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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