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3.4.24.11: neprilysin

This is an abbreviated version!
For detailed information about neprilysin, go to the full flat file.

Word Map on EC 3.4.24.11

Reaction

preferential cleavage of polypeptides between hydrophobic residues, particularly with Phe or Tyr at P1' =

Synonyms

Abeta-degrading enzyme, acute lymphoblastic leukemia antigen, antigen, CALLA (common acute lymphoblastic leukemia-associated), atriopeptidase, CALLA, CALLA (common acute lymphoblastic leukemia-associated) antigens, CALLA antigen, CALLA glycoproteins, CD10, CD10/neutral endopeptidase, CD10/neutral endopeptidase 24.11, common acute lymphoblastic leukemia antigen, common acute lymphoblastic leukemia-associated antigens, Common acute lymphocytic leukemia antigen, endopeptidase CD10, Endopeptidase-2, endopeptidase-24.11, enkephalinase, EP24.11, glycoprotein, CALLA, kidney-brush-border neutral endopeptidase, kidney-brush-border neutral peptidase, kidney-brush-border neutral proteinase, membrane metallo-endopeptidase, membrane metalloendopeptidase, MME, NEP, NEP 24.11, NEP, enkephalinase, neutrophil cluster-differentiation antigen 10, common acute lymphoblastic leukemia antigen, NEP-1, NEP/CD10, NEP2, NEP4A, NEP4B, neprilypsin, neprilysin, neprilysin 4, neutral endopeptidase, neutral endopeptidase 24.11, neutral endopeptidase 24.11/CD10, neutral metallendopeptidase, NL-1, peptidase, endo-, peptidase, membrane metalloendo-, SEP, skin fibroblast elastase

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.24 Metalloendopeptidases
                3.4.24.11 neprilysin

Inhibitors

Inhibitors on EC 3.4.24.11 - neprilysin

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2(R,S)-2-sulfanyl-2-benzyl)acetyl-Ala-Pro
-
-
(2(R,S)-2-sulfanyl-2-benzyl)acetyl-Leu-Tyr
-
-
(2(R,S)-2-sulfanyl-2-benzyl)acetyl-Phe-Ala
-
-
(2(R,S)-2-sulfanyl-2-benzyl)acetyl-Phe-Tyr
-
-
(2(R,S)-2-sulfanyl-2-isopropyl)acetyl-Ile-Tyr
-
-
(2R)-2-(biphenyl-4-ylmethyl)-6-[4-[cyclohexyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanylhexanoic acid
-
(2R)-2-([1-[(5-ethyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
-
-
(2R)-2-[(1-[[(1S)-1-carboxy-2-(3-phenyl-1,2,4-oxadiazol-5-yl)ethyl]carbamoyl]cyclopentyl)methyl]-5-oxopentanoic acid
-
-
(2R)-2-[(1-[[(1S)-1-carboxy-2-(4-ethyl-1,3-oxazol-2-yl)ethyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
-
-
(2R)-2-[(1-[[(1S)-1-carboxy-2-(4-phenyl-1,3-oxazol-2-yl)ethyl]carbamoyl]cyclopentyl)methyl]-5-oxopentanoic acid
-
-
(2R)-2-[(1-[[(1S)-1-carboxy-2-(4-phenyl-1,3-oxazol-2-yl)ethyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
-
-
(2R)-2-[(1-[[(1S)-1-carboxy-2-(5-phenyl-1,3,4-oxadiazol-2-yl)ethyl]carbamoyl]cyclopentyl)methyl]-5-oxopentanoic acid
-
-
(2R)-2-[(1-[[(1S)-1-carboxy-2-(5-phenyl-1,3-oxazol-2-yl)ethyl]carbamoyl]cyclopentyl)methyl]-5-oxopentanoic acid
-
-
(2R)-2-[(1-[[(1S)-1-carboxy-2-(5-phenyl-1,3-oxazol-2-yl)ethyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
-
-
(2R)-2-[[1-([(1S)-1-carboxy-2-[4-(2-methylpropyl)-1,3-oxazol-2-yl]ethyl]carbamoyl)cyclopentyl]methyl]pentanoic acid
-
-
(2R)-2-[[1-([(1S)-1-carboxy-2-[5-(4-chlorophenyl)-1,3-oxazol-2-yl]ethyl]carbamoyl)cyclopentyl]methyl]-5-oxopentanoic acid
-
-
(2R)-6-[4-[cyclohexyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanyl-2-[4-(thiophen-3-yl)benzyl]hexanoic acid
-
(2S)-2-(biphenyl-4-ylmethyl)-6-[4-[cyclohexyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanylhexanoic acid
-
(2S)-2-[(1-[[2-(hydroxymethyl)-2,3-dihydro-1H-inden-2-yl]carbamoyl]cyclopentyl)methyl]-4-methoxybutanoic acid
-
-
(2S)-2-[(1-[[3-(4-chlorophenyl)propyl]carbamoyl]cyclopentyl)methyl]-4-methoxybutanoic acid
-
-
(2S)-2-[(1-[[3-(4-fluorophenyl)propyl]carbamoyl]cyclopentyl)methyl]-4-methoxybutanoic acid
-
-
(2S)-2-[[(2S)-1-[[(1S)-2-(biphenyl-4-yl)-1-carboxyethyl]amino]-5-methyl-1-oxohexan-2-yl]amino]-4-phenylbutanoic acid (non-preferred name)
-
-
(2S)-4-methoxy-2-([1-[(1-methyl-2-phenylethyl)carbamoyl]cyclopentyl]methyl)butanoic acid
-
-
(2S)-4-methoxy-2-[(1-[[(1R,2S)-2-(4-methoxyphenyl)cyclopropyl]carbamoyl]cyclopentyl)methyl]butanoic acid
-
-
(2S)-6-[4-[cyclohexyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanyl-2-[4-(thiophen-3-yl)benzyl]hexanoic acid
-
(S)-N-[2-(phosphonomethylamino)-3-(4-biphenylyl)-propionyl]-3-aminopropionic acid
-
effects of neutral endopeptidase in acute inflammation in the lung are studied using a newly developed murine model of smoke and burn injury using NEP antagonist CGS-24592. Smoke and burn-induced lung injury and inflammation in mice pretreated with CGS-24592 is exacerbated, leading to more plasma extravasation and severe airway inflammation
1,10-phenanthroline
2,3-Dimercaptopropan-1-ol
-
weak
2-(1-heptylcarbamoyl-cyclopentylmethyl)-4-methoxy-butyric acid tert-butyl ester
-
-
2-(4-bromobenzyl)-4-oxo-5-sulfanyl-6-[4-(2-sulfanylpropan-2-yl)phenyl]hexanoic acid
-
2-(4-bromobenzyl)-4-oxo-5-sulfanyl-6-[4-(3-sulfanylpentan-3-yl)phenyl]hexanoic acid
-
2-(4-bromobenzyl)-4-oxo-6-phenyl-5-sulfanylhexanoic acid
-
2-(4-bromobenzyl)-4-oxo-6-[4-[piperidin-4-yl(sulfanyl)methyl]phenyl]-5-sulfanylhexanoic acid
-
2-(4-bromobenzyl)-6-(4-bromophenyl)-4-oxo-5-sulfanylhexanoic acid
-
2-(4-bromobenzyl)-6-[4-(butan-2-yl)phenyl]-1-(morpholin-4-yl)-5-sulfanylhexane-1,4-dione
-
2-(4-bromobenzyl)-6-[4-(butan-2-yl)phenyl]-4-oxo-5-sulfanylhexanoic acid
-
2-(4-bromobenzyl)-6-[4-[2,3-dihydro-1H-inden-2-yl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanylhexanoic acid
-
2-(4-bromobenzyl)-6-[4-[cyclohexyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanylhexanoic acid
-
2-(4-bromobenzyl)-6-[4-[cyclopentyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanylhexanoic acid
-
2-(biphenyl-4-ylmethyl)-4-oxo-6-[4-[piperidin-4-yl(sulfanyl)methyl]phenyl]-5-sulfanylhexanoic acid
-
2-(biphenyl-4-ylmethyl)-6-[4-[2,3-dihydro-1H-inden-2-yl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanylhexanoic acid
-
2-(biphenyl-4-ylmethyl)-6-[4-[cyclohexyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanylhexanoic acid
-
2-(biphenyl-4-ylmethyl)-6-[4-[cyclopentyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanylhexanoic acid
-
2-([1-[(1,3-benzodioxol-5-ylmethyl)carbamoyl]cyclopentyl]methyl)pentanoic acid
-
IC50: 1500 nM
2-([1-[(1-benzyl-2-hydroxyethyl)carbamoyl]cyclopentyl]methyl)pentanoic acid
-
IC50: 384 nM
2-([1-[(1-benzyl-6-oxo-1,6-dihydropyridin-3-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
-
IC50: 313 nM
2-([1-[(1-ethyl-1H-1,2,3-triazol-4-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
-
IC50: 82 nM
2-([1-[(3-ethylpyridin-2-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
-
IC50: 1710 nM
2-([1-[(4-benzylpyridin-2-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
-
IC50: 96 nM
2-([1-[(4-butylpyridin-2-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
-
IC50: 184 nM
2-([1-[(4-carbamoylcyclohexyl)carbamoyl]cyclopentyl]methyl)pentanoic acid
-
IC50: 150 nM
2-([1-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
-
IC50: 30 nM
2-([1-[(5-ethyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)-4-phenylbutanoic acid
-
IC50: 46 nM
2-([1-[(5-ethyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)-5-methylhexanoic acid
-
IC50: 120 nM
2-([1-[(5-ethyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)hexanoic acid
-
IC50: 84 nM
2-([1-[(5-ethyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
-
IC50: 60 nM
2-([1-[(5-methyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
-
IC50: 176 nM
2-([1-[(5-phenyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
-
IC50: 283 nM
2-([1-[(6-methoxypyridazin-3-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
-
IC50: 374 nM
2-([1-[5-(1-benzyl-6-oxo-1,6-dihydropyridin-3-yl)-1,3,4-oxadiazol-2-yl]cyclopentyl]methyl)pentanoic acid
-
IC50: 1139 nM
2-benzyl-4-oxo-6-phenyl-5-sulfanylhexanoic acid
-
2-benzyl-6-(4-bromophenyl)-4-oxo-5-sulfanylhexanoic acid
-
2-mercaptoethanol
2-methoxymethyl-3-[1-(trans-2-phenyl-cyclopropylcarbamoyl)-cyclopentyl]-propionic acid tert-butyl ester
-
-
2-[(1-[[(1R)-1-phenylethyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
-
IC50: 530 nM
2-[(1-[[(1R)-3-(dimethylcarbamoyl)cyclohexyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
-
IC50: 297 nM
2-[(1-[[(1R,2R)-2-benzylcyclohexyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
-
IC50: 195 nM
2-[(1-[[(1R,2S)-2-propylcyclohexyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
-
IC50: 890 nM
2-[(1-[[(3R)-1-benzylpyrrolidin-3-yl]carbamoyl]cyclopentyl)methyl]pentanoic acid
-
IC50: 1060 nM
2-[(1-[[(3R)-1-carbamoylpyrrolidin-3-yl]carbamoyl]cyclopentyl)methyl]pentanoic acid
-
IC50: 213 nM
2-[(1-[[(5-methyl-1,3,4-thiadiazol-2-yl)methyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
-
IC50: 700 nM
2-[(1-[[1-(hydroxymethyl)cyclopentyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
-
IC50: 1710 nM
2-[(1-[[2-(hydroxymethyl)-2,3-dihydro-1H-inden-2-yl]carbamoyl]cyclopentyl)methyl]pentanoic acid
-
IC50: 96 nM
2-[(1-[[4-(dimethylcarbamoyl)cyclohexyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
-
IC50: 370 nM
2-[(1-[[5-(2-methylpropyl)-1,3,4-thiadiazol-2-yl]carbamoyl]cyclopentyl)methyl]pentanoic acid
-
IC50: 124 nM
2-[(1-[[5-(cyclopropylmethyl)-1,3,4-thiadiazol-2-yl]carbamoyl]cyclopentyl)methyl]pentanoic acid
-
IC50: 38 nM
2-[(3-iodo-4-hydroxy)phenylmethyl]-4-N-[3-hydroxyamino-3-oxo-1(phenylmethyl)propyl]amino-4-oxobutanoic acid
-
i.e. RB104, use of the inhibitor in detecting nanogram quantities of the enzyme by inhibitor gel electrophoresis
2-[(3-iodohydroxy)phenylmethyl]-4-N-[3-hydroxyamino-3-oxo-1-phenylmethylpropyl]-amino-4-oxobutanoic acid
-
i.e. RB104, highly selective and potent inhibitor
2-[1-(2-hydroxymethyl-indan-2-ylcarbamoyl)-cyclopentylmethyl]-4-methoxy-butyric acid tert-butyl ester
-
-
2-[1-(4-butyl-pyridin-2-ylcarbamoyl)-cyclopentylmethyl]-4-methoxybutyric acid benzyl ester
-
-
2-[1-(5-ethyl-[1,3,4]thiadiazol-2-ylcarbamoyl)-cyclopentylmethyl]-pentanoic acid
-
-
2-[1-[2-(trans-4-chlorophenyl)-cyclopropylcarbamoyl]-cyclopentylmethyl]-4-methoxy-butyric acid tert-butyl ester
-
-
2-[1-[3-(4-chloro-phenyl)-propylcarbamoyl]-cyclopentylmethyl]-4-methoxy-butyric acid tert-butyl ester
-
-
2-[1-[3-(4-fluoro-phenyl)-propylcarbamoyl]-cyclopentylmethyl]-4-methoxy-butyric acid tert-butyl ester
-
-
2-[[1-(1,3,4-thiadiazol-2-ylcarbamoyl)cyclopentyl]methyl]pentanoic acid
-
IC50: 377 nM
2-[[1-(2,3-dihydro-1H-inden-2-ylcarbamoyl)cyclopentyl]methyl]pentanoic acid
-
IC50: 313 nM
2-[[1-(5-benzyl-1,3,4-oxadiazol-2-yl)cyclopentyl]methyl]pentanoic acid
-
IC50: 3100 nM
2-[[1-(pyridin-2-ylcarbamoyl)cyclopentyl]methyl]pentanoic acid
-
IC50: 1500 nM
3-[1-[(5-ethyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]propanoic acid
-
IC50: 237 nM
3-[1-[2-(trans-4-chlorophenyl)-cyclopropylcarbamoyl]-cyclopentyl]-2-methoxymethyl-propionic acid tert-butyl ester
-
-
4-hydroxy-nonenal
-
intracellular neprilysin develops 4-hydroxy-nonenal adducts after 24 h of 4-hydroxy-nonenal treatment. 4-Hydroxy-nonenal-modified neprilysin shows decreased catalytic activity, which is associated with elevations in amyloid beta1-40 in SH-SY5Y and H4 APP695wt cells. Incubation of cells with amyloid beta1-42 also induces 4-hydroxy-nonenal adduction of neprilysin
4-methoxy-2-(1-phenethylcarbamoyl-cyclopentylmethyl)-butyric acid benzyl ester
-
-
4-methoxy-2-[1-(3-phenyl-propylcarbamoyl)-cyclopentylmethyl]-butyric acid tert-butyl ester
-
-
4-methoxy-2-[1-(trans-2-pentyl-cyclopropylcarbamoyl)-cyclopentylmethyl]-butyric acid tert-butyl ester
-
-
4-methoxy-2-[1-(trans-2-phenyl-cyclopropylcarbamoyl)-cyclopentylmethyl]-butyric acid tert-butyl ester
-
-
4-methoxy-2-[1-[(trans-2-(4-fluorophenyl)-cyclopropylcarbamoyl)]-cyclopentylmethyl]-butyric acid tert-butyl ester
-
-
4-methoxy-2-[1-[(trans-2-(4-methoxy-phenyl)-cyclopropylcarbamoyl)]-cyclopentylmethyl]-butyric acid tert-butyl ester
-
-
4-methoxy-2-[1-[2-(4-methoxy-phenoxy)-ethylcarbamoyl]-cyclopentylmethyl]-butyric acid tert-butyl ester
-
-
4-methoxy-2-[1-[2-(4-methoxy-phenyl)-ethylcarbamoyl]-cyclopentylmethyl]-butyric acid tert-butyl ester
-
-
4-methoxy-2-[1-[3-(4-methoxy-phenyl)-propylcarbamoyl]-cyclopentylmethyl]-butyric acid tert-butyl ester
-
-
6-(biphenyl-4-yl)-2-(4-bromobenzyl)-4-oxo-5-sulfanylhexanoic acid
-
6-[4-[(1-acetylpiperidin-4-yl)(sulfanyl)methyl]phenyl]-2-(4-bromobenzyl)-4-oxo-5-sulfanylhexanoic acid
-
6-[4-[(1-benzoylpiperidin-4-yl)(sulfanyl)methyl]phenyl]-2-(4-bromobenzyl)-4-oxo-5-sulfanylhexanoic acid
-
6-[4-[(1-benzylpiperidin-4-yl)(sulfanyl)methyl]phenyl]-2-(4-bromobenzyl)-4-oxo-5-sulfanylhexanoic acid
-
6-[4-[cyclohexyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanyl-2-[4-(thiophen-3-yl)benzyl]hexanoic acid
-
Acetorphan
-
-
AHU-377
-
LCZ696 comprises molecular moieties of valsartan, and of the NEP inhibitor prodrug AHU377 ((2R,4S)-5-biphenyl-4-yl-5-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester) (1:1 molar ratio). Oral administration of LCZ696 causes dose-dependent increases in atrial natriuretic peptide immunoreactivity due to NEP inhibition in Sprague-Dawley rats and provides sustained, dose-dependent blood pressure reductions in hypertensive double-transgenic rats
amyloid beta
-
amyloid beta1-42
-
incubation of cells with amyloid beta1-42 induces 4-hydroxy-nonenal adduction of neprilysin. In an apparent compensatory response, amyloid beta-treated cells show increased neprilysin mRNA and protein expression. Despite elevations in neprilysin protein, the activity is significantly lower compared with the neprilysin protein level
-
angiotensin I
-
-
atrial natriuretic factor
-
-
-
bradykinin
-
-
Butanedione
-
-
candoxatril
-
treatment increases plasma atrial natriuretic peptide levels and leads to significantly higher levels of atrial tissue cyclic GMP as well as plasma cyclic GMP. Candoxatril suppresses the shortening of atrial effective refractory period and monophasic action potential duration in the rapid atrial pacing model
candoxatrilat
CGS24592
-
-
chymostatin
-
-
cis-4-[([1-[(2S)-2-carboxy-3-(2-methoxyethoxy)propyl]cyclopentyl]carbonyl)amino]cyclohexanecarboxylic acid
-
-
diethyl dicarbonate
-
-
diisopropyl fluorophosphate
-
-
dithiothreitol
DL-[N-(3-mercapto-2-benzylpropanoyl)]glycine
-
following neprilysin inhibition, islet amyloid deposition and beta-cell apoptosis increase by 54 and 75%, respectively
EGTA
-
-
fasidotrilat
fasidotrilat interacts with the Arg664 of hNEP with more consistent bidentate hydrogen bonding and with the His658 with monodentate hydrogen bonding
GSH
-
-
heparin
-
-
Hg2+
0.001-0.05 mM, modifies the recombinant enzyme conformation, and highly reduces the enzyme activity. Hg2+ incubation increases NEP protein levels, but does not change NEP mRNA levels nor the levels of the amyloid intracellular domain peptide, a protein fragment with transcriptional activity. The Hg2+-induced inhibition of the enzyme activity may be mediated by a conformational change resulting in reduced amyloid beta1-42 degradation
Insulin B chain
inhibits the activity with substrate N-(4-carboxy-1-oxobutyl)-L-alanyl-L-alanyl-N-(4-methoxy-2-naphthalenyl)-L-phenylalaninamide
L-Cys
LCZ696
-
LCZ696 is a dual-acting angiotensin II-receptor and neprilysin inhibitor (ARNI) in a single molecule: angiotensin-receptor blockade via its valsartan molecular moiety, and neprilysin inhibition via its AHU377 molecular moiety. In a randomized, double-blind, placebo-controlled, active comparator study it is shown that compared with valsartan, dual-acting LCZ696 provides complementary and fully additive reduction of blood pressure
Leu5-enkephalin
MCB3937
bifunctional inhibitor of NEP and DPP-IV
MCB4241
bifunctional inhibitor of NEP and DPP-IV
Met5-enkephalin
N-(2-benzyl-3-sulfanylpropanoyl)glycine
-
synthetic NEP inhibitor
N-(2-benzyl-4-oxo-6-phenyl-5-sulfanylhexanoyl)-L-alanine
-
N-(2-benzyl-4-oxo-6-phenyl-5-sulfanylhexanoyl)-L-tryptophan
-
N-([1-[(2S)-2-carboxy-3-[[N2-(methylsulfonyl)-L-lysyl]amino]propyl]cyclopentyl]carbonyl)-L-tyrosine
-
-
N-phenethylphosphonyl-L-leucyl-L-tryptophan
N-[(2RS)-3-hydroxyaminocarbonyl-2-benzyl-1-oxopropyl]-Gly
-
-
N-[(2S)-3-phenyl-2-(sulfanylmethyl)propanoyl]-L-tryptophan
-
N-[1(R,S)-carboxy-2-phenylethyl]-Phe-p-aminobenzoate
-
-
N-[2-(4-bromobenzyl)-4-oxo-5-phenyl-5-sulfanylpentanoyl]-L-alanine
-
N-[2-(4-bromobenzyl)-4-oxo-5-sulfanylhexanoyl]-L-tryptophan
-
N-[2-(4-bromobenzyl)-4-oxo-6-phenyl-5-sulfanylhexanoyl]-L-alanine
-
N-[2-(4-bromobenzyl)-4-oxo-6-phenyl-5-sulfanylhexanoyl]-L-tryptophan
-
N-[2-(4-bromobenzyl)-6-methyl-4-oxo-5-sulfanyloctanoyl]-L-alanine
-
N-[2-(biphenyl-4-ylmethyl)-4-oxo-5-sulfanylhexanoyl]-L-alanine
-
N-[2-(biphenyl-4-ylmethyl)-4-oxo-6-phenyl-5-sulfanylhexanoyl]-L-alanine
-
N-[2-(biphenyl-4-ylmethyl)-6-methyl-4-oxo-5-sulfanyloctanoyl]-L-alanine
-
N-[2-benzyl-6-(4-bromophenyl)-4-oxo-5-sulfanylhexanoyl]-L-leucine
-
N-[5-fluoresceinyl]-N'-[6-(3-mercapto-2-benzyl-1-oxopropyl)amino-1-hexyl]thiocarbamide
-
the inhibitor is a very potent probe for detecting membrane-bound enzyme for biological studies or diagnostic applications. Particularly useful for detecting the membrane-bound enzyme by flow cytometry
N-[N-[1(5)-carboxy-3-(4-hydroxyphenyl)propyl]-(5)-phenylalanyl]-(5)-isoserine
-
-
neurotensin
-
-
omapatrilat
-
opiorphin
-
-
pepstatin
-
-
Phenylglyoxal
-
-
phosphate
-
-
phosphoramidon
PMSF
weak inhibition
puromycin
-
-
sacubitril
-
sacubitrilat
LBQ657, the inhibitor is bound to the active site of NEP by an intricate network of interactions that involves all functional groups of the compound giving rise to the high inhibitory potency. The catalytic zinc atom of NEP is ligated by the side chains of residues His583, His587, and Glu646 with the fourth coordination provided by the carboxylate oxygen adjacent to the P1 methyl of the compound, the backbone amide of LBQ657 forms H-bonding interactions with the side chains of Asn542 and Arg717. Enzyme active site binding structure, interaction, and inhibition mechanism, modelling, overview. All of the molecular interactions between LBQ657 and the enzyme are noncovalent, in line with a reversible inhibition mode
SCH39370
-
-
SCH48446
-
i.e. the diiodo analog of N-[N-[1(5)-carboxy-3-(4-hydroxyphenyl)propyl]-(5)-phenylalanyl]-(5)-isoserine
sialorphin
-
opiorphin homologue inhibits NEP
SQ 28603
-
-
Substance P
-
-
Tat peptide 5118
-
-
tert-butyl 2-([1-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)-4-methoxybutanoate
-
-
thiol
thiorphan
thiorphan-NH2
tris(2-carboxyethyl)phosphine
TCEP, strong inhibition
U46619
a thromboxane mimetic
UK-69,578
-
-
valsartan
Z-Leu-Leu-Leu-H
-
additional information
-