3.4.24.71: endothelin-converting enzyme 1
This is an abbreviated version!
For detailed information about endothelin-converting enzyme 1, go to the full flat file.
Word Map on EC 3.4.24.71
-
3.4.24.71
-
endothelins
-
phosphoramidon
-
artery
-
vasoconstrictor
-
endopeptidase
-
cardiovascular
-
hypertension
-
cardiac
-
pulmonary
-
angiotensin
-
neprilysin
-
tone
-
vasoactive
-
metalloprotease
-
vessel
-
coronary
-
phosphoramidon-sensitive
-
metallopeptidases
-
contractile
-
preproet-1
-
vasospasm
-
thiorphan
-
atrial
-
natriuretic
-
pressor
-
ventricular
-
aortic
-
angiotensin-converting
-
preproendothelin-1
-
endothelium-derived
-
et-1-induced
-
insulin-degrading
-
drug development
-
baecs
-
hemodynamic
-
medicine
-
vasopeptidase
-
etb-receptors
-
3.4.24.11
-
metalloendopeptidase
-
subarachnoid
-
chymase
-
conscious
-
ednra
-
sarafotoxin
-
basilar
-
ppet-1
-
21-amino
-
prepro
-
enzyme-2
-
bosentan
-
et-1-mediated
- 3.4.24.71
- endothelins
- phosphoramidon
- artery
-
vasoconstrictor
- endopeptidase
- cardiovascular
- hypertension
- cardiac
- pulmonary
- angiotensin
- neprilysin
-
tone
-
vasoactive
- metalloprotease
- vessel
- coronary
-
phosphoramidon-sensitive
- metallopeptidases
-
contractile
-
preproet-1
- vasospasm
- thiorphan
-
atrial
-
natriuretic
-
pressor
- ventricular
- aortic
-
angiotensin-converting
- preproendothelin-1
-
endothelium-derived
-
et-1-induced
-
insulin-degrading
- drug development
-
baecs
-
hemodynamic
- medicine
-
vasopeptidase
-
etb-receptors
-
3.4.24.11
- metalloendopeptidase
-
subarachnoid
- chymase
-
conscious
-
ednra
- sarafotoxin
-
basilar
-
ppet-1
-
21-amino
-
prepro
- enzyme-2
- bosentan
-
et-1-mediated
Reaction
Hydrolysis of the -Trp21-/-Val- bond in big endothelin to form endothelin 1 =
Synonyms
ECE, ECE-1, ECE-1b, ECE-3, ECE1, endothelin converting enzyme, endothelin converting enzyme-1, Endothelin-converting enzyme, endothelin-converting enzyme 1, endothelin-converting enzyme 1 (ECE-1), endothelin-converting enzyme I, endothelin-converting enzyme-1, endothelin-converting-enzyme-1, ET converting enzyme, hECE-1, More, sECE, solECE-1
ECTree
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Inhibitors
Inhibitors on EC 3.4.24.71 - endothelin-converting enzyme 1
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(2R,3R,4R,5R)-(2S)-(4-[2-(1,3-dioxo-1H,3H-benzo[de]isoquinolin-2-yl)ethyl]-3-isobutyl-5-phosphonopyrrolidine-2-carbonyl-amino)-3-(1H-indol-3-yl)propionic acid
-
0.01 mM, 91% inhibition of enzyme activity
(2R,4S,5R,6R)-(2S)-(5-[2-(1,3-dioxo-1H,3H-benzo[de]isoquinolin-2-yl)ethyl]-4-isobutyl-6-phosphonopiperidine-2-carbonyl-amino)-3-(1H-indol-3-yl)propionic acid
-
0.01 mM, 98% inhibition of enzyme activity
(2S)-2-((3-[hydroxyl(2-phenyl-(1R)-1-([(benzyloxy)carbonyl]-amino)ethyl)phosphinyl]-(2R)-2-[(3-phenylisoxazol-5-yl)methyl]-1-oxopropyl)amino) 1H-Indole-3-propanoic acid
-
-
(2S)-2-((3-[hydroxyl(2-phenyl-(1R)-1-([(benzyloxy)carbonyl]-amino)ethyl)phosphinyl]-(2R)-2-[(3-phenylisoxazol-5-yl)methyl]-1-oxopropyl)amino)-3-(4-hydroxy-phenyl) propanoic acid
-
-
(2S)-2-((3-[hydroxyl(2-phenyl-(1R)-1-([(benzyloxy)carbonyl]-amino)ethyl)phosphinyl]-(2S)-2-[(3-phenylisoxazol-5-yl)methyl]-1-oxopropyl)amino) 1H-indole-3-propanoic acid
-
-
(2S)-2-((3-[hydroxyl(2-phenyl-(1R)-1-([(benzyloxy)carbonyl]-amino)ethyl)phosphinyl]-(2S)-2-[(3-phenylisoxazol-5-yl)methyl]-1-oxopropyl)amino)-3-(4-hydroxy-phenyl) propanoic acid
-
-
(2S)-2-((3-[hydroxyl(2-phenyl-(1R)-1-([(benzyloxy)carbonyl]amino)ethyl)phosphinyl]-(2R)-2-[(3-phenylisoxazol-5-yl)methyl]-1-oxopropyl)amino)-3-phenyl propanoic acid
-
-
(2S)-2-((3-[hydroxyl(2-phenyl-(1R)-1-([(benzyloxy)carbonyl]amino)ethyl)phosphinyl]-(2S)-2-[(3-phenylisoxazol-5-yl)methyl]-1-oxopropyl)amino)-3-phenyl propanoic acid
-
-
(2S)-2-([3-(1,1'-biphenyl)-2-([hydroxyl(2-phenyl-(1R)-1-([(benzyloxy)carbonyl]amino)ethyl)phosphinyl]methyl)-1-oxopropyl]-amino) 1H-indole-3-propanoic acid
-
-
(2S)-2-([3-(3'-[1,1'-biphenyl]-4''-yl-4',5'-dihydro-5'-isoxazolyl)-2-([hydroxyl(2-phenyl-(1R)-1-([(benzyloxy)carbonyl]amino)ethyl)-phosphinyl]methyl)-1-oxopropyl]amino) 1H-indole-3-propanoic acid
-
-
(2S,4R)-2-[(2,5-difluorobenzylamino)methyl]-4-mercaptopyrrolidine-1-carboxylic acid isopropyl ester
-
IC50: 0.00109 mM
(2S,4R)-2-[2-[[4-mercapto-1-(naphthalene-2-sulfonyl)-pyrrolidine-2-carbonyl]methylamino]acetylamino]-benzoic acid methyl ester
-
IC50: 0.01089 mM
(2S,4R)-4-acetylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo-[1,4]dioxin-5-yl ester
-
IC50: 0.0000765 mM
(2S,4R)-4-acetylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-1-carboxylic acid 2-methoxycarbonylphenylester
-
IC50: 0.0000215 mM
(2S,4R)-4-mercapto-1-(naphthalene-2-sulfonyl)pyrrolidine-2-carboxylic acid N-methyl-N-(4-methylphenylsulfonyl)hydrazide
-
IC50: 0.00253 mM
(2S,4R)-4-mercapto-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo[1,4]-dioxin-5-yl ester
-
IC50: 0.000137 mM
(2S,4R)-4-mercapto-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2-ethoxycarbonylphenylester
-
IC50: 0.000067 mM
(2S,4R)-5-[(2,5-difluorobenzylamino)methyl]-1-(5-propylpyrimidin-2-yl)pyrrolidine-3-thiol
-
IC50: 0.0000729 mM
(3R,5S)-1-(5-propylpyrimidin-2-yl)-5-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-3-thiol trifluoroacetate
-
IC50: 0.0000198 mM
(R,R)-5-[(2,4-difluorophenyl)-2-(3,3,3-trifluoro-2-methoxy-2-phenylpropionyl)amino]pent-4-ynoic acid methyl ester
-
-
(R,S)-5-[(2,4-difluorophenyl)-2-(3,3,3-trifluoro-2-methoxy-2-phenylpropionyl)amino]pent-4-ynoic acid methyl ester
-
-
(S)-2-[(tert-butoxycarbonyl)amino]-5-(2,4-difluorophenyl)pent-4-ynoic acid methyl ester
-
-
(S)-5-(2,4-difluorophenyl)-2-[[(dimethoxyphosphoryl)methyl]amino]pent-4-ynoic acid
-
-
(S)-5-(2,4-difluorophenyl)-2-[[(dimethoxyphosphoryl)methyl]amino]pent-4-ynoic acid methyl ester
-
-
(S)-[1-[(2-cyanoethyl)-1-H-tetrazol-5-yl]-4-(2-methoxyphenyl)but-3-ynyl]carbamic acid tert-butyl ester
-
-
(S)-[1-[(2-cyanoethyl)carbamoyl]-4-(2-methoxyphenyl)but-3-ynyl]carbamic acid tert-butyl ester
-
-
(S)-[[1-[[(2-biphenyl-4-ylethyl)-carbamoyl]-4-(2-fluorophenyl)but-3-ynyl]amino]methyl]phosphonic acid
-
-
(S)-[[[1-[1-(2-cyanoethyl)-1-H-tetrazol-5-yl]-4-(2-methoxyphenyl)but-3-ynyl]amino]methyl] phosphonic acid diphenyl ester
-
-
(S)-[[[[4-(2-methoxyphenyl)-1-H-tetrazol-5-yl]but-3-ynyl]amino]methyl] phosphonic acid
-
-
(S)-[[[[4-(2-methoxyphenyl)-1-H-tetrazol-5-yl]but-3-ynyl]amino]methyl] phosphonic acid diphenyl ester
-
-
(S,S)-2-[5-(2,4-difluorophenyl)-2-[[(dimethoxyphosphoryl)methyl]amino]pent-4-ynoyl]-4-methylpentanoic acid methyl ester
-
-
(S,S)-2-[[2-amino-5-(2-chlorophenyl)pent-4-ynoyl]amino]-4-methylpentanoic acid methyl ester
-
-
(S,S)-2-[[2-[(tert-butoxycarbonyl)amino]-5-(2-chlorophenyl)pent-4-ynoyl]-amino]-4-methylpentanoic acid methyl ester
-
-
(S,S)-2-[[2-[(tert-butoxycarbonyl)amino]pent-4-ynoyl]-amino]-4-methylpentanoic acid methyl ester
-
-
(S,S)-2-[[5-(2,4-difluorophenyl)-2-[(phosphonomethyl)amino]pent-4-ynoyl]amino]-4-methylpentanoic acid
-
-
(S,S)-2-[[5-(2-chlorophenyl)-2-[(phosphonomethyl)amino]pent-4-ynoyl]amino]-4-methylpentanoic acid
-
-
(S,S)-2-[[5-(2-chlorophenyl)-2-[[(dimethoxyphosphoryl)-methyl]amino]pent-4-ynoyl]amino]-4-methylpentanoic acid methyl ester
-
-
(S,S)-2-[[5-(2-fluorophenyl)-2-[(phosphonomethyl)-amino]pent-4-ynoyl]amino]-4-methyl pentanoic acid
-
-
(S,S)-2-[[5-(3-fluorophenyl)-2-[(phosphonomethyl)-amino]pent-4-ynoyl]amino]-4-methyl pentanoic acid
-
-
(S,S)-5-phenyl-2-[(3,3,3-trifluoro-2-methoxy-2-phenylpropionyl)amino]pent-4-ynoic acid (2-cyanoethyl)amide
-
-
1-(2,6-difluorobenzyl)-5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.00065 mM
1-(2-fluorobenzyl)-5-[[(1-methylcyclopentyl)acetyl]amino]-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.00012 mM
1-(cyclohexylmethyl)-5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.00086 mM
2-[(tert-butoxycarbonyl)amino]-5-(2,4-difluorophenyl)pent-4-ynoic acid methyl ester
-
-
2-{[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}-3-(naphthalen-1-yl)propanoic acid
-
2-{[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}-3-(naphthalen-2-yl)propanoic acid
-
2-{[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}-3-[3'-(trifluoromethyl)biphenyl-4-yl]propanoic acid
-
3-(2'-methoxybiphenyl-4-yl)-2-{[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(2,3'-bipyridin-5'-yl)-N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]alanine
-
3-(3'-chloro-4'-fluorobiphenyl-4-yl)-2-{[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(4'-chlorobiphenyl-4-yl)-2-{[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(4'-fluorobiphenyl-4-yl)-2-{[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-[({1-[(2-methyl-2-sulfanylpropanoyl)amino]cyclopentyl}carbonyl)amino]propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2R)-2-sulfanylhexanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2R)-3-hydroxy-2-sulfanylpropanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2R)-3-methoxy-2-sulfanylpropanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2R)-3-phenyl-2-sulfanylpropanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2R)-4-(methylsulfanyl)-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2R)-4-methyl-2-sulfanylpentanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2S)-2-sulfanylhexanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2S)-3-methyl-2-sulfanylpentanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2S)-4-methyl-2-sulfanylpentanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(3S)-3-methoxy-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(3S)-3-methyl-2-sulfanylpentanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-[4-(furan-2-yl)pyrimidin-5-yl]-N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]alanine
-
3-[4-(furan-3-yl)pyrimidin-5-yl]-N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]alanine
-
3-[5-(2-methoxyphenyl)pyridin-3-yl]-N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]alanine
-
3-[6-(3-aminophenyl)pyridin-3-yl]-N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]alanine
-
3-{6-[3-(acetylamino)phenyl]pyridin-3-yl}-N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]alanine
-
4-chloro-N-[(4-cyano-3-methyl-1-phenyl-1H-pyrazol-5-yl)amino]carbonyl benzenesulfonamide
-
-
4-cyclohexyl-N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]phenylalanine
-
4-furan-2-yl-N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]phenylalanine
-
4-[([5-[(2,2-dimethylpropyl)carbamoyl]-1-(2-fluorobenzyl)-1H-indol-2-yl]carbonyl)amino]benzoic acid
-
IC50: 0.00039 mM
5-[(3,3-dimethylbutanethioyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.00066 mM
5-[(3,3-dimethylbutanoyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.00022 mM
5-[(3,3-dimethylbutanoyl)amino]-1-(2-methylbenzyl)-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.003 mM
5-[(3,3-dimethylbutanoyl)amino]-1-[(2-methyl-1,3-thiazol-4-yl)methyl]-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.0022 mM
5-[(3,3-dimethylbutanoyl)amino]-N,1-diphenyl-1H-indole-2-carboxamide
-
IC50: 0.0059 mM
5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1-(2-phenylethyl)-1H-indole-2-carboxamide
-
IC50: 0.0051 mM
5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1-[2-(trifluoromethyl)benzyl]-1H-indole-2-carboxamide
-
IC50: 0.00017 mM
5-[(4,4-dimethylpentanoyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.00074 mM
5-[(bicyclo[2.2.1]hept-2-ylacetyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.0003 mM
5-[(cyclopentylacetyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.0064 mM
5-[([5-[(2,2-dimethylpropyl)carbamoyl]-1-(2-fluorobenzyl)-1H-indol-2-yl]carbonyl)amino]pyridine-3-carboxylic acid
-
IC50: 0.074 mM
5-[[(2,2-dimethylpropyl)sulfonyl]amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.0067 mM
benzoylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo[1,4]-dioxin-5-yl ester
-
IC50: 0.0004805 mM
cyclohexyl-2-[[5-(2,4-difluorophenyl)-2-[(phosphonomethyl)-amino]pent-4-ynoyl]amino]propionic acid
-
-
ECEi
-
addition of an ECE-1 specific inhibitor (ECEi) to PC-3 cells reduces phosphorylation of focal adhesion kinase
-
L-tryptophan, N-[[1-[[(2S)-2-(acetylthio)-4-methyl-1 oxopentyl]amino]cyclopentyl]-carbonyl]-methyl ester
-
CGS 37808, at an oral dose of 10 mgEq per kg, CGS 37808 produced 71% and 67% inhibition of the big ET-1 pressor response at 30 and 120 min, respectively
L-tryptophan, N-[[1-[[(2S)-2-mercapto-4-methyl-1-oxopentyl]amino]-cyclopentyl]carbonyl]
-
CGS 35601, IC50: 55 nM
N-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-2-(3-phenyl-1,2,4-oxadiazol-5-yl)-1H-indole-5-carboxamide
-
IC50: 0.01 mM
N-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-2-[(phenylamino)methyl]-1H-indole-5-carboxamide
-
IC50: 0.01 mM
N-(2-benzyl-3-[[(1R)-1-[[(benzyloxy)carbonyl]amino]-2-phenylethyl](hydroxy)phosphoryl]propanoyl)-L-tryptophan
-
-
N-(3-{[(1R)-1-{[(benzyloxy)carbonyl]amino}-2-phenylethyl](hydroxy)phosphoryl}-2-{[3-(biphenyl-4-yl)-4,5-dihydro-1,2-oxazol-5-yl]methyl}propanoyl)-L-tryptophan
-
-
N-(alpha-L-rhamnopyranosyl-oxyhydroxy-phosphinyl)-L-Leu-L-Trp
mechanism of inhibitor binding analysed (cocrystallization)
N-(alpha-rhamnopyranosyloxyhydroxyphosphinyl)-Leu-Trp
-
phosphoramidon, synthetic inhibitor, ECE-1/NEP inhibitor
N-[(1-{[(2R)-2-sulfanylhexanoyl]amino}cyclopentyl)carbonyl]-3-[4-(thiophen-3-yl)pyrimidin-5-yl]alanine
-
N-[(1-{[(2R)-2-sulfanylpentanoyl]amino}cyclopentyl)carbonyl]-3-[4-(thiophen-3-yl)pyrimidin-5-yl]alanine
-
N-[(1-{[(2S)-2-sulfanylhexanoyl]amino}cyclopentyl)carbonyl]-3-[4-(thiophen-3-yl)pyrimidin-5-yl]alanine
-
N-[(1-{[(2S)-2-sulfanylpentanoyl]amino}cyclopentyl)carbonyl]-3-[4-(thiophen-3-yl)pyrimidin-5-yl]alanine
-
N-[(1-{[(2S)-3-cyclohexyl-2-sulfanylpropanoyl]amino}cyclopentyl)carbonyl]-3-[4-(thiophen-3-yl)pyrimidin-5-yl]alanine
-
N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]-3-(4-phenylpyrimidin-5-yl)alanine
-
N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]-3-[4-(thiophen-3-yl)pyrimidin-5-yl]alanine
-
N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]-3-[6-(3-nitrophenyl)pyridin-3-yl]alanine
-
N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]-4-thiophen-3-ylphenylalanine
-
N-[(1-{[(2S)-4-(methylsulfanyl)-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]-3-[4-(thiophen-3-yl)pyrimidin-5-yl]alanine
-
N-[(1-{[(2S)-4-methyl-2-sulfanylpentanoyl]amino}cyclopentyl)carbonyl]-3-[4-(thiophen-3-yl)pyrimidin-5-yl]alanine
-
N-[3-{[(1R)-1-{[(benzyloxy)carbonyl]amino}-2-phenylethyl](hydroxy)phosphoryl}-2-(biphenyl-4-ylmethyl)propanoyl]-L-tryptophan
-
-
N-{(2S)-3-{[(1R)-1-{[(benzyloxy)carbonyl]amino}-2-phenylethyl](hydroxy)phosphoryl}-2-[(3-phenyl-1,2-oxazol-5-yl)methyl]propanoyl}-L-tryptophan
-
-
N2-(4-carbamoylphenyl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
-
IC50: 0.00022 mM
N2-(5-aminopyridin-2-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
-
IC50: 0.0012 mM
N2-(6-aminopyridin-3-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
-
IC50: 0.00017 mM
N2-(6-chloropyridin-3-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
-
IC50: 0.00044 mM
N2-[4-(dimethylcarbamoyl)phenyl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
-
IC50: 0.00021 mM
N2-[4-[(butylsulfonyl)amino]phenyl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
-
IC50: 0.0002 mM
N2-[6-(acetylamino)pyridin-3-yl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
-
IC50: 0.00013 mM
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-(3-[[4-(methylsulfamoyl)phenyl]carbamoyl]phenyl)-1H-indole-2,5-dicarboxamide
-
IC50: 0.00015 mM
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-1,3,4-thiadiazol-2-yl-1H-indole-2,5-dicarboxamide
-
IC50: 0.0023 mM
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-1H-pyrazol-3-yl-1H-indole-2,5-dicarboxamide
-
IC50: 0.01 mM
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-phenyl-1H-indole-2,5-dicarboxamide
-
IC50: 0.007 mM; IC50: 0.01 mM
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-pyridin-3-yl-1H-indole-2,5-dicarboxamide
-
IC50: 0.00085 mM
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-[3-[(4-sulfamoylphenyl)carbamoyl]phenyl]-1H-indole-2,5-dicarboxamide
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IC50: 0.000039 mM
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-[5-[(4-methylpiperazin-1-yl)carbonyl]pyridin-3-yl]-1H-indole-2,5-dicarboxamide
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IC50: 0.09 mM
SLV-306
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KC-12792, synthetic inhibitor, ECE-1/NEP inhibitor, clinical trial for treatment of arterial hypertension and heart failure in human
specific ECE-1 inhibitor
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in the presence of 0.001 M ECE-1 inhibitor, cell number was effectively reduced to ~70% of control
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[Lys-Gly-His-Lys-Cu]+
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metallopeptide, IC50: 0.0049 mM under hydrolytic condtions
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4-chloro-N-(((4-cyano-3-methyl-1-phenyl-1H-pyrazol-5-yl)amino)carbonyl)benzenesulfonamide
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0.03 mM, Zn2+ restores, Cu2+, Co2+, Mn2+ or Fe2+ partially restores, not Ca2+ or Mg2+
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i.e. (2S,4R)-4-mercapto-2-(2,4,5-trifluoro-benzyloxymethyl)-pyrrolidine-1-carboxylic acid 2-methoxycarbonyl-phenyl ester, a selective ECE-1 inhibitor
SM-19712
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a specific ECE-1 inhibitor. SM-191712 causes sustained ERK2 activation in cytosolic and nuclear fractions after substance P removal
SM-19712
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a specific ECE-1 inhibitor. SM-191712 causes sustained ERK2 activation in cytosolic and nuclear fractions after substance P removal
SM-19712
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ECE-1 inhibitor prevents endosomal substance P degardation. Thus, neurokinin 1 receptor (NK1R) recycling is suppressed by more than 50%
SM-19712
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a specific ECE-1 inhibitor. SM-191712 causes sustained ERK2 activation in cytosolic and nuclear fractions after substance P removal
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leupeptin, chymostatin, pepstatin A, E-64, p-chloromercuriphenylsulfonic acid, N-ethylmaleimide or 4-amidinophenylmethyl sulfonylfluoride; no inhibition by thiorphan, captopril
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additional information
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neither exogenously added ET-1 nor the blockade of the receptors with bosentan modifies ECE-1 protein, overview
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additional information
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acidification to pH 6.4 inhibits plasma membrane ECE activity
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additional information
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prevention of acidification of endosomes using bafilomycin A1 inhibits the degradation of internalized somatostatin-14
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additional information
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carbachol and phorbol 12-myristate 13-acetate reduce enzyme expression in neuroblastoma NB7 cells, only isozyme ECE-1c remains detectable, overview
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additional information
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RNAi-induced knockdown of ECE-1 reduces ECE-1 mRNA and protein levels leading to 80% to 90% inhibition of endothelin-1 secretion by the ovarian carcinoma cells, analysation of cell's behaviour and effect on the cancer
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additional information
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ECE-1 inhibition causes endosomal retention of the substance P neurokinin 1 receptor, beta-arrestins, and Src, resulting in markedly sustained ERK2 activation in the cytosol and nucleus. ECE-1 inhibition also enhances substance P-induced expression and phosphorylation of the nuclear death receptor Nur77, resulting in cell death
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additional information
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phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1, while sparing neprilysin, inhibitors, overview
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additional information
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expression of ECE-1 is significantly reduced in the cortex of adult rats after 15 mins of global ischemia, and is also significantly reduced in the striatum of rats subjected to prenatal hypoxia
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additional information
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ECE-1 inhibition causes endosomal retention of the substance P neurokinin 1 receptor, beta-arrestins, and Src, resulting in markedly sustained ERK2 activation in the cytosol and nucleus. ECE-1 inhibition also enhances substance P-induced expression and phosphorylation of the nuclear death receptor Nur77, resulting in cell death
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