Target Validation Information
Target ID T82577
Target Name Angiotensin-converting enzyme
Target Type
Successful
Drug Potency against Target LY-292223 Drug Info IC50 = 13400 nM [527383]
Lisinopril Drug Info IC50 = 3.3 nM [553114]
Spirapril Drug Info IC50 = 0.81 nM [553138]
Ramipril Drug Info IC50 = 4.0 nM [553114]
Perindopril Drug Info IC50 = 1.11 ng/mL [552368]
Omapatrilat Drug Info Ki = 5 nM [553251]
Rescinnamine Drug Info IC50 = 1530 nM [552791]
Quinapril Drug Info IC50 = 8.3 nM [553164]
Moexipril Drug Info IC50 = 165 nM [553173]
Trandolapril Drug Info IC50 = 1.7 nM [552376]
Fosinopril Drug Info IC50 = 55000 nM [552268]
Captopril Drug Info IC50 = 22 nM [552209]
BUTEIN Drug Info IC50 = 730 nM [530737]
Cilazapril Drug Info IC50 = 1.93 nM [553114]
RIP Drug Info IC50 = 12000 nM [533492]
N-Carboxymethyl-N-cyclopentyl-phthalamic acid Drug Info IC50 = 0.1 nM [533393]
SQ-26332 Drug Info IC50 = 30 nM [527799]
[Cyclopentyl-(2-nitro-benzoyl)-amino]-acetic acid Drug Info IC50 = 0.1 nM [533393]
Enalapril Drug Info IC50 = 240 nM [553175]
Enalaprilat Drug Info IC50 = 3.12 nM [553114]
SCH-54470 Drug Info IC50 = 2.5 nM [530505]
Action against Disease Model Enalapril An oral dose of 0.1 mg kg-1 cilazapril evoked the same maxim uM degree of plasma ACE inhibition (approximately 76%) in the rat as 0.25 mg kg-1 enalapril. Cilazapril (0.25 mg kg-1 p.o.) inhibited plasma ACE by greater than 95%. The rate of recovery of ACE activity was slower with cilazapril (5-6% h-1) than with enalapril (10% h-1).In anaesthetised rats cilazaprilat was equipotent with ramiprilat and slightly more potent (1.5x) than enalaprilat as an inhibitor of the angiotensin I pressor response.Following oral administration to conscious rats and intravenous administration to anaesthetised dogs, cilazapril was 2-4.5x more potent than enalapril as an ACE inhibitor. [553114] Drug Info
References
Ref 527383J Med Chem. 2005 Jan 27;48(2):483-98.Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells.
Ref 553114A review of the preclinical cardiovascular pharmacology of cilazapril, a new angiotensin converting enzyme inhibitor. Br J Clin Pharmacol. 1989;27 Suppl 2:139S-150S.
Ref 553138Angiotensin converting enzyme inhibitory activity of SCH 33844 (spirapril) in rats, dogs and monkeys. Arch Int Pharmacodyn Ther. 1987 Apr;286(2):216-29.
Ref 553114A review of the preclinical cardiovascular pharmacology of cilazapril, a new angiotensin converting enzyme inhibitor. Br J Clin Pharmacol. 1989;27 Suppl 2:139S-150S.
Ref 552368The pharmacokinetics of perindopril and its effects on serum angiotensin converting enzyme activity in hypertensive patients with chronic renal failure. Br J Clin Pharmacol. 1992 Jan;33(1):93-9.
Ref 553251Dual metalloprotease inhibitors: mercaptoacetyl-based fused heterocyclic dipeptide mimetics as inhibitors of angiotensin-converting enzyme and neutral endopeptidase. J Med Chem. 1997 May 23;40(11):1570-7.
Ref 552791High-throughput screening for daunorubicin-mediated drug resistance identifies mometasone furoate as a novel ABCB1-reversal agent. J Biomol Screen. 2008 Mar;13(3):185-93. doi: 10.1177/1087057108314610. Epub 2008 Feb 29.
Ref 553164CI-906 and CI-907: new orally active nonsulfhydryl angiotensin-converting enzyme inhibitors. Fed Proc. 1984 Apr;43(5):1326-9.
Ref 553173Moexipril, a new angiotensin-converting enzyme (ACE) inhibitor: pharmacological characterization and comparison with enalapril. J Pharmacol Exp Ther. 1995 Nov;275(2):854-63.
Ref 553114A review of the preclinical cardiovascular pharmacology of cilazapril, a new angiotensin converting enzyme inhibitor. Br J Clin Pharmacol. 1989;27 Suppl 2:139S-150S.
Ref 552376Trandolapril in hypertension: overview of a new angiotensin-converting enzyme inhibitor. Am J Cardiol. 1992 Oct 29;70(12):27D-34D.
Ref 552268Mechanism of intestinal absorption and renal reabsorption of an orally active ace inhibitor: uptake and transport of fosinopril in cell cultures. Drug Metab Dispos. 2001 Oct;29(10):1307-15.
Ref 552209LKPNM: a prodrug-type ACE-inhibitory peptide derived from fish protein. Immunopharmacology. 1999 Oct 15;44(1-2):123-7.
Ref 530737Bioorg Med Chem Lett. 2010 Mar 15;20(6):1990-3. Epub 2010 Jan 25.The synthesis and angiotensin converting enzyme (ACE) inhibitory activity of chalcones and their pyrazole derivatives.
Ref 553114A review of the preclinical cardiovascular pharmacology of cilazapril, a new angiotensin converting enzyme inhibitor. Br J Clin Pharmacol. 1989;27 Suppl 2:139S-150S.
Ref 533492J Med Chem. 1985 Nov;28(11):1553-5.Difluorostatine- and difluorostatone-containing peptides as potent and specific renin inhibitors.
Ref 533393J Med Chem. 1985 Mar;28(3):328-32.Angiotensin converting enzyme inhibitors. (Mercaptoaroyl)amino acids.
Ref 527799J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
Ref 533393J Med Chem. 1985 Mar;28(3):328-32.Angiotensin converting enzyme inhibitors. (Mercaptoaroyl)amino acids.
Ref 553175Compared properties of trandolapril, enalapril, and their diacid metabolites. J Cardiovasc Pharmacol. 1994;23 Suppl 4:S11-5.
Ref 553114A review of the preclinical cardiovascular pharmacology of cilazapril, a new angiotensin converting enzyme inhibitor. Br J Clin Pharmacol. 1989;27 Suppl 2:139S-150S.
Ref 530505J Med Chem. 2010 Jan 14;53(1):208-20.Phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1 inhibitors.

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