Target Validation Information
TTD ID T82577
Target Name Angiotensin-converting enzyme (ACE)
Type of Target
Successful
Drug Potency against Target Captopril Drug Info IC50 = 22 nM [7]
Cilazapril Drug Info IC50 = 1.93 nM [12]
Enalapril Drug Info IC50 = 240 nM [16]
Enalaprilat Drug Info IC50 = 3.12 nM [12]
Fosinopril Drug Info IC50 = 55000 nM [8]
Lisinopril Drug Info IC50 = 3.3 nM [12]
Moexipril Drug Info IC50 = 165 nM [15]
Perindopril Drug Info IC50 = 1.11 ng/mL [9]
Quinapril Drug Info IC50 = 8.3 nM [14]
Ramipril Drug Info IC50 = 4.0 nM [12]
Rescinnamine Drug Info IC50 = 1530 nM [11]
Spirapril Drug Info IC50 = 0.81 nM [13]
Trandolapril Drug Info IC50 = 1.7 nM [10]
Omapatrilat Drug Info Ki = 5 nM [17]
BUTEIN Drug Info IC50 = 730 nM [4]
LY-292223 Drug Info IC50 = 13400 nM [1]
N-Carboxymethyl-N-cyclopentyl-phthalamic acid Drug Info IC50 = 0.1 nM [5]
RIP Drug Info IC50 = 12000 nM [6]
SCH-54470 Drug Info IC50 = 2.5 nM [3]
SQ-26332 Drug Info IC50 = 30 nM [2]
[Cyclopentyl-(2-nitro-benzoyl)-amino]-acetic acid Drug Info IC50 = 0.1 nM [5]
Action against Disease Model Enalapril Drug Info 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. [12]
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 Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
REF 3 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.
REF 4 The synthesis and angiotensin converting enzyme (ACE) inhibitory activity of chalcones and their pyrazole derivatives. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1990-3.
REF 5 Angiotensin converting enzyme inhibitors. (Mercaptoaroyl)amino acids. J Med Chem. 1985 Mar;28(3):328-32.
REF 6 Difluorostatine- and difluorostatone-containing peptides as potent and specific renin inhibitors. J Med Chem. 1985 Nov;28(11):1553-5.
REF 7 LKPNM: a prodrug-type ACE-inhibitory peptide derived from fish protein. Immunopharmacology. 1999 Oct 15;44(1-2):123-7.
REF 8 Mechanism 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 9 The 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 10 Trandolapril in hypertension: overview of a new angiotensin-converting enzyme inhibitor. Am J Cardiol. 1992 Oct 29;70(12):27D-34D.
REF 11 High-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.
REF 12 A 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 13 Angiotensin converting enzyme inhibitory activity of SCH 33844 (spirapril) in rats, dogs and monkeys. Arch Int Pharmacodyn Ther. 1987 Apr;286(2):216-29.
REF 14 CI-906 and CI-907: new orally active nonsulfhydryl angiotensin-converting enzyme inhibitors. Fed Proc. 1984 Apr;43(5):1326-9.
REF 15 Moexipril, a new angiotensin-converting enzyme (ACE) inhibitor: pharmacological characterization and comparison with enalapril. J Pharmacol Exp Ther. 1995 Nov;275(2):854-63.
REF 16 Compared properties of trandolapril, enalapril, and their diacid metabolites. J Cardiovasc Pharmacol. 1994;23 Suppl 4:S11-5.
REF 17 Dual 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.

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