM [530554]
Glu-Trp-Pro-Arg-Pro-Gln-Ile-Pro-Pro Drug Info Ki = 800 nM [533536]
Pro-His-Pro-His-Phe-Phe-Val-Tyr-Lys Drug Info Ki = 2000 nM [533536]
Pro-His-Pro-His-Phe-Phe-Val-Tyr Drug Info Ki = 1000 nM [533536]
ZANKIREN Drug Info IC50 = 1.1 nM [530066]
Sul-Pro-Phe-N-MeHis-LVA-Ile-Amp Drug Info IC50 = 1.8 nM [530554]
References
Ref 533426J Med Chem. 1988 Sep;31(9):1839-46.Synthesis and biological activity of some transition-state inhibitors of human renin.
Ref 531120J Med Chem. 2010 Nov 11;53(21):7490-520.Direct renin inhibitors as a new therapy for hypertension.
Ref 533442J Med Chem. 1987 Oct;30(10):1729-37.Renin inhibitors. Dipeptide analogues of angiotensinogen incorporating transition-state, nonpeptidic replacements at the scissile bond.
Ref 533493J Med Chem. 1985 Dec;28(12):1779-90.Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analogue inhibitors containing a novel analogue of statine.
Ref 533536J Med Chem. 1981 Apr;24(4):355-61.Inhibition of the renin-angiotensin system. A new approach to the therapy of hypertension.
Ref 530554J Med Chem. 1991 Feb;34(2):633-42.Renin inhibitory peptides. Incorporation of polar, hydrophilic end groups into an active renin inhibitory peptide template and their evaluation in a human renin infused rat model and in conscious sodium-depleted monkeys.
Ref 530554J Med Chem. 1991 Feb;34(2):633-42.Renin inhibitory peptides. Incorporation of polar, hydrophilic end groups into an active renin inhibitory peptide template and their evaluation in a human renin infused rat model and in conscious sodium-depleted monkeys.
Ref 533493J Med Chem. 1985 Dec;28(12):1779-90.Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analogue inhibitors containing a novel analogue of statine.
Ref 533493J Med Chem. 1985 Dec;28(12):1779-90.Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analogue inhibitors containing a novel analogue of statine.
Ref 530554J Med Chem. 1991 Feb;34(2):633-42.Renin inhibitory peptides. Incorporation of polar, hydrophilic end groups into an active renin inhibitory peptide template and their evaluation in a human renin infused rat model and in conscious sodium-depleted monkeys.
Ref 533536J Med Chem. 1981 Apr;24(4):355-61.Inhibition of the renin-angiotensin system. A new approach to the therapy of hypertension.
Ref 533536J Med Chem. 1981 Apr;24(4):355-61.Inhibition of the renin-angiotensin system. A new approach to the therapy of hypertension.
Ref 533536J Med Chem. 1981 Apr;24(4):355-61.Inhibition of the renin-angiotensin system. A new approach to the therapy of hypertension.
Ref 530066J Med Chem. 2009 Jun 25;52(12):3689-702.Design and preparation of potent, nonpeptidic, bioavailable renin inhibitors.
Ref 530554J Med Chem. 1991 Feb;34(2):633-42.Renin inhibitory peptides. Incorporation of polar, hydrophilic end groups into an active renin inhibitory peptide template and their evaluation in a human renin infused rat model and in conscious sodium-depleted monkeys.

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