Target Information
| Target General Information | Top | |||||
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| Target ID |
T70071
(Former ID: TTDR00416)
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| Target Name |
Endothelin-converting enzyme (ECE)
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| Synonyms |
Endothelin converting enzyme
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| Gene Name |
NO-GeName
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 3 Target-related Diseases | + | ||||
| 1 | Heart failure [ICD-11: BD10-BD1Z] | |||||
| 2 | Intracranial injury [ICD-11: NA07] | |||||
| 3 | Cardiovascular disease [ICD-11: BA00-BE2Z] | |||||
| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 3 Clinical Trial Drugs | + | ||||
| 1 | SLV 306 | Drug Info | Phase 2 | Acute decompensated heart failure | [2], [3] | |
| 2 | SLV-334 | Drug Info | Phase 2 | Brain injury | [1] | |
| 3 | SLV-338 | Drug Info | Phase 1 | Cardiovascular disease | [4] | |
| Discontinued Drug(s) | [+] 2 Discontinued Drugs | + | ||||
| 1 | SM-19712 | Drug Info | Terminated | Hypertension | [5], [6] | |
| 2 | WS-75624B | Drug Info | Terminated | Cardiovascular disease | [7] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Modulator | [+] 4 Modulator drugs | + | ||||
| 1 | SLV 306 | Drug Info | [1] | |||
| 2 | SLV-334 | Drug Info | [8] | |||
| 3 | SLV-338 | Drug Info | [4], [9] | |||
| 4 | WS-75624B | Drug Info | [1], [11] | |||
| Inhibitor | [+] 2 Inhibitor drugs | + | ||||
| 1 | SM-19712 | Drug Info | [1], [10] | |||
| 2 | Phosphoramidon | Drug Info | [12] | |||
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| References | Top | |||||
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| REF 1 | The dual endothelin converting enzyme/neutral endopeptidase inhibitor SLV-306 (daglutril), inhibits systemic conversion of big endothelin-1 in humans. Life Sci. 2012 Oct 15;91(13-14):743-8. | |||||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6506). | |||||
| REF 3 | ClinicalTrials.gov (NCT00160225) Study to Evaluate the Efficacy and Safety of Daglutril Compared to Placebo on Top of Losartan in Type 2 Diabetics With Overt Nephropathy and Well Controlled Hypertension. U.S. National Institutes of Health. | |||||
| REF 4 | Renoprotective effects of combined endothelin-converting enzyme/neutral endopeptidase inhibitor SLV338 in acute and chronic experimental renal damage. Clin Lab. 2011;57(7-8):507-15. | |||||
| REF 5 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5272). | |||||
| REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015442) | |||||
| REF 7 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006851) | |||||
| REF 8 | Clinical trials in traumatic brain injury: past experience and current developments.Neurotherapeutics.2010 Jan;7(1):115-26. | |||||
| REF 9 | Endothelin-converting enzyme/neutral endopeptidase inhibitor SLV338 prevents hypertensive cardiac remodeling in a blood pressure-independent manner.Hypertension.2011 Apr;57(4):755-63. | |||||
| REF 10 | Protective effect of SM-19712, a novel and potent endothelin converting enzyme inhibitor, on ischemic acute renal failure in rats. Jpn J Pharmacol. 2000 Sep;84(1):16-24. | |||||
| REF 11 | WS75624 A and B, new endothelin converting enzyme inhibitors isolated from Saccharothrix sp. No. 75624. II. Structure elucidation of WS75624 A and B. J Antibiot (Tokyo). 1995 Oct;48(10):1073-5. | |||||
| REF 12 | In vitro enzymatic processing of radiolabelled big ET-1 in human kidney. Biochem Pharmacol. 1998 Mar 1;55(5):697-701. | |||||
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