Information on EC 3.4.24.71 - endothelin-converting enzyme 1

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The expected taxonomic range for this enzyme is: Euteleostomi

EC NUMBER
COMMENTARY hide
3.4.24.71
-
RECOMMENDED NAME
GeneOntology No.
endothelin-converting enzyme 1
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
Hydrolysis of the -Trp21-/-Val- bond in big endothelin to form endothelin 1
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY hide
138238-81-0
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
-
-
Manually annotated by BRENDA team
killifish
UniProt
Manually annotated by BRENDA team
Mus musculus C57BL/6
C57BL/6
-
-
Manually annotated by BRENDA team
Mus musculus C57BL/6J
C57BL/6J
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
metabolism
physiological function
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
(7-methoxy-coumarin-4-yl)acetyl-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys(2,4-dinitrophenyl) + H2O
?
show the reaction diagram
-
fluorogenic substrate
-
-
?
(7-methoxycoumarin-4-yl)acetyl-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys-2,4-dinitrophenyl-OH + H2O
?
show the reaction diagram
-
-
-
-
?
amyloid beta peptide + H2O
?
show the reaction diagram
-
-
-
-
?
amyloid-beta peptide + H2O
?
show the reaction diagram
amyloid-beta peptide + H2O
amyloid-beta peptide + ?
show the reaction diagram
-
protein kinase C epsilon, PKCepsilon, stimulates the amyloid-beta peptide degradation by ECE-1 in mice leading to a decrease in plaque-associated astrocytosis and dystrophic neurites, overview
-
-
?
Angiotensin I + H2O
?
show the reaction diagram
-
-
-
-
?
angiotensin-I + H2O
?
show the reaction diagram
-
degradation, no activity with angiotensin-II
-
-
?
big endothelin + H2O
endothelin + ?
show the reaction diagram
big endothelin + H2O
endothelin 1 + ?
show the reaction diagram
big endothelin + H2O
endothelin-1 + ?
show the reaction diagram
Big endothelin 1 + H2O
?
show the reaction diagram
-
key enzyme in endothelin production, generates potent vasoconstrictor endothelin from its inactive precursor
-
-
-
big endothelin-1 + H2O
big endothelin fragment 22-38 + ?
show the reaction diagram
-
-
-
-
?
big endothelin-1 + H2O
endothelin + ?
show the reaction diagram
big endothelin-1 + H2O
endothelin-1 + ?
show the reaction diagram
big endothelin-3 + H2O
endothelin-3 + ?
show the reaction diagram
big endothelin-I + H2O
endothelin + ?
show the reaction diagram
Bradykinin + H2O
?
show the reaction diagram
calcitonin gene-related peptide + H2O
?
show the reaction diagram
corticotropin-releasing factor + H2O
?
show the reaction diagram
-
ECE-1 cleaves urocortin-1 (Ucn1) at three different sites but cleaves corticotropin-releasing factor (CRF) at only one site. ECE-1 degrades Ucn1 at both extracellular (pH 7.4) and endosomal (pH 5.5), whereas CRF is degraded at acidic pH alone. At a low or basal level, ECE-1 can disrupt association of Ucn1 or CRF with CRF1 in endosomes and free the receptor to promote recycling and resensitization
-
-
?
Human big endothelin 1 + H2O
Endothelin 1 + big endothelin 1(21-38)
show the reaction diagram
Human big endothelin 2 + H2O
?
show the reaction diagram
Human big endothelin 3 + H2O
?
show the reaction diagram
insulin B chain + H2O
?
show the reaction diagram
-
-
-
-
?
M7-methoxycoumarin-4-ylacetyl-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys(2,4-dinitrophenyl)-OH + H2O
?
show the reaction diagram
-
-
-
-
?
neurotensin + H2O
?
show the reaction diagram
-
-
-
-
?
preendothelin + H2O
endothelin + ?
show the reaction diagram
-
-
-
?
preproendothelin-1 + H2O
endothelin-1 + ?
show the reaction diagram
-
-
-
-
?
proendothelin-1 + H2O
endothelin + ?
show the reaction diagram
activation
-
-
?
somatostatin + H2O
?
show the reaction diagram
-
-
-
-
?
Somatostatin-14 + H2O
?
show the reaction diagram
-
i.e. SST-14, degradation of rat substrate internalized via recombinantly expressed somatostatin receptor subtype sst2A into HEK-293 cells
-
-
?
Substance P + H2O
?
show the reaction diagram
urocortin-1 + H2O
?
show the reaction diagram
-
ECE-1 cleaves urocortin-1 (Ucn1) at three different sites but cleaves corticotropin-releasing factor (CRF) at only one site. ECE-1 cleaves Ucn1 at Arg-34, which allows this ligands to bind and activate CRF1. ECE-1 degrades Ucn1 at both extracellular (pH 7.4) and endosomal (pH 5.5), whereas CRF is degraded at acidic pH alone. At a low or basal level, ECE-1 can disrupt association of Ucn1 or CRF with CRF1 in endosomes and free the receptor to promote recycling and resensitization
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
amyloid beta peptide + H2O
?
show the reaction diagram
-
-
-
-
?
amyloid-beta peptide + H2O
?
show the reaction diagram
Angiotensin I + H2O
?
show the reaction diagram
-
-
-
-
?
angiotensin-I + H2O
?
show the reaction diagram
-
degradation, no activity with angiotensin-II
-
-
?
big endothelin + H2O
endothelin + ?
show the reaction diagram
big endothelin + H2O
endothelin 1 + ?
show the reaction diagram
-
-
-
-
?
big endothelin + H2O
endothelin-1 + ?
show the reaction diagram
Big endothelin 1 + H2O
?
show the reaction diagram
-
key enzyme in endothelin production, generates potent vasoconstrictor endothelin from its inactive precursor
-
-
-
big endothelin-1 + H2O
big endothelin fragment 22-38 + ?
show the reaction diagram
-
-
-
-
?
big endothelin-1 + H2O
endothelin + ?
show the reaction diagram
big endothelin-1 + H2O
endothelin-1 + ?
show the reaction diagram
big endothelin-3 + H2O
endothelin-3 + ?
show the reaction diagram
-
specific for this substrate, big-endothelin-1 is no substrate
-
?
big endothelin-I + H2O
endothelin + ?
show the reaction diagram
-
key enzyme in the biosynthesis of the endothelins
-
?
Bradykinin + H2O
?
show the reaction diagram
calcitonin gene-related peptide + H2O
?
show the reaction diagram
-
degradation, co-internalization with ECE-1 into early endosomes, calcitonin gene-related peptide degradation promotes CLR/RAMP1 recycling and beta-arrestin2 redistribution into the cytosol, ECE-1 inhibition or knockdown traps CLR/RAMP1 and beta-arrestin2 in endosomes and inhibits CLR/RAMP1 recycling and resensitization, whereas ECE-1 overexpression has the opposite effect, mechanism, overview
-
-
?
neurotensin + H2O
?
show the reaction diagram
-
-
-
-
?
preendothelin + H2O
endothelin + ?
show the reaction diagram
-
-
-
?
preproendothelin-1 + H2O
endothelin-1 + ?
show the reaction diagram
-
-
-
-
?
proendothelin-1 + H2O
endothelin + ?
show the reaction diagram
A7LFV6
activation
-
-
?
somatostatin + H2O
?
show the reaction diagram
-
-
-
-
?
Substance P + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Ca2+
-
metalloprotease
Mg2+
-
-
Zinc
-
zinc metalloproteinase, zinc-binding domain
additional information
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(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-amino-5-(2,4-difluorophenyl)pent-4-ynoic acid methyl ester
-
-
(S)-2-[(tert-butoxycarbonyl)amino]-5-(2,4-difluorophenyl)pent-4-ynoic acid
-
-
(S)-2-[(tert-butoxycarbonyl)amino]-5-(2,4-difluorophenyl)pent-4-ynoic acid methyl ester
-
-
(S)-2-[(tert-butoxycarbonyl)amino]pent-4-ynoic acid
-
-
(S)-3-[5-[1-amino-4-(2-methoxyphenyl)but-3-ynyl]tetrazol-1-yl]propionitrile
-
-
(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-cyanoethyl)carbamoyl]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
-
-
1,10-phenanthroline
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-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
CGS 26303
CGS 26393
-
slight inhibition
CGS 26582
-
synthetic inhibitor, ECE/NEP/ACE inhibitor
CGS 34043
-
synthetic inhibitor, ECE-1/NEP inhibitor
CGS 34226
-
synthetic inhibitor, ECE-1/NEP inhibitor
CGS 35066
CGS 35339
-
-
CGS 35601
-
synthetic inhibitor, ECE/NEP/ACE inhibitor
CGS-26303
-
specific, complete inhibition at 0.025 mM
CGS-35066
Co3+-ATCUN complex
-
-
-
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
-
FR-901533
-
-
FR9015133
-
specific ECE-1 inhibitor, in vitro not in vivo
-
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
-
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
-
IC50: 0.09 mM
PD 069185
-
-
PD-069185
-
-
PD069185
-
a more selective ECE inhibitor
phosphoramidon
RO 67-7447
RXPA380
-
-
SCH 54470
-
synthetic inhibitor, ECE/NEP/ACE inhibitor
SCH-54,470
-
-
SLV-306
-
KC-12792, synthetic inhibitor, ECE-1/NEP inhibitor, clinical trial for treatment of arterial hypertension and heart failure in human
SM-19712
specific ECE-1 inhibitor
-
in the presence of 0.001 M ECE-1 inhibitor, cell number was effectively reduced to ~70% of control
-
thiorphan
WS-79089B
-
natural inhibitor, selective ECE-1 inhibitor
WS75624A
-
natural inhibitor, selective ECE-1 inhibitor
WS79089A
-
natural inhibitor, selective ECE-1 inhibitor
WS79089C
-
natural inhibitor, selective ECE-1 inhibitor
[KGHK-Cu]+
-
-
-
[Lys-Gly-His-Lys-Co(NH3)2]2+
-
metallopeptide
[Lys-Gly-His-Lys-Cu]+
-
metallopeptide, IC50: 0.0049 mM under hydrolytic condtions
additional information
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
captopril
-
solECE, activity 106.9%
chymostatin
-
-
E-64
-
-
pepstatin A
-
-
PMSF
-
-
additional information
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0046
(7-methoxycoumarin-4-yl)acetyl-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys-2,4-dinitrophenyl-OH
-
pH not specified in the publication, temperature not specified in the publication
0.0002 - 0.04831
Big endothelin-1
0.00046
big endothelin-2
-
-
0.00014 - 0.00027
big endothelin-3
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00528 - 0.112
Big endothelin-1
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000008
(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
-
pH not specified in the publication, temperature not specified in the publication
0.000014
(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
-
pH not specified in the publication, temperature not specified in the publication
0.000026
(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
-
pH not specified in the publication, temperature not specified in the publication
0.000275
(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
-
pH not specified in the publication, temperature not specified in the publication
0.0000077
(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
-
pH not specified in the publication, temperature not specified in the publication
0.00024
(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
-
pH not specified in the publication, temperature not specified in the publication
0.01
(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
0.000022
CGS 35066
-
pH not specified in the publication, temperature not specified in the publication
0.0012
N-(2-benzyl-3-[[(1R)-1-[[(benzyloxy)carbonyl]amino]-2-phenylethyl](hydroxy)phosphoryl]propanoyl)-L-tryptophan
-
pH not specified in the publication, temperature not specified in the publication
0.00091
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
-
pH not specified in the publication, temperature not specified in the publication
0.0021
N-[3-{[(1R)-1-{[(benzyloxy)carbonyl]amino}-2-phenylethyl](hydroxy)phosphoryl}-2-(biphenyl-4-ylmethyl)propanoyl]-L-tryptophan
-
pH not specified in the publication, temperature not specified in the publication
0.005
N-{(2S)-3-{[(1R)-1-{[(benzyloxy)carbonyl]amino}-2-phenylethyl](hydroxy)phosphoryl}-2-[(3-phenyl-1,2-oxazol-5-yl)methyl]propanoyl}-L-tryptophan
-
pH not specified in the publication, temperature not specified in the publication
0.0012
phosphoramidon
-
pH not specified in the publication, temperature not specified in the publication
0.05
RXPA380
-
pH not specified in the publication, temperature not specified in the publication
0.00008
SCH-54,470
-
pH not specified in the publication, temperature not specified in the publication
0.00207
[KGHK-Cu]+
-
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00109
(2S,4R)-2-[(2,5-difluorobenzylamino)methyl]-4-mercaptopyrrolidine-1-carboxylic acid isopropyl ester
Homo sapiens
-
IC50: 0.00109 mM
0.01089
(2S,4R)-2-[2-[[4-mercapto-1-(naphthalene-2-sulfonyl)-pyrrolidine-2-carbonyl]methylamino]acetylamino]-benzoic acid methyl ester
Homo sapiens
-
IC50: 0.01089 mM
0.0000765
(2S,4R)-4-acetylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo-[1,4]dioxin-5-yl ester
Homo sapiens
-
IC50: 0.0000765 mM
0.0000215
(2S,4R)-4-acetylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-1-carboxylic acid 2-methoxycarbonylphenylester
Homo sapiens
-
IC50: 0.0000215 mM
0.00253
(2S,4R)-4-mercapto-1-(naphthalene-2-sulfonyl)pyrrolidine-2-carboxylic acid N-methyl-N-(4-methylphenylsulfonyl)hydrazide
Homo sapiens
-
IC50: 0.00253 mM
0.000137
(2S,4R)-4-mercapto-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo[1,4]-dioxin-5-yl ester
Homo sapiens
-
IC50: 0.000137 mM
0.000067
(2S,4R)-4-mercapto-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2-ethoxycarbonylphenylester
Homo sapiens
-
IC50: 0.000067 mM
0.0000729
(2S,4R)-5-[(2,5-difluorobenzylamino)methyl]-1-(5-propylpyrimidin-2-yl)pyrrolidine-3-thiol
Homo sapiens
-
IC50: 0.0000729 mM
0.0000198
(3R,5S)-1-(5-propylpyrimidin-2-yl)-5-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-3-thiol trifluoroacetate
Homo sapiens
-
IC50: 0.0000198 mM
0.00065
1-(2,6-difluorobenzyl)-5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.00065 mM
0.00012
1-(2-fluorobenzyl)-5-[[(1-methylcyclopentyl)acetyl]amino]-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.00012 mM
0.00086
1-(cyclohexylmethyl)-5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.00086 mM
0.00039
4-[([5-[(2,2-dimethylpropyl)carbamoyl]-1-(2-fluorobenzyl)-1H-indol-2-yl]carbonyl)amino]benzoic acid
Homo sapiens
-
IC50: 0.00039 mM
0.00066
5-[(3,3-dimethylbutanethioyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.00066 mM
0.00022
5-[(3,3-dimethylbutanoyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.00022 mM
0.003
5-[(3,3-dimethylbutanoyl)amino]-1-(2-methylbenzyl)-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.003 mM
0.0022
5-[(3,3-dimethylbutanoyl)amino]-1-[(2-methyl-1,3-thiazol-4-yl)methyl]-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.0022 mM
0.0059
5-[(3,3-dimethylbutanoyl)amino]-N,1-diphenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.0059 mM
0.0051
5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1-(2-phenylethyl)-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.0051 mM
0.00017
5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1-[2-(trifluoromethyl)benzyl]-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.00017 mM
0.00074
5-[(4,4-dimethylpentanoyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.00074 mM
0.0003
5-[(bicyclo[2.2.1]hept-2-ylacetyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.0003 mM
0.0064
5-[(cyclopentylacetyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.0064 mM
0.074
5-[([5-[(2,2-dimethylpropyl)carbamoyl]-1-(2-fluorobenzyl)-1H-indol-2-yl]carbonyl)amino]pyridine-3-carboxylic acid
Homo sapiens
-
IC50: 0.074 mM
0.0067
5-[[(2,2-dimethylpropyl)sulfonyl]amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.0067 mM
0.0004805
benzoylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo[1,4]-dioxin-5-yl ester
Homo sapiens
-
IC50: 0.0004805 mM
0.000017 - 0.0011
CGS 26303
0.00062
CGS 26582
Sus scrofa
-
-
0.0000058
CGS 34043
Homo sapiens
-
human recombinant ECE-1 overexpressed in CHO cells
0.000011
CGS 34226
Homo sapiens
-
human recombinant ECE-1 overexpressed in CHO cells
0.000022
CGS 35066
Homo sapiens
-
COS-1 cell membrane with overexpression of human ECE-1
0.000055
CGS 35601
0.01
N-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-2-(3-phenyl-1,2,4-oxadiazol-5-yl)-1H-indole-5-carboxamide
0.0035
N-(alpha-rhamnopyranosyloxyhydroxyphosphinyl)-Leu-Trp
Sus scrofa
-
potency varies with pH of medium
0.00022
N2-(4-carbamoylphenyl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.00022 mM
0.0012
N2-(5-aminopyridin-2-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.0012 mM
0.00017
N2-(6-aminopyridin-3-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.00017 mM
0.00044
N2-(6-chloropyridin-3-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.00044 mM
0.00021
N2-[4-(dimethylcarbamoyl)phenyl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.00021 mM
0.0002
N2-[4-[(butylsulfonyl)amino]phenyl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.0002 mM
0.00013
N2-[6-(acetylamino)pyridin-3-yl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.00013 mM
0.00015
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-(3-[[4-(methylsulfamoyl)phenyl]carbamoyl]phenyl)-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.00015 mM
0.0023
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-1,3,4-thiadiazol-2-yl-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.0023 mM
0.01
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-1H-pyrazol-3-yl-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.01 mM
0.007 - 0.01
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-phenyl-1H-indole-2,5-dicarboxamide
0.00085
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-pyridin-3-yl-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.00085 mM
0.000039
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-[3-[(4-sulfamoylphenyl)carbamoyl]phenyl]-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.000039 mM
0.09
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-[5-[(4-methylpiperazin-1-yl)carbonyl]pyridin-3-yl]-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.09 mM
0.0000012
RO 67-7447
Rattus norvegicus
-
-
0.00008
SCH 54470
Cavia sp.
-
-
0.000042
SM-19712
Sus scrofa
-
in vitro result, in vivo potency is lower than expected compared to in vitro result
0.00014
WS-79089B
Bos taurus
-
-
0.00073
WS79089A
Bos taurus
-
-
0.00342
WS79089C
Bos taurus
-
-
0.0049
[Lys-Gly-His-Lys-Cu]+
Homo sapiens
-
metallopeptide, IC50: 0.0049 mM under hydrolytic condtions
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.0001799
-
recombinant enzyme
0.00127
-
-
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
5.5
-
ECE-1 degrades Ucn1 and CRF at endosomal (pH 5.5)
6.1 - 6.4
-
solECE-1
6.6
-
-
6.6 - 6.8
-
-
6.7 - 6.9
-
ECE-1
7.5
-
assay at
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
5.5 - 6.8
-
solECE-1 half-maximal activity at pH 5.7 and pH 6.7
5.7 - 7.3
-
native ECE-1, half-maximal activity at pH 6.2 and pH 7.0
5.8 - 7.8
-
about half-maximal activity at pH 5.8 and 7.8
6.5 - 7.2
-
active in a narrow range
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
ECE-1 overexpression, immunohistochemic ECE-1 expression analysis of 600 different samples, the expression of ECE-1 is correlated to VEGF expression, overview
Manually annotated by BRENDA team
-
cerebellar, lower expression of ECE-1
Manually annotated by BRENDA team
-
ECE-1 expression in Alzheimer's disease brain shows no significant difference compared with age-matched controls
Manually annotated by BRENDA team
-
from healthy persons and from patients with Crohn's disease, enzyme expression anaylsis in different samples, healthy tissue shows enzyme expression mainly in the muscular layer and the vasculature, while in Crohn'sdisease colonic tissue, the enzyme is found at inflammatory sites and fibrotic tissue, overview
Manually annotated by BRENDA team
-
expression and localization of the ECE-1 isozymes, overview
Manually annotated by BRENDA team
-
expression of isozymes ECE-1a-d
Manually annotated by BRENDA team
-
ECE-1 promotes re-sensitization of SP-induced inflammation
Manually annotated by BRENDA team
-
enzyme distribution in the endometrium during different developmental phases, the enzyme expression varies during the menstrual cycle, epithelial cell, overview
Manually annotated by BRENDA team
-
endometrial, primary cell culture
Manually annotated by BRENDA team
-
enzyme expression in chalizia in meibomian adenomers, conjunctival epithelium, tarsal mucous glands, and in inflammatory cells, immunohistochemic analysis, overview
Manually annotated by BRENDA team
-
expression and localization of the ECE-1 isozymes, overview
Manually annotated by BRENDA team
-
from blood, determination of enzyme expression by immunohistochemical analysis using a combination of ECE-1 isoform-specific antibodies, expression of isozymes ECE-1a and ECE-1c
Manually annotated by BRENDA team
-
expression and localization of the ECE-1 isozymes, overview
Manually annotated by BRENDA team
-
increased ECE-1 content in hypercholesterolemic patients
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
expression and localization of the ECE-1 isozymes, overview
Manually annotated by BRENDA team
-
primary cells derived from malignant tissue from radical prostatectomies, expression and localization of the ECE-1 isozymes, overview, upregulation of the isozyme ECE-1c
Manually annotated by BRENDA team
-
primary cells derived from benign tissue from radical prostatectomies, expression and localization of the ECE-1 isozymes, overview
Manually annotated by BRENDA team
-
cerebellar
Manually annotated by BRENDA team
-
dorsal skin, ECE-1 promotes re-sensitization of SP-induced inflammation
Manually annotated by BRENDA team
-
aortic, determination of enzyme expression by immunohistochemical analysis using a combination of ECE-1 isoform-specific antibodies, expression of isozyme ECE-1a
Manually annotated by BRENDA team
-
ECE-1 protein level in stellate cell from bile duct ligation-injured liver is increased twofold compared to those in normal stellate cell, ECE-1 protein is also up-regulated in cell from CCl4-injured liver and culture-activated stellate cell. Exposure of stellate cell from injured livers to TGF-betaincreases ECE-1 expression
Manually annotated by BRENDA team
-
ECE-1 promotes re-sensitization of SP-induced inflammation
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
isozymes ECE-1a and ECE-1c
Manually annotated by BRENDA team
-
isozyme ECE-1b
Manually annotated by BRENDA team
-
ECE-1a but not ECE-1b co-localizes with nuclear membrane markers
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
additional information
PDB
SCOP
CATH
ORGANISM
UNIPROT
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
78000
-
crystallization, 680 residues of monomeric enzyme (extracellular domain, residues 90-770)
85520
-
rat, deduced from nucleotide sequence
85610
-
bovine, deduced from nucleotide sequence
140000
-
SDS-PAGE
170000 - 190000
-
rat, FPLC gel filtration
232000
-
gel filtration
250000 - 300000
-
gel filtration
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
?
-
x * 80000, SDS-PAGE
homodimer
monomer
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glycoprotein
phosphoprotein
-
the isozymes contain a different number of putative phosphorylation sites for protein kinase C and protein kinase A in the amino-terminal region, stimulation of phosphorylation by phorbol myristate acetate, inhibition by calphostin C, phosphorylation might play an important role in the regulation of intracellular trafficking of ECE-1 subisoforms
additional information
-
intra-molecular disulfide bond formed by C428 (homodimer)
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
cocrystallization of C428S mutant of monomeric form (extracellular domain, residues 90-770) with inhibitor N-(alpha-L-rhamnopyranosyl-oxyhydroxy-phosphinyl)-L-Leu-L-Trp
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
cell rupture by lysozyme and continuous cell disrupter, washing of insoluble pellet
-
Sepharose 4B column affinity chromatography
-
to near homogeneity
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
bovine; expressed in Chinese hamster ovary CHO-K1 cells
-
COS-1 cell membrane with overexpression of human ECE-1
DNA and amino acid sequence determination and anaylsis, genotyping, the ECE encoding gene shows several single nucleotide polymorphisms, overview
-
DNA and amino acid sequence determination and anaylsis, phylogenetic analysis
ECE-1 is endogenously expressed in HMEC-1 cells (RT-PCR, immunofluorescence)
-
ECE-1 mRNA level is 42% lower in stenotic valves
-
expressed in Chinese hamster ovary cells
-
expressed in COS-cells; rat
-
expressed in NCM-460 cells
-
expression of ECE-1 is significantly higher in the solid tumors compared with effusions
-
extracellular domain of monomeric human ECE-1 (C428S) mutant (Q90-W770) is amplified by PCR and produced recombinantly in Escherichia coli (inclusion bodies)
-
gene ECE-1b , the ECE-1 gene is located on chromosome 1, 1p36, genotyping
-
generation of apolipoprotein E-deficient mouse from strain C57BL/6J
-
GFP-tagged ECE-1 overexpression in HEK-293 cells
-
isozyme genetic structure, overview, expression of wild-type isozyme ECE-1d and of truncated variant ECE-1sv lacking the signal peptide, expression analysis of isozymes and splicing variants, overview
-
overexpression of GFP-tagged isozymes in HEK cell endosomes, subcellular localization, overview
-
sECE, constructed by fusing the cleavable signal peptide of pro-opiomelanocortin in frame to complete extracellular domain of ECE-1, expressed in CHO cells
-
solECE-1 constructed by fusing the cleavable N-terminalsignal sequence of human alkaline phosphatase in frame with the entire extracellular domain of ECE-1, transfected into CHO-K1 cells
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
alternative polyadenylation results in the production of enzyme transcripts with truncated 3'-untranslated regions which promote elevated protein expression
-
enzyme expression is significantly increased in the placenta and its implantation site of pregnant hyperinsulinemic rats. In the kidney and heart, protein expression is increased by 230 and 220%, respectively, while its level in the liver is similar in normal and hyperinsulinemic rats
nitric oxide decreases the expression of ECE-1 through a cGMP/PKG-dependent regulatory mechanism at the post-transcriptional level via the 3'-UTR of the ECE-1 gene
-
siRNA-mediated knockdown of ECE-1 results in a significant reduction in FAK phosphorylation
-
the enzyme expression is markedly inhibited by its 3'-untranslated region
-
transient ECE-1 overexpression in PNT1-a cells increases FAK phosphorylation
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
C338A
-
the mutation in isoform ECE-1b creates a new E2F-2 transcription factor binding site and enhances expression of this intracellular isoform
C428S
-
mutant of monomeric form
K198N
-
naturally occuring polymorphism, the mutant shows impaired function
additional information
Renatured/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
inclusion bodies solubilized in Tris-HCl, urea, beta-mercaptoethanol, dithiotreithol, glutathione, glycine
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
drug development
medicine
Show AA Sequence (344 entries)
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