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Literature summary for 3.4.24.71 extracted from
- Endothelin-converting enzyme inhibitors: their application in cardiovascular diseases (2008), Rev. Port. Cardiol., 27, 385-408.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | analysis of effect of various ECE inhibitors in myocardial infarction, pulmonary hypertension, arterial hypertension. Overview is given on human studies | Homo sapiens |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| COS-1 cell membrane with overexpression of human ECE-1 | Homo sapiens |
| COS-1 cell membrane with overexpression of human ECE-1 | Sus scrofa |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| CGS 26303 | synthetic inhibitor, ECE-1/NEP inhibitor | Homo sapiens |  |
| CGS 26303 | synthetic inhibitor, ECE-1/NEP inhibitor | Sus scrofa | |
| CGS 26582 | synthetic inhibitor, ECE/NEP/ACE inhibitor | Sus scrofa | |
| CGS 34043 | synthetic inhibitor, ECE-1/NEP inhibitor | Homo sapiens | |
| CGS 34226 | synthetic inhibitor, ECE-1/NEP inhibitor | Homo sapiens | |
| CGS 35066 | synthetic inhibitor, selective ECE-1 inhibitor | Homo sapiens | |
| CGS 35601 | synthetic inhibitor, ECE/NEP/ACE inhibitor | Homo sapiens | |
| N-(alpha-rhamnopyranosyloxyhydroxyphosphinyl)-Leu-Trp | phosphoramidon, synthetic inhibitor, ECE-1/NEP inhibitor | Sus scrofa | |
| RO 67-7447 | synthetic inhibitor, selective ECE-1 inhibitor | Rattus norvegicus | |
| SCH 54470 | synthetic inhibitor, ECE/NEP/ACE inhibitor | Cavia sp. | |
| SLV-306 | KC-12792, synthetic inhibitor, ECE-1/NEP inhibitor, clinical trial for treatment of arterial hypertension and heart failure in human | Homo sapiens | |
| SM-19712 | synthetic inhibitor, selective ECE-1 inhibitor | Sus scrofa | |
| WS-79089B | natural inhibitor, selective ECE-1 inhibitor | Bos taurus | |
| WS75624A | natural inhibitor, selective ECE-1 inhibitor | Bos taurus | |
| WS79089A | natural inhibitor, selective ECE-1 inhibitor | Bos taurus | |
| WS79089C | natural inhibitor, selective ECE-1 inhibitor | Bos taurus | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Zn2+ | - |
Homo sapiens | |
| Zn2+ | - |
Rattus norvegicus | |
| Zn2+ | - |
Sus scrofa | |
| Zn2+ | - |
Cavia sp. | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Bos taurus | - |
- |
- |
| Cavia sp. | - |
- |
- |
| Homo sapiens | - |
- |
- |
| Rattus norvegicus | - |
- |
- |
| Sus scrofa | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| aortic endothelial cell | - |
Sus scrofa | - |
| carotid artery endothelial cell | - |
Bos taurus | - |
| kidney | - |
Rattus norvegicus | - |
| left ventricle | - |
Rattus norvegicus | - |
| pleura | - |
Cavia sp. | - |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| ECE-1 | - |
Homo sapiens |
| ECE-1 | - |
Rattus norvegicus |
| ECE-1 | - |
Sus scrofa |
| ECE-1 | - |
Bos taurus |
| ECE-1 | - |
Cavia sp. |
| endothelin-converting enzyme-1 | - |
Homo sapiens |
| endothelin-converting enzyme-1 | - |
Rattus norvegicus |
| endothelin-converting enzyme-1 | - |
Sus scrofa |
| endothelin-converting enzyme-1 | - |
Bos taurus |
| endothelin-converting enzyme-1 | - |
Cavia sp. |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000012 | - |
- |
Rattus norvegicus | RO 67-7447 | |
| 0.0000058 | - |
human recombinant ECE-1 overexpressed in CHO cells | Homo sapiens | CGS 34043 | |
| 0.000011 | - |
human recombinant ECE-1 overexpressed in CHO cells | Homo sapiens | CGS 34226 | |
| 0.000017 | - |
optimized form of inhibitor, human recombinant ECE-1 overexpressed in CHO cells | Homo sapiens | CGS 26303 | |
| 0.000022 | - |
COS-1 cell membrane with overexpression of human ECE-1 | Homo sapiens | CGS 35066 | |
| 0.000042 | - |
in vitro result, in vivo potency is lower than expected compared to in vitro result | Sus scrofa | SM-19712 | |
| 0.000055 | - |
- |
Homo sapiens | CGS 35601 | |
| 0.00008 | - |
- |
Cavia sp. | SCH 54470 | |
| 0.00014 | - |
- |
Bos taurus | WS-79089B | |
| 0.00062 | - |
- |
Sus scrofa | CGS 26582 | |
| 0.00073 | - |
- |
Bos taurus | WS79089A | |
| 0.0011 | - |
long-active in vivo | Sus scrofa | CGS 26303 | |
| 0.00342 | - |
- |
Bos taurus | WS79089C | |
| 0.0035 | - |
potency varies with pH of medium | Sus scrofa | N-(alpha-rhamnopyranosyloxyhydroxyphosphinyl)-Leu-Trp | |
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