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(VGVAPG)2V + H2O
VGVAPGVGV + APGV + VGVAPG + VGVAPGV
-
human elastin exon 24-derived peptide substrate, hydrolysis by the enzyme occurs when its active site is fully occupied by the substrate, cleavage at Val-Ala and at Gly-Val bonds, the latter to a lesser extent
-
-
?
(VGVAPG)3V + H2O
VGVAPGVGV + APGVGVAPGV + VGVAPGVGVAPGVGV + APGV + VGVAPG + VGVAPGVGVAPGV + GVAPGV
-
human elastin exon 24-derived peptide substrate, hydrolysis by the enzyme occurs when its active site is fully occupied by the substrate, cleavage at Val-Ala and at Gly-Val bonds, the latter to a lesser extent
-
-
?
1-ethyl-3,3-dimethyl-2-[(E)-2-[6-(2,2,3,3,3-pentafluoropropanamido)-2,3-dihydro-1H-xanthen-4-yl]ethenyl]-3H-indol-1-ium + H2O
2-[(E)-2-(6-amino-2,3-dihydro-1H-xanthen-4-yl)ethenyl]-1-ethyl-3,3-dimethyl-3H-indol-1-ium + 2,2,3,3,3-pentafluoropropanal
-
-
-
-
ir
2-(chloroacetyl)-3-naphthoic acid o-toluidide + H2O
?
-
-
-
-
?
2-aminobenzoyl-APEEIMDQQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-APEEI + MDQQ-N-(2,4-dinitrophenyl)ethylenediamine
-
kcat/Km is 136times greater for neutrophil elastase than for proteinase 3
-
-
?
2-aminobenzoyl-APEEIMDRQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-APEEI + MDRQ-N-(2,4-dinitrophenyl)ethylenediamine
-
kcat/Km is 47times greater for neutrophil elastase than for proteinase 3
-
-
?
2-aminobenzoyl-APEEIMDRYQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-APEEI + MDRYQ-N-(2,4-dinitrophenyl)ethylenediamine
-
kcat/Km is 30times greater for neutrophil elastase than for proteinase 3
-
-
?
2-aminobenzoyl-APEEIMDYQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-APEEI + MDYQ-N-(2,4-dinitrophenyl)ethylenediamine
-
kcat/Km is 114times greater for neutrophil elastase than for proteinase 3
-
-
?
2-aminobenzoyl-APEEIMPRQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-APEEI + MPRQ-N-(2,4-dinitrophenyl)ethylenediamine
-
kcat/Km is over 11times greater for neutrophil elastase than for proteinase 3
-
-
?
2-aminobenzoyl-APEEIMRRQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
2-aminobenzoyl-APEEI + MRRQ-N-(2,4-dinitrophenyl)ethylenediamine
-
kcat/Km is over 500times greater for neutrophil elastase than for proteinase 3
-
-
?
4-(2-hydroxyethyl)-1-piperazine ethanesulfonic acid + H2O
?
-
-
-
?
Abz-APEEIMDDQ-ethylene diamine 2,4 dinitrophenyl + H2O
2-aminobenzoyl-APEEI + MDDQ-N-(2,4-dinitrophenyl)ethylenediamine
-
kcat/Km is 45times greater for neutrophil elastase than for proteinase 3
-
-
?
Abz-QPMAVVQSVPQ-EDDnp + H2O
?
-
-
-
-
?
acetyl-Ala-Ala-Ala-p-nitroanilide + H2O
?
acetyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
?
-
-
-
-
?
acetyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
acetyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
-
-
-
?
acetyl-L-Phe-2-naphthyl ester + H2O
acetyl-L-Phe + 2-naphthol
-
-
-
-
?
alpha1-PI + H2O
?
-
important antiprotease of the lung, enzyme reduces the lungs primary protection against proteolysis
-
-
?
Antithrombin III + H2O
?
degradation
-
-
?
APG(VGVAPG)2 + H2O
APGVGV + APGVAPGV + APGVGVAPGVGV + APGVGVAPG + APGV + VGVAPGV
-
human elastin exon 24-derived peptide substrate, hydrolysis by the enzyme occurs when its active site is fully occupied by the substrate, cleavage at Val-Ala and at Gly-Val bonds, the latter to a lesser extent
-
-
?
azocasein + H2O
?
-
-
-
-
?
benzyloxycarbonyl-Ala-3-hydroxy-5-phenylpyrrole + H2O
?
-
-
-
-
?
benzyloxycarbonyl-Ala-4-nitrophenol + H2O
benzyloxycarbonyl-Ala + 4-nitrophenol
-
-
-
-
?
benzyloxycarbonyl-L-Ala 2-naphthyl ester + H2O
benzyloxycarbonyl-Ala + 2-naphthol
-
-
-
-
?
Bovine serum albumin + H2O
?
-
-
-
-
?
BP180/type XVII collagen + H2O
peptide p561 + peptide p506
-
neutrophil elastase degrades recombinant mouse BP180 within the immunodominant extracellular domain at amino acid positions 506 and 561
-
-
?
Cartilage proteoglycan + H2O
?
-
-
-
-
?
CD2 + H2O
?
-
CD2 on peripheral blood T lymphocytes
-
-
?
CD4 + H2O
?
-
CD4 on peripheral blood T lymphocytes
-
-
?
CD8 + H2O
?
-
CD8 on peripheral blood T lymphocytes
-
-
?
coagulation factor V + H2O
?
-
-
-
-
?
coagulation factor VIII + H2O
?
-
-
-
-
?
coagulation factor XI + H2O
?
-
-
-
-
?
coagulation factor XIII + H2O
?
-
-
-
-
?
Collagen type I + H2O
?
-
-
-
-
?
collagen type II + H2O
?
-
-
-
-
?
Collagen type III + H2O
?
-
-
-
-
?
collagen type IV + H2O
?
-
-
-
-
?
collagenase + H2O
?
-
-
-
-
?
complement factor C3 + H2O
?
-
-
-
-
?
complement factor C5 + H2O
?
-
-
-
-
?
complement receptor + H2O
?
-
-
-
-
?
corticosteroid-binding globulin + H2O
?
Cut homeobox 1 + H2O
?
-
-
-
-
?
EMILIN1 + H2O
?
-
-
-
-
?
Factor VIIIa + H2O
?
-
neutrophil elastase inactivates factor VIIIa. The enzyme proteolyses the heavy chain of factor VIIIa into two terminal products, A11-358 and A2375-708, by limited proteolysis at Val358, Val374, and Val708
-
-
?
Fibronectin + H2O
?
-
-
-
-
?
Gelatinase + H2O
?
-
-
-
-
?
gp120 protein + H2O
?
-
-
-
-
?
GRGGAGGRG + H2O
GRGGA + GGRG
-
-
-
-
?
GRGGFGGRG + H2O
GRGGF + GGRG
-
-
-
-
?
GRGGLGGRG + H2O
GRGGL + GGRG
-
-
-
-
?
GRGGRGGRG + H2O
GRGGR + GGRG
-
-
-
-
?
GRGGVGGRG + H2O
GRGGV + GGRG
-
-
-
-
?
heparin-antithrombin complex + H2O
?
-
-
-
-
?
histone H1 + H2O
?
-
-
-
-
?
histone H2A ending on Val114 + H2O
VTIAQGGVLPNIQAV + ?
-
-
-
-
?
histone H4 + H2O
?
-
-
-
-
?
human IgG3 + H2O
?
-
-
-
-
?
human SP-D protein + H2O
SP-D protein peptide fragments
IgA + H2O
?
-
involved in the regulation of inflammation by a feedback mechanism, elastase treated IgA preparations are unable to induce oxidative burst of polymorphonuclear leukocytes
protein cleaved in the hinge region
-
?
IgG + H2O
?
-
involved in the regulation of inflammation by a feedback mechanism, elastase treated IgG preparations are unable to induce oxidative burst of polymorphonuclear leukocytes
protein cleaved in the hinge region
-
?
immunoglobulin A + H2O
?
-
-
-
-
?
immunoglobulin G + H2O
?
-
-
-
-
?
immunoglobulin M + H2O
?
-
-
-
-
?
insulin receptor substrate-1 + H2O
?
-
-
-
-
?
intercellular adesion molecule-1 + H2O
?
-
-
-
-
?
intercellular adhesion molecule-1 + H2O
?
-
-
-
-
?
interleukin-1 + H2O
?
-
-
-
-
?
interleukin-2 + H2O
?
-
-
-
-
?
interleukin-36 receptor antagonist + H2O
activated interleukin-36 receptor antagonist V2 + ?
-
the enzyme cleaves 9 amino acids upstream of the A-X-D consensus of interleukin-36 receptor antagonist
-
-
?
interleukin-6 + H2O
?
-
-
-
-
?
IpaB protein + H2O
?
-
neutrophil elastase cleaves IpaB protein after alanine, valine, isoleucine, or threonine residues
-
-
?
kininogen + H2O
?
-
-
-
-
?
Laminin + H2O
?
-
-
-
-
?
laminin-332 + H2O
?
-
neutrophil elastase shows the greatest activity toward the gamma2 chain of laminin-332, in addition, neutrophil elastase cleaves a synthetic peptide derived from the region of human laminin gamma2 containing the matrix metalloproteinase-2 cleavage site, suggesting that neutrophil elastase may generate laminin-332 fragments that are also promigratory
-
-
?
lung surfactant + H2O
?
-
-
-
-
?
MAAPV-p-nitroanilide + H2O
MAAPV + p-nitroaniline
-
-
-
-
?
major outer membrane protein F + H2O
?
-
-
-
-
?
matrix metalloprotease 9 + H2O
matrix metalloprotease 9 peptide fragments
-
i.e. MMP-9, neutrophil elastase cleaves and activates at two specific cleavage sites, between Val38 and Ala39, and between Ala 39 and Glu40
-
-
?
matrix metalloproteinase-7 + H2O
?
-
human leukocyte elastase may be a natural inactivator of matrix metalloproteinase-7 which can counteract matrix metalloproteinase-7-induced apoptosis resistance
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Ala-4-nitroanilide
?
-
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Ala-thiobenzyl ester
?
-
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-alpha-aminobutyryl-4-nitroanilide + H2O
?
-
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Met-4-nitroanilide + H2O
?
-
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Val-4-methylcoumarin 7-amide + H2O
methoxysuccinyl-Ala-Ala-Pro-Val + 7-amino-4-methylcoumarin
methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
?
methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroanilide
-
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
methoxysuccinyl-Ala-Ala-Pro-Val-7-amido-4-methylcoumarin + H2O
methoxysuccinyl-Ala-Ala-Pro-Val + 7-amino-4-methylcoumarin
-
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Val-thiobenzyl ester
?
-
-
-
-
?
methoxysuccinyl-Ala-Ile-Pro-Met-4-nitroanilide + H2O
?
-
-
-
-
?
methoxysuccinyl-Ala-Pro-Ala-4-nitroanilide
?
-
-
-
-
?
methoxysuccinyl-Ala-Pro-Ala-thiobenzyl ester
?
-
-
-
-
?
methoxysuccinyl-Ala-Pro-Val-4-nitroanilide
?
-
-
-
-
?
methoxysuccinyl-Ala-Pro-Val-thiobenzyl ester
?
-
-
-
-
?
methoxysuccinyl-Pro-Val-4-nitroanilide
?
-
-
-
-
?
methoxysuccinyl-Pro-Val-thiobenzyl ester
?
-
-
-
-
?
methoxysuccinyl-Val-4-nitroanilide
methoxysuccinyl-Val + 4-nitroaniline
-
-
-
-
?
methoxysuccinyl-Val-thiobenzyl ester
?
-
-
-
-
?
N-(4-(4-morpholinylcarbonyl)benzoyl)-Val-Pro-Ile + H2O
?
-
-
-
?
N-methoxy-succinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
N-methoxy-succinyl-Ala-Ala-Pro-Val + 4-nitroaniline
N-methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
N-methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
N-methoxysuccinyl-Ala-Ala-Pro-Val-7-amido-4-methylcoumarin + H2O
N-methoxysuccinyl-Ala-Ala-Pro-Val + 7-amino-4-methylcoumarin
-
-
-
-
?
N-methoxysuccinyl-L-Ala-L-Ala-L-Pro-L-Val-4-nitroanilide + H2O
N-methoxysuccinyl-L-Ala-L-Ala-L-Pro-L-Val + 4-nitroaniline
-
-
-
-
?
N-methoxysuccinyl-L-Ala-L-Ala-L-Pro-L-Val-7-amido-4-methylcoumarin + H2O
N-methoxysuccinyl-L-Ala-L-Ala-L-Pro-L-Val + 7-amino-4-methylcoumarin
-
-
-
-
?
N-succinyl-Ala-Ala-Ala 4-nitroanilide + H2O
N-succinyl-Ala-Ala-Ala + 4-nitroaniline
N-succinyl-Ala-Ala-Ala-4-nitroanilide + H2O
N-succinyl-Ala-Ala-Ala + 4-nitroaniline
-
-
-
-
?
N-succinyl-Ala-Ala-Pro-Phe-4-nitroanilide + H2O
N-succinyl-Ala-Ala-Pro-Phe + 4-nitroaniline
-
-
-
-
?
N-succinyl-Ala-Ala-Val 4-nitroanilide + H2O
N-succinyl-Ala-Ala-Val + 4-nitroaniline
Nalpha-methoxysuccinyl-Nepsilon-2-picolinoyl-L-lysinyl-L-Ala-L-Pro-L-Val 4-nitroanilide + H2O
?
-
-
-
-
?
native type I collagen + H2O
3/4 length fragments similar in size to those produced by interstitial collagenase
-
human, bovine and rat type I collagen, the enzyme can cleave native type I collagen in the helix
-
?
o-aminobenzoic acid-Ala-Pro-Glu-Glu-Ile-Met-Asp-Arg-Gln-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoic acid-Glu-Ala-Ile-Pro-Met-Ser-Ile-Pro-Gln-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoic acid-Glu-Ala-Ile-Pro-Met-Ser-Ile-Pro-Pro-Glu-Val-Lys-Phe-Asn-Lys-Gln-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoic acid-Gly-Ile-Ala-Thr-Phe-Cys-Met-Leu-Met-Pro-Glu-Gln-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoic acid-Ile-Val-Ser-Ala-Arg-Met-Ala-Pro-Glu-Glu-Ile-Ile-Met-Asp-Arg-Gln-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoic acid-Met-Met-Arg-Cys-Ala-Gln-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoic acid-Thr-Phe-Cys-Met-Leu-Glu-Gln-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoic acid-Val-Ala-Asp-Cys-Ala-Gln-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoic acid-Val-Ala-Glu-Cys-Cys-Gln-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoic acid-Val-Ser-Ala-Arg-Gln-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
-
-
-
?
oxidized B chain of insulin + H2O
?
oxytalan fibre + H2O
?
-
the elastase degrades the interfibrillar substances in the periodontal ligament and exposed individual collagen fibrils but not the collagen fibers of the transverse sections of rat mandibular first molars
-
-
?
plasminogen + H2O
?
-
-
-
-
?
plasminogen + H2O
miniplasminogen + ?
-
-
-
-
?
plasminogen activator inhibitor type-1 + H2O
?
-
-
-
-
?
platelet IIb/IIIa receptor + H2O
?
-
-
-
-
?
procarboxypeptidase R + H2O
carboxypeptidase R + ?
-
generation of activated carboxypeptidase R from procarboxypeptidase R by elastase from activated neutrophils at the site of inflammation should contribute to the suppression of excessive inflammation and any abnormality in this mechanism can induce serious hyper-inflammation such as seen in multiple organ failure
-
-
?
progranulin + H2O
?
-
-
-
-
?
progranulin + H2O
granulin + ?
-
-
-
-
?
Protein + H2O
?
-
enzyme capable of degrading proteins of the lung extracellular matrix in vitro
-
-
?
protein C + H2O
small peptides
proteinase-activated receptor 2 N-terminus + H2O
GPNSKGRSLIGRLDTPPPITGKGAPVEPGFSVDEFSAS + VLTGKLTTVFLP
-
-
-
-
?
secretory leucoprotease inhibitor + H2O
?
secretory leukocyte protease inhibitor + H2O
?
-
-
-
?
SLPI + H2O
?
-
important antiprotease of the lung, enzyme reduces the lungs primary protection against proteolysis
-
-
?
SP-D protein + H2O
SP-D protein peptide fragments
succinyl-Ala-Ala-Ala-p-nitroanilide + H2O
succinyl-Ala-Ala-Ala + p-nitroaniline
-
-
-
-
?
succinyl-Ala-Ala-NH-4-nitroanilide + H2O
succinyl-Ala-Ala-NH2 + 4-nitroaniline
succinyl-Ala-Ala-Pro-Ala-4-nitroanilide + H2O
?
-
-
-
-
?
succinyl-Ala-Ala-Pro-Ile-4-nitroanilide + H2O
?
-
-
-
-
?
succinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
?
-
-
-
-
?
succinyl-Tyr-Leu-Val-4-nitroanilide + H2O
?
-
-
-
-
?
syndecan-1 + H2O
?
-
the heparan sulfate moiety of shed syndecan-1 binds and restricts neutrophil elastase from inhibition by alpha-1-antitrypsin
-
-
?
tert-butyloxycarbonyl-Ala-2-naphthyl ester + H2O
tert-butyloxycarbonyl-Ala + 2-naphthol
-
-
-
-
?
tert-butyloxycarbonyl-Ala-4-nitrophenyl ester + H2O
tert-butyloxycarbonyl-Ala + 4-nitrophenol
tert-butyloxycarbonyl-L-Val-4-nitrophenyl ester + H2O
tert-butyloxycarbonyl-L-Val + 4-nitrophenol
-
-
-
-
?
tert-butyloxycarbonyl-Val-4-nitrophenyl ester + H2O
tert-butyloxycarbonyl-Val + 4-nitrophenol
-
-
-
-
?
thrombomodulin + H2O
?
-
-
-
-
?
tissue inhibitor of metalloprotease + H2O
?
-
-
-
-
?
tissue inhibitor of metalloprotease-1 + H2O
tissue inhibitor of metalloprotease-1 peptide fragments
-
i.e. TIMP-1, neutrophil elastase degrades TIMP-1 and cleaves between Val69-Cys70
-
-
?
tissue necrosis factor alpha + H2O
?
-
-
-
-
?
tosyl-Ala-3-hydroxy-5-phenylpyrrole + H2O
?
-
-
-
-
?
tosyl-Ala-4-nitrophenol + H2O
tosyl-Ala + 4-nitrophenol
-
-
-
-
?
tropoelastin + H2O
?
-
-
-
-
?
VAPGVGVAPGV + H2O
VAPGVGV + APGV + VAPGV + GVAPGV
-
human elastin exon 24-derived peptide substrate, hydrolysis by the enzyme occurs when its active site is fully occupied by the substrate, cleavage at Val-Ala and at Gly-Val bonds, the latter to a lesser extent
-
-
?
VLLFSEVL + H2O
VLLF + SEVL
-
-
-
-
?
VLLISEVL + H2O
VLLI + SEVL
-
-
-
-
?
VLLVSEVL + H2O
VLLV + SEVL
-
-
-
-
?
H2 heavy chain of inter-alpha-trypsin inhibitor + H2O
additional information
-
acetyl-Ala-Ala-Ala-p-nitroanilide + H2O
?
-
-
-
-
?
acetyl-Ala-Ala-Ala-p-nitroanilide + H2O
?
-
weak
-
-
?
annexin 1 + H2O
?
-
annexin 1 is externalized and truncated upon adhesion of polymorphonuclear leukocytes to endothelial cells, annexin 1 participates in regulating leukocyte emigration into inflamed tissue through N-terminal peptides generated at inflammatory sites, overview
-
-
?
annexin 1 + H2O
?
-
cleavage of N-terminal peptides, recombinant substrate
-
-
?
antithrombin + H2O
?
-
catalyzes the inactivation of antithrombin by a specific and limited proteinolytic cleavage
-
-
?
antithrombin + H2O
?
-
leukocyte elastase inactivates antithrombin by a specific and limited proteolytic cleavage
-
-
?
Collagen + H2O
?
-
-
-
-
?
Collagen + H2O
?
-
type I, II, III, and IV
-
-
?
Collagen + H2O
?
degradation
-
-
?
corticosteroid-binding globulin + H2O
?
-
cleavage by neutrophil elastase destroys ligand binding capacity and supposedly liberates cortisol at sites of inflammation. Enzyme activity on wild-type and mutant CBG serpin recombinantly produced by 293-EBNA cells, overview. CBG mutant G335V is more sensitive for elastase cleavage, while CBG mutant T342A is more resistant to elastase cleavage
-
-
?
corticosteroid-binding globulin + H2O
?
-
a serpin family of serine protease inhibitor secreted by the liver
-
-
?
elafin + H2O
?
-
-
-
-
?
elafin + H2O
?
-
elafin is cleaved by its cognate enzyme neutrophil elastase, neutrophil elastase-mediated cleavage of elafin abolishes the capacity of the inhibitor to cross-link to fibronectin by transglutamination, neutrophil elastase-mediated cleavages of elafin at Val5-Lys-6 and Val9-Ser10 peptide bonds only occur with 2x excess of neutrophil elastase, a partial cleavage of the inhibitor is identified at the scissile peptide bond Ala24-Met25
-
-
?
Elastin + H2O
?
-
-
-
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, involved in the etiology of emphysema, rheumatoid arthritis, psoriasis, and adult respiratory distress syndrome
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
-
-
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
-
647546, 647548, 647552, 663596, 663821, 663914, 664635, 664846, 664848, 665158, 665458, 665911, 666151, 666152, 696403, 696938, 697329, 697826, 698394, 717369, 717904, 718421, 731106, 731124, 731591, 731788, 731991, 732294, 732438, 732564, 732600, 732758, 732907, 754758 -
-
?
Elastin + H2O
?
-
bovine neck ligament elastin
-
-
?
Elastin + H2O
?
-
the enzyme cleaves elastin selectively near the cross-linking desmosine residues
-
-
?
Elastin + H2O
?
degradation
-
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells also might be damaged, involved in the onset of emphysema and rheumatoid arthritis
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, enzyme is assumed to play a key role in the gradual decrease of lung function during cystic fibrosis
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, involved in the etiology of emphysema, rheumatoid arthritis, psoriasis, and adult respiratory distress syndrome
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, involved in the onset of emphysema, acute respiratory distress syndrome, and rheumatoid arthritis
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
generation of soluble peptides by limited proteolysis, elastin-derived peptides play roles in cell migration, differentiation, proliferation, chemotaxis, tumor progression, and up-regulation of metalloproteinases, the sequence GXXPG is required within the enzyme to stimulate the cellular effects, overview
-
-
?
Elastin + H2O
?
-
human substrate, generation of soluble peptides by limited proteolysis
-
-
?
Elastin + H2O
?
-
-
-
-
?
Elastin + H2O
?
-
-
-
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, involved in the etiology of emphysema, rheumatoid arthritis, psoriasis, and adult respiratory distress syndrome
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
-
-
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, could participate in neutrophil migration
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, involved in the etiology of emphysema, rheumatoid arthritis, psoriasis, and adult respiratory distress syndrome
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, involved in the onset of emphysema and rheumatoid arthritis
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
-
-
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, involved in the etiology of emphysema, rheumatoid arthritis, psoriasis, and adult respiratory distress syndrome
protein cleaved at at least one location
-
?
Fibrin + H2O
?
-
-
-
-
?
Fibrin + H2O
?
degradation
-
-
?
Fibrinogen + H2O
?
-
-
-
-
?
Fibrinogen + H2O
?
degradation
-
-
?
G-CSF receptor + H2O
?
-
neutrophil elastase proteolytically cleaves the G-CSF receptor, G-CSFR, a transmembrane protein, in its extracellular region on neutrophils and blocks G-CSFR-mediated granulopoiesis in vitro, and growth of neutrophils and monocytes, CFU-GM, overview
-
-
?
G-CSF receptor + H2O
?
-
neutrophil elastase proteolytically cleaves the G-CSF receptor, G-CSFR, a transmembrane protein, in its extracellular region on neutrophils and blocks G-CSFR-mediated granulopoiesis in vitro, and growth of neutrophils and monocytes, CFU-GM
-
-
?
human SP-D protein + H2O
SP-D protein peptide fragments
-
-
cleavage product identification by N-terminal sequencing, overview
-
?
human SP-D protein + H2O
SP-D protein peptide fragments
-
cleavage in the lungs of the cystic fibrosis human host, but not in helathy human hosts
cleavage product identification by N-terminal sequencing, overview
-
?
methoxysuccinyl-Ala-Ala-Pro-Val-4-methylcoumarin 7-amide + H2O
methoxysuccinyl-Ala-Ala-Pro-Val + 7-amino-4-methylcoumarin
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Val-4-methylcoumarin 7-amide + H2O
methoxysuccinyl-Ala-Ala-Pro-Val + 7-amino-4-methylcoumarin
-
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
?
-
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
?
-
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
?
-
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
-
-
-
?
mucin + H2O
?
-
proteolysis of mucin is suggested to be involved in cell damaging processes during chronic infection and inflammation of the respiratory tract
-
-
?
mucin + H2O
?
-
hog gastric mucin
-
-
?
N-methoxy-succinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
N-methoxy-succinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
-
-
-
?
N-methoxy-succinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
N-methoxy-succinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
-
-
-
?
N-methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
N-methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
-
-
-
?
N-methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
N-methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
-
663987, 683043, 683056, 683536, 683810, 683956, 697329, 698394, 698834, 699427, 699737, 700570, 701184, 707673, 707710, 707735, 707913, 708387, 708691, 709357, 709363, 709472, 709493, 709989, 717334, 717895, 717904, 718423 -
-
?
N-methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
N-methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
specific neutrophil elastase substrate
-
-
?
N-methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
N-methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
highly specific synthetic substrate for neutrophil elastase
-
-
?
N-methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
N-methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
-
-
-
?
N-methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
N-methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
a fluorogenic enzyme-specific substrate
-
-
?
N-methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
N-methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
-
-
-
?
N-methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
N-methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
highly specific synthetic substrate
-
-
?
N-methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
N-methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
-
-
-
?
N-methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
N-methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
-
-
-
?
N-succinyl-Ala-Ala-Ala 4-nitroanilide + H2O
N-succinyl-Ala-Ala-Ala + 4-nitroaniline
-
-
-
-
?
N-succinyl-Ala-Ala-Ala 4-nitroanilide + H2O
N-succinyl-Ala-Ala-Ala + 4-nitroaniline
-
-
-
-
?
N-succinyl-Ala-Ala-Val 4-nitroanilide + H2O
N-succinyl-Ala-Ala-Val + 4-nitroaniline
-
-
-
-
?
N-succinyl-Ala-Ala-Val 4-nitroanilide + H2O
N-succinyl-Ala-Ala-Val + 4-nitroaniline
-
-
-
-
?
oxidized B chain of insulin + H2O
?
-
-
-
-
?
oxidized B chain of insulin + H2O
?
-
most susceptible bonds are Val12-Glu13, Val18-Cys(O3H)-19. Other bonds hydrolyzed are Ala14-Leu15, Ser9-His10 and Cys(O3H)7-Gly8
-
-
?
oxidized B chain of insulin + H2O
?
-
initial cleavage sites for proteinase 2A and 2B are the Ala14-Leu15 and Val18-Cys19 bonds. Cleavage of the Val12-Glu13 bond is a secondary event resulting from the further cleavage of the primary peptide Phe1-Ala14
-
-
?
protein C + H2O
small peptides
-
the enzyme splits protein C in vitro, and also in vivo degradation of protein C may take place
-
?
protein C + H2O
small peptides
-
the enzyme splits protein C in vitro and also in vivo degradation of protein C may take place
-
?
Proteoglycan + H2O
?
-
-
-
-
?
Proteoglycan + H2O
?
degradation
-
-
?
secretory leucoprotease inhibitor + H2O
?
-
i.e. SLPI, SLPI is cleaved and inactivated by neutrophil elastase in cystic fibrosis lungs
-
-
?
secretory leucoprotease inhibitor + H2O
?
-
i.e. SLPI, recombinant human, a neutrophil serine protease inhibitor, neutrophil elastase cleaves the protein at two sites in the NH2-terminal region and abrogate its ability to bind lipopolysaccharides and NF-kappaB consensus binding sites but not its ability to inhibit activity of the serine protease cathepsin G
-
-
?
SP-D protein + H2O
SP-D protein peptide fragments
-
-
cleavage product identification by N-terminal sequencing, overview
-
?
SP-D protein + H2O
SP-D protein peptide fragments
-
no activity in healthy lungs, but in 50% of cystic fibrosis patient lungs
cleavage product identification by N-terminal sequencing, overview
-
?
succinyl-Ala-Ala-NH-4-nitroanilide + H2O
succinyl-Ala-Ala-NH2 + 4-nitroaniline
-
-
-
-
?
succinyl-Ala-Ala-NH-4-nitroanilide + H2O
succinyl-Ala-Ala-NH2 + 4-nitroaniline
-
-
-
-
?
tert-butyloxycarbonyl-Ala-4-nitrophenyl ester + H2O
tert-butyloxycarbonyl-Ala + 4-nitrophenol
-
-
-
-
?
tert-butyloxycarbonyl-Ala-4-nitrophenyl ester + H2O
tert-butyloxycarbonyl-Ala + 4-nitrophenol
-
-
-
-
?
H2 heavy chain of inter-alpha-trypsin inhibitor + H2O
additional information
-
-
-
early cleavage products consists of heavy chain H1 linked to the light chain, known as bikunin
?
additional information
?
-
-
neutrophil elastase cleaves vascular endothelial growth factor, VEGF, to generate a VEGF fragment with altered activity. Recombinant human VEGF165 is a substrate for the enzyme. The neutrophil elastase-generated VEGF fragment shows significantly reduced binding to VEGF receptor 2 and heparin, yet retains the ability to bind to VEGF receptor 1. The VEGF fragment shows altered signaling in pulmonary artery endothelial cells compared with intact VEGF165, detailed overview. Substrate and product analysis by mass spectrometry. PDGF is also a substrate of neutrophil elastase, while TNFalpha and FGF2 are not
-
-
?
additional information
?
-
-
development of an ELISA for equine neutrophil elastase measurement in EDTA-plasma samples, method development, evaluation, and validation, overview
-
-
?
additional information
?
-
-
catalyzes the inactivation of antithrombin by a specific and limited proteinolytic cleavage
-
-
?
additional information
?
-
-
elastase in contrast to human elastase, may play a minor role in mediating tissue damage and organ failure
-
-
?
additional information
?
-
-
the enzyme may contribute to the intracellular degradation of phagocytized material, its release from activated polymorphonuclear leukocytes into extracellular spaces. The enzyme has been implicated in the pathogenesis of various diseases and is thought to be responsible for tissue damage
-
-
?
additional information
?
-
-
proteolysis of connective tissue by enzymes such as PMN-elastase is a crucial step during inflammation and metastasis
-
-
?
additional information
?
-
-
imbalance between elastase and its endogenous inhibitors may result in several pathophysiological states such as chronic obstructive pulmonary disease, asthma, emphysema, cystic fibrosis and chronic inflammatory diseases
-
-
?
additional information
?
-
-
neutrophil elastase is a key component of the bodys inflammatory defenses, assisting the neutrophil in its migration to the site of inflammation and participating in the proteolytic degradation of invading microorganisms. In addition the enzyme is involved in tissue remodeling and wound healing. Under homeostatic conditions, the destructive effects of the enzyme are limited to the microenvironment immediately surrounding the neutrophil by endogenous proteinase inhibitors such as alpha1-proteinase inhibitor. As a consequence of chronic inflammation, however, the balance between the enzyme and alpha1-antitrypsin can be shifted in favor of the enzyme, resulting in uncontrolled tissue destruction. The enzyme has been implicated in the promotion or exacerbation of a number of diseases including pancreatitis acute respiratory distress syndrome, rheumatoid arthritis, atherosclerosis, pulmonary emphysema and cystic fibrosis
-
-
?
additional information
?
-
-
the enzyme may be involved in a number of important disease states. Including the pulmonary emphysema associated with a hereditary deficiency of alpha1-proteinase inhibitor
-
-
?
additional information
?
-
-
leukocyte elastase induces keratinocyte proliferation by epidermal growth factor receptor activation
-
-
?
additional information
?
-
-
neutrophil elastase induces MUC5AC mucin production in human airway epithelial cells via a cascade involving protein kinase C, reactive oxygen species, and TNF-alpha-converting enzyme
-
-
?
additional information
?
-
-
release of leukocyte elastase and cathepsin G from neutrophils specifically down-regulates the responsiveness of neutrophils to C5a. Elastase and cathepsin play an important role in the down-regulation of acute inflammation
-
-
?
additional information
?
-
-
a massive release of PMN-elastase from neutrophils occurs during surgical procedures, effects on the enzyme of cholecystectomy via laparoscopic or open surgical operation of patients with gallbladder cholethiasis, overview
-
-
?
additional information
?
-
-
inflammatory lung secretions inhibit dendritic cell maturation and function via neutrophil elastase, neutrophil elastase downregulated the expression of CD40, CD80, and CD86, but of not major histocompatibility complex II, on dendritic cells and inhibited LPS-induced dendritic cell maturation, and the the antigen-presenting ability of muring dendritic cells, overview
-
-
?
additional information
?
-
-
neutrophil elastase converts human immature dendritic cells into transforming growth factor-beta1-secreting cells and reduces allostimulatory ability, elastase induces IkappaBalpha degradation in dendritic cells, overview
-
-
?
additional information
?
-
-
neutrophil elastase, a component of the innate host defense system, is bactericidal for Gram-negative bacteria and degrades bacterial virulence factors, resistance of Pseudomonas aeruginosa to the bactericidal effect of neutrophil elastase, as well as this organisms ability to sense this enzymes presence and downregulate the synthesis of a pathogen-associated molecular pattern, may be the key factors in allowing Pseudomonas aeruginosa to colonize the lungs, overview
-
-
?
additional information
?
-
the enzyme digests microbes after phagocytosis in polymorphonuclear neutrophil primary granules, which fuse with neutrophil phagolysosomes, and also acts extracellularly at sites of inflammation, overview, mutations in the human neutrophil elastase gene cause cyclic and congenital neutropenia leading to an immunodeficiency characterized by decreased or oscillating levels of neutrophils in the blood
-
-
?
additional information
?
-
-
the enzyme digests microbes after phagocytosis in polymorphonuclear neutrophil primary granules, which fuse with neutrophil phagolysosomes, and also acts extracellularly at sites of inflammation, overview, mutations in the human neutrophil elastase gene cause cyclic and congenital neutropenia leading to an immunodeficiency characterized by decreased or oscillating levels of neutrophils in the blood
-
-
?
additional information
?
-
-
product determination by mass spectrometry, overview, no activity with elastin exon 24-derived peptide VGVAPGV
-
-
?
additional information
?
-
structure-function relationships, overview
-
-
?
additional information
?
-
-
structure-function relationships, overview
-
-
?
additional information
?
-
-
human neutrophil elastase induces interleukin-8 release from HUVEC cells
-
-
?
additional information
?
-
-
neutrophil elastase possesses potent microbicidal activity, and is speculated to assist with phagocytosis of pathogens by activated neutrophils, moreover, neutrophil elastase can indirectly help the host eradication of pathogens by upregulating the expression of potent antiprotease/antimicrobial agents such as elafin, secretory leukocyte protease inhibitor, and human beta defensin-2
-
-
?
additional information
?
-
-
neutrophil elastase reduces secretion of secretory leukoproteinase inhibitor by lung epithelial cells
-
-
?
additional information
?
-
-
does not cleave N-succinyl-Ala-Ala-Pro-Phe-4-nitroanilide
-
-
?
additional information
?
-
-
leukocyte elastase induces binding activity of NF-kappaB to lung epithelial cells, and induces phosphorylation of p53 on Ser46 and alters its localization. And leukocyte elastase induces expression of PUMA, a p53-upregulated modulator of apoptosis
-
-
?
additional information
?
-
-
leukocyte elastase is an acid endonuclease
-
-
?
additional information
?
-
-
neutrophil elastase does not cleave the N-terminal domains and does not disarm either PAR-1 or PAR-2
-
-
?
additional information
?
-
-
neutrophil elastase induces NF-kappaB activation by p65 in airway smooth muscle, which leads to induction of TGF-beta1. Neutrophil elastase suppresses NF-kappaB response gene IL-8/CXCL8 release and mRNA expression in airway smooth muscle cells at the transcription level mediated by induction of NF-kappaB repressing factor, NRF. In A549 and Beas-2B cells, neutrophil elastase only stimulates NF-kappaB activation by p65 and IL-8/CXCL8 induction, but not NRF, overview
-
-
?
additional information
?
-
-
neutrophil elastase interacts with phosphonoformate immunoassociated protein 5, i.e. PFAAP5 or N4BP2L2, with potential participation in a feedback circuit in which neutrophil elastase regulates its own transcription
-
-
?
additional information
?
-
-
nano-LC tandem mass spectrometry neutrophil elastase cleavage site identification, overview
-
-
?
additional information
?
-
-
the neutrophil elastase is a serine protease
-
-
?
additional information
?
-
-
histone H3 is not degraded by neutrophil elastase
-
-
?
additional information
?
-
-
high concentrations of neutrophil elastase inhibit nuclear decondensation. This autoinhibition can be caused by neutrophil elastase autodegradation
-
-
?
additional information
?
-
substrates with a hydrophobic side chain at P1 are efficiently cleaved and P1-valine is preferred over an alanine or a phenylalanine
-
-
?
additional information
?
-
-
substrates with a hydrophobic side chain at P1 are efficiently cleaved and P1-valine is preferred over an alanine or a phenylalanine
-
-
?
additional information
?
-
-
the enzyme prefers L-Val in the P1 position but also cleaves substrates with L-Ile relatively efficiently and does not cleave after aromatic amino acids
-
-
?
additional information
?
-
-
the protease shows self-cleaving activity
-
-
?
additional information
?
-
-
no activity with succiny-Ala-Ala-Pro-Phe-4-nitroanilide, succiny-Leu-Leu-Val-Tyr-4-nitroanilide, succiny-Ala-Ala-Pro-Leu-4-nitroanilide, succiny-Val-Leu-Gly-Arg-4-nitroanilide, Z-Gly-Pro-Arg-4-nitroanilide, acetyl-Tyr-Val-Ala-Asp-4-nitroanilide, acetyl-Val-Glu-Ile-Asp-4-nitroanilide, and acetyl-Ile-Glu-Pro-Asp-4-nitroanilide
-
-
?
additional information
?
-
-
neutrophil elastase influences the proliferation and differentiation of primary early myeloid cells expressing low levels of PML-retioic acid receptor alpha
-
-
?
additional information
?
-
-
involvement of neutrophil elastase in leukotriene B4-induced neutrophil transmigration in vivo, specific NE inhibitor suppresses neutrophil migration through IL-1beta-stimulated cremasteric venules at the level of the basement membrane
-
-
?
additional information
?
-
-
the enzyme digests microbes after phagocytosis in polymorphonuclear neutrophils, as well as extracellularly, but causes tissue damage and inflammation in the latter case, serine protease inhibitor 6-deficient Spi6 KO mice have increased neutrophil immunity to Pseudomonas aeruginosa, enzyme inhibitor Spi6 protects the cells from self-inflicted damage, the enzyme protects against Pseudomonas aeruginosa infection, overview
-
-
?
additional information
?
-
-
neutrophil elastase is required for maximal intracellular killing of Pseudomonas aeruginosa by neutrophils
-
-
?
additional information
?
-
-
neutrophil elastase cleaves vascular endothelial growth factor, VEGF, to generate a VEGF fragment with altered activity. Recombinant human VEGF165 is a substrate for the enzyme. The neutrophil elastase-generated VEGF fragment, VEGFf, and the wild-type VEGF both activate Akt, and VEGFf appears to be more effective. Substrate and product analysis by mass spectrometry
-
-
?
additional information
?
-
-
the enzyme digests microbes after phagocytosis in polymorphonuclear neutrophils, as well as extracellularly, but causes tissue damage and inflammation in the latter case, serine protease inhibitor 6-deficient Spi6 KO mice have increased neutrophil immunity to Pseudomonas aeruginosa, enzyme inhibitor Spi6 protects the cells from self-inflicted damage, the enzyme protects against Pseudomonas aeruginosa infection, overview
-
-
?
additional information
?
-
-
neutrophils and the elastase thereof play a role in the progression of gut barrier dysfunction during acut alveolar hypoxia, inhibition of neutrophil elastase attenuates gut mucosal injury evoked by acute alveolar hypoxia in rabbits, overview
-
-
?
additional information
?
-
-
elastase in contrast to human elastase, may play a minor role in mediating tissue damage and organ failure
-
-
?
additional information
?
-
-
neutrophil elastase cleaves vascular endothelial growth factor, VEGF, to generate a VEGF fragment with altered activity. Recombinant human VEGF165 is a substrate for the enzyme. The neutrophil elastase-generated VEGF fragment shows significantly reduced binding to VEGF receptor 2 and heparin, yet retains the ability to bind to VEGF receptor 1. Substrate and product analysis by mass spectrometry
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
alpha1-PI + H2O
?
-
important antiprotease of the lung, enzyme reduces the lungs primary protection against proteolysis
-
-
?
annexin 1 + H2O
?
-
annexin 1 is externalized and truncated upon adhesion of polymorphonuclear leukocytes to endothelial cells, annexin 1 participates in regulating leukocyte emigration into inflamed tissue through N-terminal peptides generated at inflammatory sites, overview
-
-
?
Antithrombin III + H2O
?
degradation
-
-
?
BP180/type XVII collagen + H2O
peptide p561 + peptide p506
-
neutrophil elastase degrades recombinant mouse BP180 within the immunodominant extracellular domain at amino acid positions 506 and 561
-
-
?
coagulation factor V + H2O
?
-
-
-
-
?
coagulation factor VIII + H2O
?
-
-
-
-
?
coagulation factor XI + H2O
?
-
-
-
-
?
coagulation factor XIII + H2O
?
-
-
-
-
?
Collagen type I + H2O
?
-
-
-
-
?
collagen type II + H2O
?
-
-
-
-
?
Collagen type III + H2O
?
-
-
-
-
?
collagen type IV + H2O
?
-
-
-
-
?
collagenase + H2O
?
-
-
-
-
?
complement factor C3 + H2O
?
-
-
-
-
?
complement factor C5 + H2O
?
-
-
-
-
?
complement receptor + H2O
?
-
-
-
-
?
corticosteroid-binding globulin + H2O
?
-
cleavage by neutrophil elastase destroys ligand binding capacity and supposedly liberates cortisol at sites of inflammation. Enzyme activity on wild-type and mutant CBG serpin recombinantly produced by 293-EBNA cells, overview. CBG mutant G335V is more sensitive for elastase cleavage, while CBG mutant T342A is more resistant to elastase cleavage
-
-
?
EMILIN1 + H2O
?
-
-
-
-
?
Factor VIIIa + H2O
?
-
neutrophil elastase inactivates factor VIIIa. The enzyme proteolyses the heavy chain of factor VIIIa into two terminal products, A11-358 and A2375-708, by limited proteolysis at Val358, Val374, and Val708
-
-
?
Fibronectin + H2O
?
-
-
-
-
?
G-CSF receptor + H2O
?
-
neutrophil elastase proteolytically cleaves the G-CSF receptor, G-CSFR, a transmembrane protein, in its extracellular region on neutrophils and blocks G-CSFR-mediated granulopoiesis in vitro, and growth of neutrophils and monocytes, CFU-GM, overview
-
-
?
Gelatinase + H2O
?
-
-
-
-
?
gp120 protein + H2O
?
-
-
-
-
?
histone H1 + H2O
?
-
-
-
-
?
histone H2A ending on Val114 + H2O
VTIAQGGVLPNIQAV + ?
-
-
-
-
?
histone H4 + H2O
?
-
-
-
-
?
human SP-D protein + H2O
SP-D protein peptide fragments
-
cleavage in the lungs of the cystic fibrosis human host, but not in helathy human hosts
cleavage product identification by N-terminal sequencing, overview
-
?
IgA + H2O
?
-
involved in the regulation of inflammation by a feedback mechanism, elastase treated IgA preparations are unable to induce oxidative burst of polymorphonuclear leukocytes
protein cleaved in the hinge region
-
?
IgG + H2O
?
-
involved in the regulation of inflammation by a feedback mechanism, elastase treated IgG preparations are unable to induce oxidative burst of polymorphonuclear leukocytes
protein cleaved in the hinge region
-
?
immunoglobulin A + H2O
?
-
-
-
-
?
immunoglobulin G + H2O
?
-
-
-
-
?
immunoglobulin M + H2O
?
-
-
-
-
?
insulin receptor substrate-1 + H2O
?
-
-
-
-
?
intercellular adhesion molecule-1 + H2O
?
-
-
-
-
?
interleukin-1 + H2O
?
-
-
-
-
?
interleukin-2 + H2O
?
-
-
-
-
?
interleukin-36 receptor antagonist + H2O
activated interleukin-36 receptor antagonist V2 + ?
-
the enzyme cleaves 9 amino acids upstream of the A-X-D consensus of interleukin-36 receptor antagonist
-
-
?
interleukin-6 + H2O
?
-
-
-
-
?
IpaB protein + H2O
?
-
neutrophil elastase cleaves IpaB protein after alanine, valine, isoleucine, or threonine residues
-
-
?
kininogen + H2O
?
-
-
-
-
?
Laminin + H2O
?
-
-
-
-
?
lung surfactant + H2O
?
-
-
-
-
?
major outer membrane protein F + H2O
?
-
-
-
-
?
methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroanilide
-
-
-
-
?
mucin + H2O
?
-
proteolysis of mucin is suggested to be involved in cell damaging processes during chronic infection and inflammation of the respiratory tract
-
-
?
oxytalan fibre + H2O
?
-
the elastase degrades the interfibrillar substances in the periodontal ligament and exposed individual collagen fibrils but not the collagen fibers of the transverse sections of rat mandibular first molars
-
-
?
plasminogen + H2O
?
-
-
-
-
?
plasminogen + H2O
miniplasminogen + ?
-
-
-
-
?
plasminogen activator inhibitor type-1 + H2O
?
-
-
-
-
?
platelet IIb/IIIa receptor + H2O
?
-
-
-
-
?
procarboxypeptidase R + H2O
carboxypeptidase R + ?
-
generation of activated carboxypeptidase R from procarboxypeptidase R by elastase from activated neutrophils at the site of inflammation should contribute to the suppression of excessive inflammation and any abnormality in this mechanism can induce serious hyper-inflammation such as seen in multiple organ failure
-
-
?
progranulin + H2O
?
-
-
-
-
?
progranulin + H2O
granulin + ?
-
-
-
-
?
protein C + H2O
small peptides
-
the enzyme splits protein C in vitro and also in vivo degradation of protein C may take place
-
?
proteinase-activated receptor 2 N-terminus + H2O
GPNSKGRSLIGRLDTPPPITGKGAPVEPGFSVDEFSAS + VLTGKLTTVFLP
-
-
-
-
?
secretory leucoprotease inhibitor + H2O
?
-
i.e. SLPI, SLPI is cleaved and inactivated by neutrophil elastase in cystic fibrosis lungs
-
-
?
SLPI + H2O
?
-
important antiprotease of the lung, enzyme reduces the lungs primary protection against proteolysis
-
-
?
SP-D protein + H2O
SP-D protein peptide fragments
-
no activity in healthy lungs, but in 50% of cystic fibrosis patient lungs
cleavage product identification by N-terminal sequencing, overview
-
?
thrombomodulin + H2O
?
-
-
-
-
?
tissue inhibitor of metalloprotease + H2O
?
-
-
-
-
?
tissue necrosis factor alpha + H2O
?
-
-
-
-
?
tropoelastin + H2O
?
-
-
-
-
?
additional information
?
-
Collagen + H2O
?
-
-
-
-
?
Collagen + H2O
?
degradation
-
-
?
elafin + H2O
?
-
-
-
-
?
elafin + H2O
?
-
elafin is cleaved by its cognate enzyme neutrophil elastase, neutrophil elastase-mediated cleavage of elafin abolishes the capacity of the inhibitor to cross-link to fibronectin by transglutamination, neutrophil elastase-mediated cleavages of elafin at Val5-Lys-6 and Val9-Ser10 peptide bonds only occur with 2x excess of neutrophil elastase, a partial cleavage of the inhibitor is identified at the scissile peptide bond Ala24-Met25
-
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, involved in the etiology of emphysema, rheumatoid arthritis, psoriasis, and adult respiratory distress syndrome
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
-
697329, 697826, 698394, 717369, 717904, 718421, 731106, 731124, 731591, 731788, 731991, 732294, 732438, 732564, 732600, 732758, 732907, 754758 -
-
?
Elastin + H2O
?
degradation
-
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells also might be damaged, involved in the onset of emphysema and rheumatoid arthritis
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, enzyme is assumed to play a key role in the gradual decrease of lung function during cystic fibrosis
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, involved in the etiology of emphysema, rheumatoid arthritis, psoriasis, and adult respiratory distress syndrome
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, involved in the onset of emphysema, acute respiratory distress syndrome, and rheumatoid arthritis
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
generation of soluble peptides by limited proteolysis, elastin-derived peptides play roles in cell migration, differentiation, proliferation, chemotaxis, tumor progression, and up-regulation of metalloproteinases, the sequence GXXPG is required within the enzyme to stimulate the cellular effects, overview
-
-
?
Elastin + H2O
?
-
-
-
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, involved in the etiology of emphysema, rheumatoid arthritis, psoriasis, and adult respiratory distress syndrome
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, could participate in neutrophil migration
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, involved in the etiology of emphysema, rheumatoid arthritis, psoriasis, and adult respiratory distress syndrome
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, involved in the onset of emphysema and rheumatoid arthritis
protein cleaved at at least one location
-
?
Elastin + H2O
?
-
involved in lung defense against bacterial infection, due to the ability of the enzyme to cleave cell surface proteins, body cells might also be damaged, involved in the etiology of emphysema, rheumatoid arthritis, psoriasis, and adult respiratory distress syndrome
protein cleaved at at least one location
-
?
Fibrin + H2O
?
-
-
-
-
?
Fibrin + H2O
?
degradation
-
-
?
Fibrinogen + H2O
?
-
-
-
-
?
Fibrinogen + H2O
?
degradation
-
-
?
Proteoglycan + H2O
?
-
-
-
-
?
Proteoglycan + H2O
?
degradation
-
-
?
additional information
?
-
-
catalyzes the inactivation of antithrombin by a specific and limited proteinolytic cleavage
-
-
?
additional information
?
-
-
elastase in contrast to human elastase, may play a minor role in mediating tissue damage and organ failure
-
-
?
additional information
?
-
-
the enzyme may contribute to the intracellular degradation of phagocytized material, its release from activated polymorphonuclear leukocytes into extracellular spaces. The enzyme has been implicated in the pathogenesis of various diseases and is thought to be responsible for tissue damage
-
-
?
additional information
?
-
-
proteolysis of connective tissue by enzymes such as PMN-elastase is a crucial step during inflammation and metastasis
-
-
?
additional information
?
-
-
imbalance between elastase and its endogenous inhibitors may result in several pathophysiological states such as chronic obstructive pulmonary disease, asthma, emphysema, cystic fibrosis and chronic inflammatory diseases
-
-
?
additional information
?
-
-
neutrophil elastase is a key component of the bodys inflammatory defenses, assisting the neutrophil in its migration to the site of inflammation and participating in the proteolytic degradation of invading microorganisms. In addition the enzyme is involved in tissue remodeling and wound healing. Under homeostatic conditions, the destructive effects of the enzyme are limited to the microenvironment immediately surrounding the neutrophil by endogenous proteinase inhibitors such as alpha1-proteinase inhibitor. As a consequence of chronic inflammation, however, the balance between the enzyme and alpha1-antitrypsin can be shifted in favor of the enzyme, resulting in uncontrolled tissue destruction. The enzyme has been implicated in the promotion or exacerbation of a number of diseases including pancreatitis acute respiratory distress syndrome, rheumatoid arthritis, atherosclerosis, pulmonary emphysema and cystic fibrosis
-
-
?
additional information
?
-
-
the enzyme may be involved in a number of important disease states. Including the pulmonary emphysema associated with a hereditary deficiency of alpha1-proteinase inhibitor
-
-
?
additional information
?
-
-
leukocyte elastase induces keratinocyte proliferation by epidermal growth factor receptor activation
-
-
?
additional information
?
-
-
neutrophil elastase induces MUC5AC mucin production in human airway epithelial cells via a cascade involving protein kinase C, reactive oxygen species, and TNF-alpha-converting enzyme
-
-
?
additional information
?
-
-
release of leukocyte elastase and cathepsin G from neutrophils specifically down-regulates the responsiveness of neutrophils to C5a. Elastase and cathepsin play an important role in the down-regulation of acute inflammation
-
-
?
additional information
?
-
-
a massive release of PMN-elastase from neutrophils occurs during surgical procedures, effects on the enzyme of cholecystectomy via laparoscopic or open surgical operation of patients with gallbladder cholethiasis, overview
-
-
?
additional information
?
-
-
inflammatory lung secretions inhibit dendritic cell maturation and function via neutrophil elastase, neutrophil elastase downregulated the expression of CD40, CD80, and CD86, but of not major histocompatibility complex II, on dendritic cells and inhibited LPS-induced dendritic cell maturation, and the the antigen-presenting ability of muring dendritic cells, overview
-
-
?
additional information
?
-
-
neutrophil elastase converts human immature dendritic cells into transforming growth factor-beta1-secreting cells and reduces allostimulatory ability, elastase induces IkappaBalpha degradation in dendritic cells, overview
-
-
?
additional information
?
-
-
neutrophil elastase, a component of the innate host defense system, is bactericidal for Gram-negative bacteria and degrades bacterial virulence factors, resistance of Pseudomonas aeruginosa to the bactericidal effect of neutrophil elastase, as well as this organisms ability to sense this enzymes presence and downregulate the synthesis of a pathogen-associated molecular pattern, may be the key factors in allowing Pseudomonas aeruginosa to colonize the lungs, overview
-
-
?
additional information
?
-
the enzyme digests microbes after phagocytosis in polymorphonuclear neutrophil primary granules, which fuse with neutrophil phagolysosomes, and also acts extracellularly at sites of inflammation, overview, mutations in the human neutrophil elastase gene cause cyclic and congenital neutropenia leading to an immunodeficiency characterized by decreased or oscillating levels of neutrophils in the blood
-
-
?
additional information
?
-
-
the enzyme digests microbes after phagocytosis in polymorphonuclear neutrophil primary granules, which fuse with neutrophil phagolysosomes, and also acts extracellularly at sites of inflammation, overview, mutations in the human neutrophil elastase gene cause cyclic and congenital neutropenia leading to an immunodeficiency characterized by decreased or oscillating levels of neutrophils in the blood
-
-
?
additional information
?
-
-
human neutrophil elastase induces interleukin-8 release from HUVEC cells
-
-
?
additional information
?
-
-
neutrophil elastase possesses potent microbicidal activity, and is speculated to assist with phagocytosis of pathogens by activated neutrophils, moreover, neutrophil elastase can indirectly help the host eradication of pathogens by upregulating the expression of potent antiprotease/antimicrobial agents such as elafin, secretory leukocyte protease inhibitor, and human beta defensin-2
-
-
?
additional information
?
-
-
neutrophil elastase reduces secretion of secretory leukoproteinase inhibitor by lung epithelial cells
-
-
?
additional information
?
-
-
leukocyte elastase induces binding activity of NF-kappaB to lung epithelial cells, and induces phosphorylation of p53 on Ser46 and alters its localization. And leukocyte elastase induces expression of PUMA, a p53-upregulated modulator of apoptosis
-
-
?
additional information
?
-
-
leukocyte elastase is an acid endonuclease
-
-
?
additional information
?
-
-
neutrophil elastase does not cleave the N-terminal domains and does not disarm either PAR-1 or PAR-2
-
-
?
additional information
?
-
-
neutrophil elastase induces NF-kappaB activation by p65 in airway smooth muscle, which leads to induction of TGF-beta1. Neutrophil elastase suppresses NF-kappaB response gene IL-8/CXCL8 release and mRNA expression in airway smooth muscle cells at the transcription level mediated by induction of NF-kappaB repressing factor, NRF. In A549 and Beas-2B cells, neutrophil elastase only stimulates NF-kappaB activation by p65 and IL-8/CXCL8 induction, but not NRF, overview
-
-
?
additional information
?
-
-
neutrophil elastase interacts with phosphonoformate immunoassociated protein 5, i.e. PFAAP5 or N4BP2L2, with potential participation in a feedback circuit in which neutrophil elastase regulates its own transcription
-
-
?
additional information
?
-
-
histone H3 is not degraded by neutrophil elastase
-
-
?
additional information
?
-
-
the enzyme prefers L-Val in the P1 position but also cleaves substrates with L-Ile relatively efficiently and does not cleave after aromatic amino acids
-
-
?
additional information
?
-
-
the protease shows self-cleaving activity
-
-
?
additional information
?
-
-
neutrophil elastase influences the proliferation and differentiation of primary early myeloid cells expressing low levels of PML-retioic acid receptor alpha
-
-
?
additional information
?
-
-
involvement of neutrophil elastase in leukotriene B4-induced neutrophil transmigration in vivo, specific NE inhibitor suppresses neutrophil migration through IL-1beta-stimulated cremasteric venules at the level of the basement membrane
-
-
?
additional information
?
-
-
the enzyme digests microbes after phagocytosis in polymorphonuclear neutrophils, as well as extracellularly, but causes tissue damage and inflammation in the latter case, serine protease inhibitor 6-deficient Spi6 KO mice have increased neutrophil immunity to Pseudomonas aeruginosa, enzyme inhibitor Spi6 protects the cells from self-inflicted damage, the enzyme protects against Pseudomonas aeruginosa infection, overview
-
-
?
additional information
?
-
-
neutrophil elastase is required for maximal intracellular killing of Pseudomonas aeruginosa by neutrophils
-
-
?
additional information
?
-
-
the enzyme digests microbes after phagocytosis in polymorphonuclear neutrophils, as well as extracellularly, but causes tissue damage and inflammation in the latter case, serine protease inhibitor 6-deficient Spi6 KO mice have increased neutrophil immunity to Pseudomonas aeruginosa, enzyme inhibitor Spi6 protects the cells from self-inflicted damage, the enzyme protects against Pseudomonas aeruginosa infection, overview
-
-
?
additional information
?
-
-
neutrophils and the elastase thereof play a role in the progression of gut barrier dysfunction during acut alveolar hypoxia, inhibition of neutrophil elastase attenuates gut mucosal injury evoked by acute alveolar hypoxia in rabbits, overview
-
-
?
additional information
?
-
-
elastase in contrast to human elastase, may play a minor role in mediating tissue damage and organ failure
-
-
?
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((6R,7S)-2-{[(2S)-2-(dihydroxymethyl)pyrrolidin-1-yl]carbonyl}-7-methoxy-5,5-dioxido-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl)methyl acetate
-
-
(-)-epigallocatechin-3-gallate
-
-
(1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl)methyl 2,6-dichlorobenzoate
-
-
(1-{1-Methyl-2-oxo-2-[2-(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidin-1-yl]-ethylcarbamoyl}-ethyl)-carbamic acid benzyl ester
-
-
(1-{2-[1-(4,5-Dihydro-oxazole-2-carbonyl)-2-methyl-propylcarbamoyl]-pyrrolidine-1-carbonyl}-2-methyl-propyl)-carbamic acid benzyl ester
-
-
(1-{2-[1-(Benzooxazol-2-yl-hydroxy-methyl)-2-methyl-propylcarbamoyl]-pyrrolidine-1-carbonyl}-2-methyl-propyl)-carbamic acid benzyl ester
-
-
(1-{2-[1-(Benzooxazole-2-carbonyl)-2-methyl-propylcarbamoyl]-pyrrolidine-1-carbonyl}-2-methyl-propyl)-carbamic acid benzyl ester
-
-
(1-{2-[2-(3,3-Difluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidin-1-yl]-1-methyl-2-oxo-ethylcarbamoyl}-ethyl)-carbamic acid benzyl ester
-
-
(1-{[1-(2-tert-Butoxycarbonylamino-3-methyl-butyryl)-pyrrolidine-2-carbonyl]-amino}-2-methyl-propyl)-phosphonic acid diphenyl ester
-
-
(2-(3,5-bis-trifluoromethyl-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
(2-(3,5-difluoro-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
(2-(4-amino-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
(2-(4-chloro-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
(2-(4-formylamino-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
(2-(4-methoxy-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
(2-(4-nitro-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
(2-cyclohexyl-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
(2-isopropyl-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
(22E,24R)-ergosta-7,22-dien-2alpha,3alpha,9alpha-triol
-
-
(2R, 3R)-6-methyl-3'-geranyl-2,3-trans-5,7,4'-trihydroxyflavonol
-
-
(2S)-1-({(6R,7S)-3-[(acetyloxy)methyl]-7-methoxy-5,5-dioxido-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-2-yl}carbonyl)pyrrolidine-2-carboxylic acid
-
-
(3-methylindazol-1-yl)-m-tolyl-methanone
-
-
(3beta,5alpha,8alpha,22E)-ergosta-6,22-diene-3-ol-5,8-peroxide
-
-
(3beta,5alpha,8alpha,22E)-ergosta-6,22-diene-3-ol-5,8-peroxide 3-O-beta-D-glucoside
-
-
(3R)-1-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-3-carboxylic acid
-
-
(3S)-1-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-3-carboxylic acid
-
-
(4-tert-butyl-1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl)methyl 2,6-dichlorobenzoate
-
-
(5-Benzyloxycarbonylamino-1-{2-methyl-1-[2-(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidine-1-carbonyl]-propylcarbamoyl}-pentyl)-carbamic acid benzyl ester
-
-
(5E)-3-benzyl-5-but-2-ynylidenedihydrofuran-2(3H)-one
-
-
(5E)-3-benzyl-5-prop-2-ynylidenedihydrofuran-2(3H)-one
-
-
(5E)-3-butyl-5-prop-2-ynylidenedihydrofuran-2(3H)-one
-
-
(5E)-5-prop-2-ynylidenedihydrofuran-2(3H)-one
-
-
(5Z)-3-benzyl-5-prop-2-ynylidenedihydrofuran-2(3H)-one
-
-
(6-oxo-2-(4-fluorophenyl)-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
(6-oxo-2-phenyl-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
(6-oxo-2-pyridin-3-yl-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
(6-oxo-2-thiophen-2-yl-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
(6-oxo-2-[4-(2,2,2-trifluoro-acetylamino)-phenyl]-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
(6E)-3-benzyl-6-prop-2-ynylidenetetrahydro-2H-pyran-2-one
-
-
(6E)-6-(1-bromoethylidene)-3-isopropyltetrahydro-2H-pyran-2-one
-
-
(6E)-6-(bromomethylene)-3-isopropyltetrahydro-2H-pyran-2-one
-
-
(6R,7S)-3-[(acetyloxy)methyl]-7-methoxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid 5,5-dioxide
-
-
(6Z)-3-benzyl-6-prop-2-ynylidenetetrahydro-2H-pyran-2-one
-
-
(6Z)-6-(bromomethylene)-3-isopropyltetrahydro-2H-pyran-2-one
-
-
(E)-3-(3-(3,7-dimethylocta-2,6-dienyl)-2,4-dihydroxyphenyl)-3,5,7-trihydroxy-chroman-4-one
-
competitive inhibitor
(E)-6-O-p-coumaroyl scandoside methyl ester
-
an iridoid glycoside isolated from the methanolic extract of Hedyotis diffusa, usage of air-dried whole plant
(E)-6-O-p-feruloyl scandoside methyl ester
-
an iridoid glycoside isolated from the methanolic extract of Hedyotis diffusa, usage of air-dried whole plant
(E)-6-O-p-methoxycinnamoyl scandoside methyl ester
-
an iridoid glycoside isolated from the methanolic extract of Hedyotis diffusa, usage of air-dried whole plant. Molecular docking simulation and structural model for the inhibition of human neutrophil elastase, overview
(R)-3-phenyl-2-(1,1,3-trioxo-1,3-dihydro-1lambda6-1,2-benzisothiazol-2-yl-methanesulfonylamino)-propionic acid methyl ester
-
-
(S)-1-[(S)-2-(4-methoxybenzamido)-3-methylbutyryl]-N-[(S)-2-methyl-1-(trifluoroacetyl)propyl]pyrrolidine-2-carboxamide
-
-
(S)-3-phenyl-2-(1,1,3-trioxo-1,3-dihydro-1lambda6-1,2-benzisothiazol-2-yl-methanesulfonylamino)-propionic acid methyl ester
-
-
(Z)-6-O-p-coumaroyl scandoside methyl ester
-
an iridoid glycoside isolated from the methanolic extract of Hedyotis diffusa, usage of air-dried whole plant
(Z)-6-O-p-methoxycinnamoyl scandoside methyl ester
-
an iridoid glycoside isolated from the methanolic extract of Hedyotis diffusa, usage of air-dried whole plant
1(6H)-Pyrimidineacetamide, 2-(4-aminophenyl)-5-[(methylsulfonyl)amino]-6-oxo-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
-
1(6H)-Pyrimidineacetamide, 2-(4-fluorophenyl)-5-(methylamino)-6-oxo-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
-
1(6H)-Pyrimidineacetamide, 5-(ethylamino)-6-oxo-2-(2-thienyl)-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
-
1(6H)-Pyrimidineacetamide, 5-(formylamino)-6-oxo-2-(2-thienyl)-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
-
1(6H)-Pyrimidineacetamide, 5-amino-2-(4-fluorophenyl)-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]-6-oxo-
-
-
1(6H)-Pyrimidineacetamide, 5-amino-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]-6-oxo-2-(2-thienyl)-
-
-
1(6H)-Pyrimidineacetamide, 5-[[(cyclohexylamino)sulfonyl]amino]-2-(4-fluorophenyl)-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]-6-oxo-
-
-
1(6H)-Pyrimidineacetamide, 6-oxo-2-phenyl-5-[(trifluoroacetyl)amino]-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
-
1,2,5-thiadiazolidin-3-one 1,1-dioxide
-
the inhibitor causes rapid, time-dependent, irreversible loss of enzymatic activity
1-(2-((1-methyl-1H-imidazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione
-
-
1-(2-((5-phenyl-1,3,4-oxadiazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione
-
-
1-(2-((benzo[d]oxazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione
-
-
1-(2-((benzo[d]thiazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione
-
-
1-(2-Acetylamino-propionyl)-pyrrolidine-2-carboxylic acid (3-chloro-1-methyl-2-oxo-propyl)-amide
-
-
1-(2-methylbenzoyl)-1H-indazole-3-carboxylic acid phenylamide
-
-
1-(3-aminobenzoyl)-1H-indazole-3-carboxylic acid ethyl ester
-
-
1-(3-aminobenzoyl)-1H-indazole-3-carboxylic acid phenylamide
-
-
1-(3-methoxybenzoyl)-1H-indazole-3-carboxylic acid ethyl ester
-
-
1-(3-methoxybenzoyl)-1H-indazole-3-carboxylic acid methyl ester
-
-
1-(3-methoxybenzoyl)-1H-indazole-3-carboxylic acid phenylamide
-
-
1-(3-methoxybenzoyl)-1H-indazole-3-carboxylic acid propyl ester
-
-
1-(3-methylbenzoyl)-1H-indazole-3-carboxylic acid methyl ester
-
-
1-(4-((5-phenyl-1,3,4-oxadiazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione
-
-
1-(4-((benzo[d]oxazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione
-
-
1-(4-((benzo[d]thiazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione
-
-
1-(4-chlorophenyl)-3,3-diethylazetidine-2,4-dione
-
-
1-(4-chlorophenyl)-3,3-dimethylazetidine-2,4-dione
-
-
1-(4-cyanobenzoyl)-1H-indazole-3-carboxylic acid ethyl ester
-
-
1-(6-((benzo[d]thiazol-2-ylthio)methyl)pyridin-3-yl)-3,3-diethylazetidine-2,4-dione
-
-
1-(pyridine-4-carbonyl)-1H-indazole-3-carboxylic acid phenylamide
-
-
1-(thiophene-3-carbonyl)-1H-indazole-3-carboxylic acid ethyl ester
-
-
1-(thiophene-3-carbonyl)-1H-indazole-3-carboxylic acid methyl ester
-
-
1-(thiophene-3-carbonyl)-1H-indazole-3-carboxylic acid phenylamide
-
-
1-(thiophene-3-carbonyl)-1H-indazole-3-carboxylic acid propyl ester
-
-
1-benzoyl-1H-indazole-3-carboxylic acid methyl ester
-
-
1-benzoyl-1H-indazole-3-carboxylic acid phenylamide
-
-
1-benzyl-3,3-dimethylazetidine-2,4-dione
-
-
1-butyryl-1H-indazole-3-carboxylic acid ethyl ester
-
-
1-cyclopentanecarbonyl-1H-indazole-3-carboxylic acid ethyl ester
-
-
1-methyl-1H-tetrazole-5-thiol
-
-
1-propionyl-1H-indazole-3-carboxylic acid ethyl ester
-
-
1-[(3-chlorophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
-
-
1-[(3-fluorophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
-
-
1-[(3-methylphenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
-
-
1-[(3-nitrophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
-
-
1-[(4-chlorophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
-
-
1-[(4-cyanophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
-
-
1-[(4-fluorophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
-
-
1-[(4-methylphenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
-
-
1-[(methylsulfonyl)oxy]pyrrolidine-2,5-dione
-
-
1-[2-(2-Acetylamino-propionylamino)-propionyl]-pyrrolidine-2-carboxylic acid (3-chloro-1-isopropyl-2-oxo-propyl)-amide
-
-
1-[2-(2-Acetylamino-propionylamino)-propionyl]-pyrrolidine-2-carboxylic acid (3-chloro-1-methyl-2-oxo-propyl)-amide
-
-
1-[2-(4-Benzenesulfonylaminocarbonyl-benzoylamino)-3-methyl-butyryl]-pyrrolidine-2-carboxylic acid (3,3-difluoro-1-isopropyl-2-oxo-3-phenethylcarbamoyl-propyl)-amide
-
-
1-[2-(chloromethyl)phenyl]-3,3-difluoroazetidin-2-one
-
-
1-[3-(5-cyclobutyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
-
-
1-[3-(5-cyclopropyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
-
-
1-[3-(5-ethyl-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
-
-
1-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
-
-
1-[3-(5-methyl-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
-
-
1-[3-(7-methoxy-4-oxo-5-propyl-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
-
-
1-[3-[7-methoxy-4-oxo-5-(propan-2-yl)-4H-3,1-benzoxazin-2-yl]pyridin-2-yl]piperidine-4-carboxylic acid
-
-
1-{2-[4-(4-Bromo-benzenesulfonylaminocarbonyl)-benzoylamino]-3-methyl-butyryl}-pyrrolidine-2-carboxylic acid (3,3,3-trifluoro-1-isopropyl-2-oxo-propyl)-amide
-
-
1-{2-[4-(4-Chloro-benzenesulfonylaminocarbonyl)-benzoylamino]-3-methyl-butyryl}-pyrrolidine-2-carboxylic acid (1-isopropyl-2,3-dioxo-heptyl)-amide
-
-
1-{2-[4-(4-Chloro-benzenesulfonylaminocarbonyl)-benzoylamino]-3-methyl-butyryl}-pyrrolidine-2-carboxylic acid (3,3,3-trifluoro-1-isopropyl-2-oxo-propyl)-amide
-
-
1-{3-Methyl-2-[(naphthalene-2-carbonyl)-amino]-butyryl}-pyrrolidine-2-carboxylic acid (1-isopropyl-2,3-dioxo-heptyl)-amide
-
-
1-{[({2-[3-(trifluoromethyl)phenyl]ethyl}amino)carbonyl]oxy}pyrrolidine-2,5-dione
-
-
14alpha-hydroxy-ergosta-4,7,9(11),22-tetraen-3,6-dione
-
-
1H-indazol-1-yl(3-methylphenyl)methanone
-
-
2,2,2-trifluoroethyl 1-(phenylcarbonyl)-1H-indazole-3-carboxylate
-
-
2,2,2-trifluoroethyl 1-(thiophen-3-ylcarbonyl)-1H-indazole-3-carboxylate
-
-
2,2,2-trifluoroethyl 1-[(3-aminophenyl)carbonyl]-1H-indazole-3-carboxylate
-
-
2,2,2-trifluoroethyl 1-[(3-methoxyphenyl)carbonyl]-1H-indazole-3-carboxylate
-
-
2,2,2-trifluoroethyl 1-[(3-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
-
-
2,2-Dimethyl-propionic acid 4-[2-(2,2-dihydroxy-ethylcarbamoyl)-benzenesulfonylamino]-phenyl ester
-
-
2,2-Dimethyl-propionic acid 4-[4-(2,2-dimethyl-propionyloxy)-benzoyl]-phenyl ester
-
-
2,3-dihydro-6-[3-(2-hydroxymethyl)-phenyl-2-propenyl]5-benzofuranol
-
the synthetic inhibitor may provide a new and useful therapeutic for the treatment of diseases characterized by polymorphonuclear elastase involvement
2-(2,4-dinitrophenyl)-1,2-benzisothiazol-3(2H)-one 1,1-dioxide
-
-
2-(2-ethylbutanoyl)-1,2-benzisothiazol-3(2H)-one
-
-
2-(2-furoyl)-1,2-benzisothiazol-3(2H)-one
-
-
2-(2-furoyl)-1,2-benzisothiazol-3(2H)-one 1,1-dioxide
-
-
2-(2-methoxypyridin-3-yl)-5-methyl-4H-3,1-benzoxazin-4-one
-
-
2-(2-phenoxypyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
-
2-(2-[4-[2-(dimethylamino)ethyl]piperazin-1-yl]pyridin-3-yl)-5-ethyl-7-methoxy-4H-3,1-benzoxazin-4-one
-
-
2-(2-[[2-(dimethylamino)ethyl](methyl)amino]pyridin-3-yl)-5-methyl-4H-3,1-benzoxazin-4-one
-
-
2-(2-[[2-(dimethylamino)ethyl]amino]pyridin-3-yl)-5-methyl-4H-3,1-benzoxazin-4-one
-
-
2-(3,3,3-Trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidine-1-carboxylic acid benzyl ester
-
-
2-(3-trifluoromethylphenylamino)-4H-thieno[2,3-d][1,3]oxazin-4-one
-
-
2-(4-(3,3-diethyl-2,4-dioxoazetidin-1-yl)benzylthio)benzo[d ]-oxazole-6-carboxylic acid
-
-
2-(4-Chloro-benzenesulfonylamino)-5,5-dihydroxy-pentanoic acid (2-isopropylamino-5-methyl-4-oxo-4H-benzo[d][1,3]oxazin-7-yl)-amide
-
-
2-(4-Dihydroxymethyl-phenoxy)-3,3-diethyl-4-oxo-azetidine-1-carboxylic acid 4-methyl-benzylamide
-
-
2-(5-amino-6-oxo-2-thien-2-ylpyrimidin-1(6H)-yl)-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide
-
-
2-(chloromethyl)-1,2-benzisothiazol-3(2H)-one 1,1-dioxide
-
-
2-(thiophen-2-ylcarbonylthio)-N-(2-oxo-2,3,4,5-tetrahydrothiophen-3-yl)propionamide
-
reversible, slow-binding, fully competitive
2-(trifluoromethyl)-4H-3,1-benzoxazin-4-one
-
-
2-Acetylamino-N-(1-ethylcarbamoyl-ethyl)-propionamide
-
-
2-Acetylamino-N-[1-(3-chloro-1-methyl-2-oxo-propylcarbamoyl)-ethyl]-propionamide
-
-
2-Acetylamino-N-[2-(2-{2-[(2-chloro-acetyl)-isopropyl-amino]-acetyl}-pyrrolidin-1-yl)-1-methyl-2-oxo-ethyl]-propionamide
-
-
2-Acetylamino-N-{1-[1-(3-chloro-1-methyl-2-oxo-propylcarbamoyl)-ethylcarbamoyl]-ethyl}-propionamide
-
-
2-amino-4H-3,1-benzoxazin-4-one
-
-
2-amino-5-ethyl-4H-3,1-benzoxazin-4-one
-
-
2-benzoyl-1,2-benzisothiazol-3(2H)-one 1,1-dioxide
-
-
2-CF3CF2C(O)NH-C6H4-SO2-F
-
-
2-chloro-4-(1-hydroxyoctadecyl)benzoic acid
2-ethoxy-4H-3,1-benzoxazin-4-one
-
-
2-ethoxy-5-ethyl-4H-3,1-benzoxazin-4-one
-
-
2-hydroxyethyl (4R)-4-[4-cyanophenyl-6-methyl-2-oxo-1-[3-(trifluoromethyl)phenyl]]-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
2-methyl-4H-3,1-benzoxazin-4-one
-
-
2-nitrophenylboronic acid
-
-
2-[(Imidazole-1-carbonyl)-amino]-pentanoic acid methyl ester
-
-
2-[2-(1H-imidazol-1-yl)pyridin-3-yl]-5-methyl-4H-3,1-benzoxazin-4-one
-
-
2-[2-(4-butylpiperazin-1-yl)pyridin-3-yl]-5-ethyl-7-methoxy-4H-3,1-benzoxazin-4-one
-
-
2-[2-(4-cyclopentylpiperazin-1-yl)pyridin-3-yl]-5-ethyl-7-methoxy-4H-3,1-benzoxazin-4-one
-
-
2-[2-(4-fluorophenyl)-6-oxo-5-[(cyclohexylsulfamoyl)-amino]-1,6-dihydro-1-pyrimidinyl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide
-
-
2-[2-[4-(cyclopropylmethyl)piperazin-1-yl]pyridin-3-yl]-5-ethyl-7-methoxy-4H-3,1-benzoxazin-4-one
-
-
2-[4-(2,2-Dihydroxy-ethyl)-phenoxy]-3,3-diethyl-4-oxo-azetidine-1-carboxylic acid (1-benzo[1,3]dioxol-5-yl-butyl)-amide
-
-
2-[4-(2,2-Dihydroxy-ethyl)-phenoxy]-3,3-diethyl-4-oxo-azetidine-1-carboxylic acid (1-p-tolyl-butyl)-amide
-
-
2-[4-(2,2-Dihydroxy-ethyl)-phenoxy]-3,3-diethyl-4-oxo-azetidine-1-carboxylic acid 4-methyl-benzylamide
-
-
2-[5-amino-2-(3,5-difluorophenyl)-6-oxopyrimidin-1(6H)-yl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide
-
-
2-[5-amino-6-oxo-2-(2-thienyl)-1,6-dihydro-1-pyrimidinyl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide
-
-
2-[5-amino-6-oxo-2-(4-fluorophenyl)-1,6-dihydro-1-pyrimidinyl]-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]acetamide
-
-
2-[5-[(benzyloxycarbonyl)amino]-6-oxo-2-(2-thienyl)-1,6-dihydro-1-pyrimidinyl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide
-
-
2-[benzyloxycarbonyl-NHCH2-C(O)NH]-C6H4-SO2-F
-
-
3'-geranyl-5,7,2',4'-tetrahydroxyisoflavanone
-
-
3,3-diethyl-1-(4-((phenylthio)methyl)phenyl)azetidine-2,4-dione
-
-
3,3-diethyl-1-(4-methoxyphenyl)azetidine-2,4-dione
-
-
3,3-diethyl-1-(4-methylphenyl)azetidine-2,4-dione
-
-
3,3-diethyl-1-(6-methylpyridin-3-yl)azetidine-2,4-dione
-
-
3,3-diethyl-1-(naphthalen-1-yl)azetidine-2,4-dione
-
-
3,3-diethyl-1-(pyridin-3-yl)azetidine-2,4-dione
-
-
3,3-diethyl-1-o-tolylazetidine-2,4-dione
-
-
3,3-diethyl-1-phenylazetidine-2,4-dione
-
-
3,3-diethyl-1-[4-(naphthalen-2-yloxy)phenyl]azetidine-2,4-dione
-
-
3,3-dimethyl-1-phenylazetidine-2,4-dione
-
-
3,4-dichloro-1H-isochromen-1-one
-
-
3-acetoxymethyl-7-[S]-methoxy-8-oxo-5-thia-1-aza-6[R]-bicyclo[4.2.0]oct-2-ene-2-(2-(S)-carboxypyrrolidine-carboxamide)-5,5-dioxide
-
L-658,758, cephalosporin-based anti-elastase
3-benzyl-1-(sulfooxy)pyrrolidine-2,5-dione
-
-
3-benzyl-1-[(methylsulfonyl)oxy]pyrrolidine-2,5-dione
-
-
3-benzyl-1-{[(4-vinylphenyl)sulfonyl]oxy}pyrrolidine-2,5-dione
-
-
3-benzyl-3-ethyl-1-phenylazetidine-2,4-dione
-
-
3-benzyl-3-methyl-1-phenylazetidine-2,4-dione
-
-
3-CF3-C6H4-CO-Ala-Ala-4-nitroanilide
-
-
3-chloro-1H-isochromen-1-one
-
-
3-ethyl-3-isobutyl-1-phenylazetidine-2,4-dione
-
-
3-isopropyl-1-[(methylsulfonyl)oxy]pyrrolidine-2,5-dione
-
-
3-isopropyl-1-{[(4-vinylphenyl)sulfonyl]oxy}pyrrolidine-2,5-dione
-
-
3-isopropyl-6-methylenetetrahydro-2H-pyran-2-one
-
-
3-methoxy-1-oxo-1H-isochromen-7-yl nitrite
-
-
3-methoxy-7-nitro-1H-isochromen-1-one
-
-
3-tert-butyl-1-{[(4-vinylphenyl)sulfonyl]oxy}pyrrolidine-2,5-dione
-
-
3-[(1-{2-[2-(3-Methoxycarbonyl-propionylamino)-propionylamino]-propionyl}-pyrrolidine-2-carbonyl)-amino]-4-methyl-2-oxo-pentanoic acid methyl ester
-
-
3-[2-(2-Benzyloxycarbonylamino-propionylamino)-propionylamino]-2-oxo-pentanoic acid benzyl ester
-
-
3-[4-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperazin-1-yl]propanenitrile
-
-
3-{[1-(2-Benzyloxycarbonylamino-3-methyl-butyryl)-pyrrolidine-2-carbonyl]-amino}-4-methyl-2-oxo-pentanoic acid ethyl ester
-
-
3beta,5alpha,9alpha-trihydroxy-ergosta-7,22-dien-6-one
-
-
3beta,5alpha-dihydroxy-6beta-methoxyergosta-7,22-diene
-
-
3beta,5alpha-dihydroxy-ergosta-7,22-dien-6-one
-
-
3beta-hydroxy-ergosta-7,22-dien-6-one
-
-
4-((1-(((1-(R)-(5-benzofuranyl)butyl)amino)carbonyl)-3,3-diethyl-4-oxo-2-(S)-azetidinyl)oxy)benzene acetic acid
-
the synthetic inhibitor may provide a new and useful therapeutic for the treatment of diseases characterized by polymorphonuclear elastase involvement
4-(3,3-diethyl-2,4-dioxoazetidin-1-yl)benzonitrile
-
-
4-(4-bromophenylsulfonylcarbamoyl)benzoyl-L-valyl-L-proline 1 (RS)-(1-trifluoroacetyl-2-methylpropyl)amide
-
ICI 200,355, reversible, tight, and potent inhibitor, prevents the ongoing destruction of insoluble elastin by elastase, IC50: 16 nM, 4fold excess of inhibitor over enzyme causes 83% inhibition
4-chloro-3-ethoxy-1H-isochromen-1-one
-
-
4-chloro-3-methoxy-1-oxo-1H-isochromen-7-yl nitrite
-
-
4-chloro-3-methoxy-7-nitro-1H-isochromen-1-one
-
-
4-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperazine-1-carboxylic acid
-
-
4-{5-(Adamantane-1-sulfonylamino)-6-oxo-6-[2-(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidin-1-yl]-hexylcarbamoyl}-butyric acid methyl ester
-
-
5,6-dimethyl-2-(4-nitrophenylamino)-4H-thieno[2,3-d][1,3]thioxazin-4-one
-
-
5-(2-Chloro-benzyl)-2-(2,2-dimethyl-propionyloxy)-5-hydroxy-5,6-dihydro-thieno[3,2-c]pyridin-5-ium; chloride
-
-
5-(4-Chloro-benzenesulfonylamino)-5-(2-isopropylamino-5-methyl-4-oxo-4H-benzo[d][1,3]oxazin-7-ylcarbamoyl)-pentyl-ammonium; chloride
-
-
5-aminopyridin-6-one-containing trifluoromethyl ketones
-
-
-
5-chloro-2-(2-bromophenyl)-4H-benzo[d][1,3]oxazin-4-one
-
-
5-chloro-2-(2-chlorophenyl)-4H-benzo[d][1,3]oxazin-4-one
-
-
5-chloro-2-(2-fluorophenyl)-4H-benzo[d][1,3]oxazin-4-one
-
-
5-chloro-2-(2-methoxyphenyl)-4H-benzo[d][1,3]oxazin-4-one
-
-
5-chloro-2-(2-methylphenyl)-4H-benzo[d][1,3]oxazin-4-one
-
-
5-chloro-2-(2-phenoxypyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
-
5-cyclobutyl-7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
-
5-cyclobutyl-7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
-
5-cyclopropyl-7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
-
5-cyclopropyl-7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
-
5-ethyl-2-(isopropylamino)-4H-3,1-benzoxazin-4-one
-
-
5-ethyl-2-methyl-4H-3,1-benzoxazin-4-one
-
-
5-ethyl-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
-
5-ethyl-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
-
5-ethyl-2-[2-[4-(2-hydroxyethyl)piperazin-1-yl]pyridin-3-yl]-7-methoxy-4H-3,1-benzoxazin-4-one
-
-
5-ethyl-7-methoxy-2-(2-[4-[2-(morpholin-4-yl)ethyl]piperazin-1-yl]pyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
-
5-ethyl-7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
-
5-ethyl-7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
-
5-ethyl-7-methoxy-2-[2-[4-(2-methoxyethyl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
-
5-ethyl-7-methoxy-2-[2-[4-(2-methylpropyl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
-
5-methoxy-2-(2-phenoxypyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
-
5-methyl-2-(2-methylpyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
-
5-methyl-2-(2-phenoxy-pyridin-3-yl)-benzo[d][1,3]oxazin-4-one
-
development and synthesis, overview
5-methyl-2-(2-phenoxyphenyl)-4H-3,1-benzoxazin-4-one
-
-
5-methyl-2-(2-phenoxypyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
-
5-methyl-2-(2-[[2-(morpholin-4-yl)ethyl]amino]pyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
-
5-methyl-2-(6-methylpyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
-
5-methyl-2-(pyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
-
5-methyl-2-(trifluoromethyl)-4H-3,1-benzoxazin-4-one
-
-
5-methyl-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
-
5-methyl-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
-
5-tert-butyl-7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
-
5alpha,6alpha,8alpha,9alpha-diepoxy-ergost-22-en-3beta,7alpha-diol
-
-
5alpha,6alpha-epoxy-ergosta-8(14),22-diene-3beta,7alpha-diol
-
-
5alpha,6alpha-epoxy-ergosta-8(9),22-dien-7-one-3beta-ol
-
-
6-({1-[2-(2-Benzyloxycarbonylamino-propionylamino)-propionyl]-pyrrolidine-2-carbonyl}-amino)-4,4-difluoro-5-oxo-heptanoic acid methyl ester
-
-
6-amino-2-(2,2,2-trifluoro-acetylamino)-hexanoic acid [1-(4-trifluoromethyl-phenylcarbamoyl)-ethyl]-amide
-
-
7-(4-chlorophenylsulfonyl-L-glutamyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one
7-(4-chlorophenylsulfonyl-L-lysyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one
7-(dimethylamino)-5-ethyl-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
-
7-(dimethylamino)-5-ethyl-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
-
7-amino-3-methoxy-1H-isochromen-1-one
-
-
7-amino-4-chloro-3-methoxy-1H-isochromen-1-one
-
-
7-chloro-2-(2-bromophenyl)-4H-benzo[d][1,3]oxazin-4-one
-
-
7-chloro-2-(2-chlorophenyl)-4H-benzo[d][1,3]oxazin-4-one
-
-
7-chloro-2-(2-fluorophenyl)-4H-benzo[d][1,3]oxazin-4-one
-
-
7-chloro-2-(2-methoxyphenyl)-4H-benzo[d][1,3]oxazin-4-one
-
-
7-chloro-2-(2-methylphenyl)-4H-benzo[d][1,3]oxazin-4-one
-
-
7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-5-(propan-2-yl)-4H-3,1-benzoxazin-4-one
-
-
7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-5-propyl-4H-3,1-benzoxazin-4-one
-
-
7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-5-(propan-2-yl)-4H-3,1-benzoxazin-4-one
-
-
7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-5-propyl-4H-3,1-benzoxazin-4-one
-
-
8-chloro-2-(2-bromophenyl)-4H-benzo[d][1,3]oxazin-4-one
-
-
8-chloro-2-(2-chlorophenyl)-4H-benzo[d][1,3]oxazin-4-one
-
-
8-chloro-2-(2-fluorophenyl)-4H-benzo[d][1,3]oxazin-4-one
-
-
8-chloro-2-(2-methoxyphenyl)-4H-benzo[d][1,3]oxazin-4-one
-
-
8-chloro-2-(2-methylphenyl)-4H-benzo[d][1,3]oxazin-4-one
-
-
Ac-Pro-Ala-Pro-NH2CH(CH3)CH2OH
-
-
Ac-Pro-Ala-Pro-NH2CH(CH3)CHO
-
-
Ac-Pro-Ala-Pro-NH2CH(CH3)CONH2
-
-
acetyl-Ala-Ala-Ala-Ala-CH2Cl
-
-
acetyl-Ala-Ala-Pro-Ala-CH2Cl
-
-
acetyl-Ala-Ala-Pro-Ile-CH2Cl
-
-
acetyl-Ala-Ala-Pro-Val-CH2Cl
-
-
Ala15-reactive site variant of aprotinin
-
good inhibitor for proteinase 2B and weak inhibitor of proteinase 2A
-
alginate
-
weak inhibition, elastase molecule interacts with 19 uronic acid units of alginate
alpha-1-antichymotrypsin
-
-
-
alpha-1-protease inhibitor
-
also called alpha-1-antitrypsin
-
alpha-aminobutyric acid15-reactive site variant of aprotinin
-
good inhibitor for proteinase 2B and weak inhibitor of proteinase 2A
-
alpha-aminovaleric acid15-reactive site variant of aprotinin
-
good inhibitor for proteinase 2B and weak inhibitor of proteinase 2A
-
alpha-ketobenzoxazoles
-
-
-
Alpha1-proteinase inhibitor
-
alpha2-Macroglobulin
-
-
-
benzyl 3,3,3-trifluoro-1-isopropyl-2-oxopropylcarbamate
-
-
bis(2,3,5-trimethylphenyl) (1-[[(benzyloxy)carbonyl]amino]-3-methylbutyl)phosphonate
-
-
bis(2,3-dimethylphenyl) (1-[[(benzyloxy)carbonyl]amino]-3-methylbutyl)phosphonate
-
-
bis(2-methylphenyl) (1-[[(benzyloxy)carbonyl]amino]-3-methylbutyl)phosphonate
-
-
bis(3,4,5-trimethylphenyl) (1-[[(benzyloxy)carbonyl]amino]-3-methylbutyl)phosphonate
-
-
bis(3,4-dimethylphenyl) (1-[[(benzyloxy)carbonyl]amino]-3-methylbutyl)phosphonate
-
-
bis(3-chlorophenyl) (1-[[(benzyloxy)carbonyl]amino]-3-methylbutyl)phosphonate
-
-
bis(3-chlorophenyl) (1-[[(benzyloxy)carbonyl]amino]propyl)phosphonate
-
-
bis(4-chlorophenyl) (1-[[(benzyloxy)carbonyl]amino]-3-methylbutyl)phosphonate
-
-
bis(4-chlorophenyl) (1-[[(benzyloxy)carbonyl]amino]pentyl)phosphonate
-
-
bis(4-chlorophenyl) (1-[[(benzyloxy)carbonyl]amino]propyl)phosphonate
-
-
bis(4-ethylphenyl) (1-[[(benzyloxy)carbonyl]amino]-2-methylpropyl)phosphonate
-
-
bis(4-ethylphenyl) (1-[[(benzyloxy)carbonyl]amino]-3-methylbutyl)phosphonate
-
-
bis(4-ethylphenyl) (1-[[(benzyloxy)carbonyl]amino]butyl)phosphonate
-
-
bis(4-ethylphenyl) (1-[[(benzyloxy)carbonyl]amino]ethyl)phosphonate
-
-
bis(4-ethylphenyl) (1-[[(benzyloxy)carbonyl]amino]propyl)phosphonate
-
-
bis(4-methoxyphenyl) (1-[[(benzyloxy)carbonyl]amino]-2-methylpropyl)phosphonate
-
-
bis(4-methoxyphenyl) (1-[[(benzyloxy)carbonyl]amino]pentyl)phosphonate
-
-
bis(4-methoxyphenyl) (1-[[(benzyloxy)carbonyl]amino]propyl)phosphonate
-
-
bis(4-methylphenyl) (1-[[(benzyloxy)carbonyl]amino]-3-methylbutyl)phosphonate
-
-
bis(4-tert-butylphenyl) (1-[[(benzyloxy)carbonyl]amino]-2-methylpropyl)phosphonate
-
-
bis(4-tert-butylphenyl) (1-[[(benzyloxy)carbonyl]amino]-3-methylbutyl)phosphonate
-
-
bis(4-tert-butylphenyl) (1-[[(benzyloxy)carbonyl]amino]ethyl)phosphonate
-
-
bis(4-tert-butylphenyl) (1-[[(benzyloxy)carbonyl]amino]pentyl)phosphonate
-
-
bis[3-(methylsulfanyl)phenyl] (1-[[(benzyloxy)carbonyl]amino]-3-methylbutyl)phosphonate
-
-
bis[4-(methylsulfanyl)phenyl] (1-[[(benzyloxy)carbonyl]amino]-2-methylpropyl)phosphonate
-
-
bis[4-(methylsulfanyl)phenyl] (1-[[(benzyloxy)carbonyl]amino]-3-methylbutyl)phosphonate
-
-
bis[4-(methylsulfanyl)phenyl] (1-[[(benzyloxy)carbonyl]amino]butyl)phosphonate
-
-
bis[4-(methylsulfanyl)phenyl] (1-[[(benzyloxy)carbonyl]amino]ethyl)phosphonate
-
-
bis[4-(methylsulfanyl)phenyl] (1-[[(benzyloxy)carbonyl]amino]propyl)phosphonate
-
-
bis[4-(propan-2-yl)phenyl] (1-[[(benzyloxy)carbonyl]amino]-3-methylbutyl)phosphonate
-
-
bis[4-(propan-2-yl)phenyl] (1-[[(benzyloxy)carbonyl]amino]ethyl)phosphonate
-
-
bis[4-(propan-2-yl)phenyl] (1-[[(benzyloxy)carbonyl]amino]pentyl)phosphonate
-
-
bis[4-(propan-2-yl)phenyl] (1-[[(benzyloxy)carbonyl]amino]propyl)phosphonate
-
-
Boc-Ala-Pro-isobutyl-boronic acid amide
-
-
Butyric acid 3-(3-bromomethylene-6-isopropyl-5-oxo-[1,4]dioxan-2-yl)-pyrrolidin-1-yl ester
-
-
Ca2+
-
inhibition of human SP-D protein cleavage at physiological concentrations
Carbamic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-(2-thienyl)-5-pyrimidinyl]-, 1-methylethyl ester
-
-
Carbamic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-(2-thienyl)-5-pyrimidinyl]-, 2,2,2-trifluoroethyl ester
-
-
Carbamic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-(2-thienyl)-5-pyrimidinyl]-, methyl ester
-
-
Carbamic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-phenyl-5-pyrimidinyl]-, 2,2,2-trifluoroethyl ester
-
-
Carbamic acid, [2-(4-fluorophenyl)-1,6-dihydro-1-[2-[[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]amino]-2-oxoethyl]-6-oxo-5-pyrimidinyl]-, (3,5-dimethyl-4-pyridinyl)methyl ester
-
-
Carbamic acid, [2-(4-fluorophenyl)-1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-5-pyrimidinyl]-, 2-pyridinylmethyl ester
-
-
Carbamic acid, [2-(4-fluorophenyl)-1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-5-pyrimidinyl]-, 4-pyridinylmethyl ester
-
-
Carbamothioic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-phenyl-5-pyrimidinyl]-, S-methyl ester
-
-
Carbamothioic acid, [2-(4-fluorophenyl)-1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-5-pyrimidinyl]-, S-methyl ester
-
-
CBZ-Ala-(isobutyl-difluoro-boron)amide
-
-
CBZ-Ala-isobutyl-boronic acid amide
-
-
ceftazidime
-
slight inhibition of purified elastase
cephalotin
-
IC50: 0.00025 mg/ml
CF3-CO-Ala-Ala-4-nitroanilide
-
-
CF3-CO-Ala-Ala-Ala-OH
-
-
clitocybin D
-
4-(4,6-dihydroxy-3-methoxy-3Hisoindol-1-yl)-benzoic acid, isolated from mycelia culture broth of Clitocybe aurantiaca, structure determination by NMR and mass spectroscopy
difluoro-beta-ketoamides
-
-
-
difluoromethyleneamines
-
-
-
diisopropyl fluorophosphates
-
almost complete inhibition
diisopropyl phosphorofluoridate
-
-
dimethyl 3,3'-[[(1-[[(benzyloxy)carbonyl]amino]-3-methylbutyl)phosphoryl]bis(oxy)]dibenzoate
-
-
dimethyl 4,4'-[[(1-[[(benzyloxy)carbonyl]amino]-2-methylpropyl)phosphoryl]bis(oxy)]dibenzenesulfinate
-
-
dimethyl 4,4'-[[(1-[[(benzyloxy)carbonyl]amino]-2-methylpropyl)phosphoryl]bis(oxy)]dibenzoate
-
-
dimethyl 4,4'-[[(1-[[(benzyloxy)carbonyl]amino]-3-methylbutyl)phosphoryl]bis(oxy)]dibenzoate
-
-
dimethyl 4,4'-[[(1-[[(benzyloxy)carbonyl]amino]butyl)phosphoryl]bis(oxy)]dibenzoate
-
-
dimethyl 4,4'-[[(1-[[(benzyloxy)carbonyl]amino]ethyl)phosphoryl]bis(oxy)]dibenzoate
-
-
dimethyl 4,4'-[[(1-[[(benzyloxy)carbonyl]amino]pentyl)phosphoryl]bis(oxy)]dibenzoate
-
-
dimethyl 4,4'-[[(1-[[(benzyloxy)carbonyl]amino]propyl)phosphoryl]bis(oxy)]dibenzoate
-
-
diphenyl (1-[[(benzyloxy)carbonyl]amino]-3-methylbutyl)phosphonate
-
-
diphenyl (1-[[(benzyloxy)carbonyl]amino]butyl)phosphonate
-
-
diphenyl (1-[[(benzyloxy)carbonyl]amino]ethyl)phosphonate
-
-
diphenyl (1-[[(benzyloxy)carbonyl]amino]pentyl)phosphonate
-
-
diphenyl (1-[[(benzyloxy)carbonyl]amino]propyl)phosphonate
-
-
elastase inhibitor III
-
-
-
EPI-hNE4 (depelstat)
-
-
-
epigallocatechin gallate
-
-
ergosta-4,7,22-trien-3,6-dione
-
-
ergosta-7,22-dien-2beta,3alpha,9alpha-triol
-
-
ergosta-7,22-dien-3beta,5alpha,6beta,9alpha-tetraol
-
-
erythromycin
-
acts as an alternate substrate neutrophil elastase inhibitor
ethyl (2S,3R)-2-[(2,2-dihydroxyethyl)sulfonyl]-3-ethyl-4-oxoazetidine-1-carboxylate
-
-
ethyl 1-(1,3-benzodioxol-5-ylcarbonyl)-1H-indazole-3-carboxylate
-
-
ethyl 1-(phenylcarbonyl)-1H-indazole-3-carboxylate
-
-
ethyl 1-acetyl-1H-indazole-3-carboxylate
-
-
ethyl 1-[(2-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
-
-
ethyl 1-[(3-chlorophenyl)carbonyl]-1H-indazole-3-carboxylate
-
-
ethyl 1-[(3-fluorophenyl)carbonyl]-1H-indazole-3-carboxylate
-
-
ethyl 1-[(3-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
-
-
ethyl 1-[(4-chlorophenyl)carbonyl]-1H-indazole-3-carboxylate
-
-
ethyl 1-[(4-fluorophenyl)carbonyl]-1H-indazole-3-carboxylate
-
-
ethyl 1-[(4-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
-
-
ethyl [4-(3,3-diethyl-2,4-dioxoazetidin-1-yl)phenyl]acetate
-
-
flurythromycin
-
inactivator of neutrophil elastase
Formic acid 2-(3-{1-[2-(N'-benzyloxycarbonyl-N'-propyl-hydrazinocarbonyl)-pyrrolidine-1-carbonyl]-2-methyl-propyl}-ureido)-4-methyl-pentyl ester
-
-
Formic acid 4-methyl-2-(3-{2-methyl-1-[2-(N'-phenoxycarbonyl-N'-propyl-hydrazinocarbonyl)-pyrrolidine-1-carbonyl]-propyl}-ureido)-pentyl ester
-
-
gentamycin
-
slight inhibition of purified elastase
glutaryl-Ala-Ala-Pro-NH-C3H7
-
-
gold thiomalate
-
inhibition is abolished by 1.0 M KCl
greglin
-
fast-acting and tight-binding inhibitor of neutrophil elastase
-
guamerin
-
recombinant guamerin isolated from the leech Hirudo nipponia
-
GW447631
-
i.e. (3S,3aS,6aR)-4-(5-cyclopropylaminomethyl-pyrazine-2-carbonyl)-3-isopropyl-1-methanesulfonyl-hexahydropyrrolo[3,2-b]pyrrol-2-one hydrochloride
GW469002
-
i.e. (3S,3aS,6R)-4-[1-(2,2-dimethyl-propyl)azetidine-3-carbonyl]-3-isopropyl-1-methanesulfonyl-hexahydro-pyrrolo-[3,2-b]pyrrol-2-one
horse leukocyte elastase inhibitor
-
human monocyte/neutrophil elastase inhibitor
-
effective inhibition
-
human pancreatic secretory trypsin inhibitor
variants optimized with respect to the affinity and specificity for human leukocyte elastase relative to trypsin, and in particular chymotrypsin
-
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1R)-3,3-difluoro-1-(1-methylethyl)-2,4-dioxo-4-[(2-pyridinylmethyl)amino]butyl]-
-
-
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-3,3-difluoro-1-(1-methylethyl)-2,4-dioxo-4-[(2-pyridinylmethyl)amino]butyl]-
-
-
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-3,3-difluoro-1-(1-methylethyl)-2-oxo-4-[(phenylmethyl)amino]butyl]-
-
-
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-3,3-difluoro-4-(methylamino)-1-(1-methylethyl)-2,4-dioxobutyl]-
-
-
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-4-(benzoylamino)-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
-
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-4-amino-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
-
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-4-[[(1,1-dimethylethoxy)carbonyl]amino]-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
-
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
-
L-Prolinamide, N-(phenoxycarbonyl)-L-valyl-N-[(1S)-3,3-difluoro-1-(1-methylethyl)-2,4-dioxo-4-[(2-pyridinylmethyl)amino]butyl]-
-
-
L-Prolinamide, N-(phenoxycarbonyl)-L-valyl-N-[(1S)-3,3-difluoro-4-(methylamino)-1-(1-methylethyl)-2,4-dioxobutyl]-
-
-
L-Prolinamide, N-(phenoxycarbonyl)-L-valyl-N-[(1S)-4-[[(1,1-dimethylethoxy)carbonyl]amino]-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
-
L-Prolinamide, N-(phenoxycarbonyl)-L-valyl-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
-
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-3,3-difluoro-1-(1-methylethyl)-2-oxo-4-[(phenylmethyl)amino]butyl]-
-
-
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-3,3-difluoro-4-(methylamino)-1-(1-methylethyl)-2,4-dioxobutyl]-
-
-
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-4-amino-3,3-difluoro-1-(1-methylethyl)-2,4-dioxobutyl]-
-
-
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-4-amino-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
-
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-4-[[(1,1-dimethylethoxy)carbonyl]amino]-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
-
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
-
leukocyte elastase inhibitor
-
long-chain fatty acids
-
-
m-CF3-C6H4-CO-Ala-Ala-4-nitroanilide
-
-
matrix metalloproteinase-7
-
human leukocyte elastase cleaves matrix metalloproteinase-7 resulting in loss of enzymatic activity
-
MCoTI-II K10A
-
a MCoTI-II exchange analogue
MCoTI-II K10F
-
a MCoTI-II exchange analogue
MCoTI-II K10V
-
a MCoTI-II exchange analogue
MDL101146
suicide inhibitor
MeO-Suc-Ala-Ala-Pro-Ala-CH2Cl
MeO-Suc-Ala-Ala-Pro-Val-CH2Cl
MeOSuc-Ala-Ala-Pro-Val-chloromethylketone
-
neutrophil elastase-specific inhibitor
methoxsuccinyl-Ala-Ala-Pro-Ile-boronic acid
-
-
methoxysuccinyl-Ala-Ala-Pro-(isobutyl-4,4,5,5-tetramethyl-1,3,2-dioxaborolane)amide
-
-
methoxysuccinyl-Ala-Ala-Pro-isobutyl-boronic acid amide
-
-
methoxysuccinyl-Ala-Ala-Pro-phenylethylboronic acid
-
-
methoxysuccinyl-Ala-Ala-Pro-Val chloromethyl ketone
-
specific inhibitor
methoxysuccinyl-Ala-Ala-Pro-Val-CH2Cl
methoxysuccinyl-Ala-Ala-Pro-Val-chloromethyl ketone
-
methoxysuccinyl-Ala-Ala-Pro-Val-chloromethylketone
monocyte/neutrophil elastase inhibitor
-
N'-{1-[2-(2-Acetylamino-propionylamino)-propionyl]-pyrrolidine-2-carbonyl}-N-methyl-hydrazinecarboxylic acid 1-benzylcarbamoyl-ethyl ester
-
-
N'-{1-[2-(2-Acetylamino-propionylamino)-propionyl]-pyrrolidine-2-carbonyl}-N-methyl-hydrazinecarboxylic acid 1-carbamoyl-ethyl ester
-
-
N-(1-(1-[1-(4-benzoyl-phenylcarbamoyl)-2-methyl-propylcarbamoyl]-3-methyl-butylcarbamoyl)-2-(4-hydroxy-phenyl)-ethyl)-succinamic acid
-
-
N-(1-{1-Methyl-2-oxo-2-[2-(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidin-1-yl]-ethylcarbamoyl}-ethyl)-succinamic acid methyl ester
-
-
N-(1-{2-[2-(3-Chloro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidin-1-yl]-1-methyl-2-oxo-ethylcarbamoyl}-ethyl)-succinamic acid methyl ester
-
-
N-(1-{2-[2-(4-Ethoxy-3,3-difluoro-1-isopropyl-2-oxo-butylcarbamoyl)-pyrrolidin-1-yl]-1-methyl-2-oxo-ethylcarbamoyl}-ethyl)-succinamic acid methyl ester
-
-
N-(2,2-diphenyl-ethyl)-1-(1,1,3-trioxo-1,3-dihydro-1lambda6-1,2-benzisothiazol-2-yl)-methanesulfonamide
-
-
N-(2-phenylethyl)-1H-imidazole-1-carboxamide
-
-
N-(5-(adamantane-1-sulfonylamino)-5-[1-(1-formyl-2-methyl-propylcarbamoyl)-ethylcarbamoyl]-pentyl)-succinamic acid
-
-
N-(5-(adamantane-1-sulfonylamino)-5-[1-(1-formyl-2-methyl-propylcarbamoyl)-ethylcarbamoyl]-pentyl)-terephthalamic acid
-
-
N-(5-benzyloxycarbonylamino-1-(1-[2-(1-formyl-2-methyl-propylcarbamoyl)-pyrrolidine-1-carbonyl]-2-methyl-propylcarbamoyl)-pentyl)-succinamic acid
-
-
N-(methoxysuccinyl)-Ala-Ala-Pro-Val-chloromethyl ketone
N-([3-(carboxymethyl)-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl]acetyl)-L-valyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-L-prolinamide
-
-
N-([3-(carboxymethyl)-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl]acetyl)-L-valyl-N-[(3R,S)1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl]-L-prolinamide
-
-
N-([3-(carboxymethyl)-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl]acetyl)-L-valyl-N-[(3S)-1-(benzylamino)-4-methyl-1,2-dioxopentan-3-yl]-L-prolinamide
-
-
N-([3-(carboxymethyl)-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl]acetyl)-L-valyl-N-[(3S)-1-methoxy-4-methyl-1,2-dioxopentan-3-yl]-L-prolinamide
-
-
N-([3-(carboxymethyl)-2,4-dioxoimidazolidin-1-yl]acetyl)-L-valyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-L-prolinamide
-
-
N-([3-(carboxymethyl)-2,5-dioxoimidazolidin-1-yl]acetyl)-L-valyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-L-prolinamide
-
-
N-([3-(carboxymethyl)-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl]acetyl)-L-valyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-L-prolinamide
-
-
N-([3-(carboxymethyl)-2,6-dioxotetrahydropyrimidin-1(2H)-yl]acetyl)-L-valyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-L-prolinamide
-
-
N-([3-(carboxymethyl)-2-oxoimidazolidin-1-yl]acetyl)-L-valyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-L-prolinamide
-
-
N-([3-(carboxymethyl)-2-oxoimidazolidin-1-yl]acetyl)-L-valyl-N-[(3R)-1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl]-L-prolinamide
-
-
N-([3-(carboxymethyl)-2-oxoimidazolidin-1-yl]acetyl)-L-valyl-N-[(3S)-1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl]-L-prolinamide
-
i.e. AE-3763, it effects in lipopolysaccharide-induced lung injury model of lung edema and leukocyte infiltration, overveiw
N-([3-(carboxymethyl)-4,4-dimethyl-2,5-dioxoimidazolidin-1-yl]acetyl)-L-valyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-L-prolinamide
-
-
N-([3-(carboxymethyl)-5,5-dimethyl-2,4-dioxoimidazolidin-1-yl]acetyl)-L-valyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-L-prolinamide
-
-
N-([3-(carboxymethyl)-5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl]acetyl)-L-valyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-L-prolinamide
-
-
N-([4-(carboxymethoxy)phenoxy]acetyl)-L-valyl-N-[(benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-L-prolinamide
-
-
N-([4-(carboxymethyl)-2,3-dioxopiperazin-1-yl]acetyl)-L-valyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-L-prolinamide
-
-
N-([4-(carboxymethyl)-2,3-dioxopiperazin-1-yl]acetyl)-L-valyl-N-[(3S)-1-(benzylamino)-4-methyl-1,2-dioxopentan-3-yl]-L-prolinamide
-
-
N-([4-(carboxymethyl)-2,3-dioxopiperazin-1-yl]acetyl)-L-valyl-N-[(3S)-1-methoxy-4-methyl-1,2-dioxopentan-3-yl]-L-prolinamide
-
-
N-([4-(carboxymethyl)-2,5-dioxopiperazin-1-yl]acetyl)-L-valyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-L-prolinamide
-
-
N-([4-(carboxymethyl)-3,5-dioxo-4,5-dihydro-1,2,4-triazin-2(3H)-yl]acetyl)-L-valyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-L-prolinamide
-
-
N-([4-(carboxymethyl)-6-methyl-3,5-dioxo-4,5-dihydro-1,2,4-triazin-2(3H)-yl]acetyl)-L-valyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-L-prolinamide
-
-
N-([4-(carboxymethyl)piperazin-1-yl]acetyl)-L-valyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-L-prolinamide
-
-
N-benzyl-1-(1,1,3-trioxo-1,3-dihydro-1lambda6-1,2-benzisothiazol-2-yl)-methanesulfonamide
-
-
N-galloyl-4-alkyliden-beta-lactam
-
a beta-lactam with an N-linked galloyl moiety, specific noncompetitive inhibition of the enzyme, but not affecting chemotactic response and viability of polymorphonuclear leukocytes, synthesis and structure, overview
N-methoxysuccinyl-Ala-Ala-Pro-Ala chloromethylketone
-
irreversible inhibitor
-
N-methoxysuccinyl-Ala-Ala-Pro-Val chloromethyl ketone
-
-
N-methoxysuccinyl-Ala-Ala-Pro-Val-chloromethyl ketone
-
neutrophil elastase-specific inhibitor
N-phenethyl-1-(1,1,3-trioxo-1,3-dihydro-1lambda6-1,2-benzisothiazol-2-yl)-methanesulfonamide
-
-
N-[(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetyl]-L-valyl-N-[(3R,S)-1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl]-L-prolinamide
-
-
N-{1-[2-(2-{2-[(2-Chloro-acetyl)-isopropyl-amino]-acetyl}-pyrrolidin-1-yl)-1-methyl-2-oxo-ethylcarbamoyl]-ethyl}-succinamic acid
-
-
N-{1-[2-(2-{2-[(2-Chloro-acetyl)-isopropyl-amino]-acetyl}-pyrrolidin-1-yl)-1-methyl-2-oxo-ethylcarbamoyl]-ethyl}-succinamic acid methyl ester
-
-
N-{1-[2-(2-{2-[Isopropyl-(4-nitro-phenoxycarbonyl)-amino]-acetyl}-pyrrolidin-1-yl)-1-methyl-2-oxo-ethylcarbamoyl]-ethyl}-succinamic acid methyl ester
-
-
N-{2-[3-(trifluoromethyl)phenyl]ethyl}-1H-imidazole-1-carboxamide
-
-
N-{5-(Adamantane-1-sulfonylamino)-5-[1-(1-formyl-2-methyl-propylcarbamoyl)-ethylcarbamoyl]-pentyl}-4-dihydroxymethyl-benzamide
-
-
N2-[4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]benzoyl]-N-(2-propylphenyl)-L-leucinamide
-
NaCl
-
1.0 M, 50% inhibition
nigranoic acid
-
significant inhibitory activity
oleoyl-Ala-Ala-Pro-Ala
-
-
oleoyl-Ala-Ala-Pro-Val
-
-
pancreatic secretory trypsin inhibitor
-
variants of human secretory trypsin inhibitor are constructed with the aim of producing inhibitors specific for human leukocyte elastase. Models of the human pancreatic secretory trypsin inhibitor/human leukocytic elastase and human pancreatic secretory trypsin inhibitor/chymotrypsin complexes are generated by computer aided protein design and used to plan better human leukocyte elastase inhibitors. The native human pancreatic secretory trypsin inhibitor with Lys in position P1 (amino acid 18) is a highly potent inhibitor for trypsin and completely inactive towards chymotrypsin and elastase like proteinases. Replacing the Lys in P1 by Leu (pancreatic secretory trypsin inhibitor 7) causes a drastic change of the specificity : this variant no longer inhibits trypsin-like enzymes but is an excellent inhibitor of chymotrypsin and human leukocytic elastase
-
phenylmethylsulfonyl fluoride
-
-
polysaccharide sulfates
-
-
-
prolastin
-
i.e. alpha1-antitrypsin, acts similar to monocyte/neutrophil elastase inhibitor, MNEI
-
propan-2-yl 1-(phenylcarbonyl)-1H-indazole-3-carboxylate
-
-
propan-2-yl 1-(thiophen-3-ylcarbonyl)-1H-indazole-3-carboxylate
-
-
propan-2-yl 1-[(3-aminophenyl)carbonyl]-1H-indazole-3-carboxylate
-
-
propan-2-yl 1-[(3-methoxyphenyl)carbonyl]-1H-indazole-3-carboxylate
-
-
propan-2-yl 1-[(3-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
-
-
propolis
-
IC50: 0.002 mg dry weight per ml for ethyl acetate extract of propolis
-
propyl 1-(phenylcarbonyl)-1H-indazole-3-carboxylate
-
-
propyl 1-[(3-aminophenyl)carbonyl]-1H-indazole-3-carboxylate
-
-
propyl 1-[(3-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
-
-
secretory leukocyte protease inhibitor
-
-
-
secretory leukoprotease inhibitor
-
-
-
secretory leukoproteinase inhibitor
-
important inhibitor of neutrophil elastase
-
semisynthetic glucan sulfates
-
with pullulan as basic polysaccharide: PulS1, PulS2, PulS3 (IC50: 0.0000181 mM), PulS4, PulS5, PulS6 and PulS7, with glucuronoxylan as basic polysaccharide: PPS, and with phycarine as basic polysaccharide: PS3
-
serine protease inhibitor 6
-
weak inhibition in vivo
-
serum leukocyte protease inhibitor
-
-
-
sivelestat sodium
-
neutrophil elastase specific inhibitor
sivelestat sodium hydrate
succinyl-Ala-Ala-Pro-Val-CH2Cl
-
-
succinyl-Tyr-D-Leu-D-Val-4-nitroanilide
-
-
tert-butoxycarbonyl-Val-Val-Val-NH-(CH2)11-CH3
-
-
tert-butyl (6R,7S)-3-[(acetyloxy)methyl]-7-chloro-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate 5,5-dioxide
-
-
tert-butyl (6R,7S)-3-[(acetyloxy)methyl]-7-methoxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate 5,5-dioxide
-
-
thieno[2,3-d]-1,3-oxazin-4-ones
-
-
thieno[2,3-d]-1,3-thioxazin-4-ones
-
-
thieno[3,2-d]-1,3-oxazin-4-ones
-
-
thieno[3,2-d]-1,3-thioxazin-4-ones
-
-
tobramycin
-
slight inhibition of purified elastase
trifluoromethylketones
-
-
Trypsin inhibitor
-
lima-bean trypsin inhibitor; soya-bean trypsin inhibitor
-
Val15-reactive site variant of aprotinin
-
good inhibitor for proteinase 2B and weak inhibitor of proteinase 2A
-
ZD0892
-
synthetic neutrophil elastase inhibitor
ZN200355
-
pharmacologic inhibition of neutrophil elastase significantly reduces infarct volume, blood-brain barrier disruption, vasogenic edema, and leukocyte-endothelial adherence after transient middle cerebral artery occlusion
-
[(4S)-5-benzyl-4-(2-methylpropyl)-1,1-dioxido-3-oxo-1,2,5-thiadiazolidin-2-yl]methyl 2-(4-benzoylphenyl)propanoate
-
-
[(4S)-5-benzyl-4-(2-methylpropyl)-1,1-dioxido-3-oxo-1,2,5-thiadiazolidin-2-yl]methyl 2-(4-phenoxyphenyl)propanoate
-
-
[(4S)-5-benzyl-4-(2-methylpropyl)-1,1-dioxido-3-oxo-1,2,5-thiadiazolidin-2-yl]methyl 2-(acetyloxy)benzoate
-
-
[(4S)-5-benzyl-4-(2-methylpropyl)-1,1-dioxido-3-oxo-1,2,5-thiadiazolidin-2-yl]methyl 2-hydroxybenzoate
-
-
[(4S)-5-benzyl-4-(2-methylpropyl)-1,1-dioxido-3-oxo-1,2,5-thiadiazolidin-2-yl]methyl 2-[4-(propan-2-yl)phenyl]propanoate
-
-
[(4S)-5-benzyl-4-(2-methylpropyl)-1,1-dioxido-3-oxo-1,2,5-thiadiazolidin-2-yl]methyl 3-phenylpropanoate
-
-
[(4S)-5-benzyl-4-(2-methylpropyl)-1,1-dioxido-3-oxo-1,2,5-thiadiazolidin-2-yl]methyl phenylacetate
-
-
[(4S)-5-benzyl-4-(2-methylpropyl)-1,1-dioxido-3-oxo-1,2,5-thiadiazolidin-2-yl]methyl [2-[(2,6-dichlorophenyl)amino]phenyl]acetate
-
-
[(4S)-5-methyl-4-(2-methylpropyl)-1,1-dioxido-3-oxo-1,2,5-thiadiazolidin-2-yl]methyl 2-(4-benzoylphenyl)propanoate
-
-
[(4S)-5-methyl-4-(2-methylpropyl)-1,1-dioxido-3-oxo-1,2,5-thiadiazolidin-2-yl]methyl 2-(4-phenoxyphenyl)propanoate
-
-
[(4S)-5-methyl-4-(2-methylpropyl)-1,1-dioxido-3-oxo-1,2,5-thiadiazolidin-2-yl]methyl 2-(acetyloxy)benzoate
-
-
[(4S)-5-methyl-4-(2-methylpropyl)-1,1-dioxido-3-oxo-1,2,5-thiadiazolidin-2-yl]methyl 2-hydroxybenzoate
-
-
[(4S)-5-methyl-4-(2-methylpropyl)-1,1-dioxido-3-oxo-1,2,5-thiadiazolidin-2-yl]methyl 2-[4-(propan-2-yl)phenyl]propanoate
-
-
[(4S)-5-methyl-4-(2-methylpropyl)-1,1-dioxido-3-oxo-1,2,5-thiadiazolidin-2-yl]methyl 3-phenylpropanoate
-
-
[(4S)-5-methyl-4-(2-methylpropyl)-1,1-dioxido-3-oxo-1,2,5-thiadiazolidin-2-yl]methyl phenylacetate
-
-
[(4S)-5-methyl-4-(2-methylpropyl)-1,1-dioxido-3-oxo-1,2,5-thiadiazolidin-2-yl]methyl [2-[(2,6-dichlorophenyl)amino]phenyl]acetate
-
-
[({(2R,3S)-3-ethyl-1-[(4-methylphenyl)sulfonyl]-4-oxoazetidin-2-yl}carbonyl)oxy]acetic acid
-
-
[6-Oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-2-(4-trifluoromethyl-phenyl)-1,6-dihydro-pyrimidin-5-yl]-carbamic acid benzyl ester
-
-
{(6R,7S)-2-[(tert-butylamino)carbonyl]-7-methoxy-5,5-dioxido-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl}methyl acetate
-
-
{1-[2-(1-Acetyl-2-methyl-propylcarbamoyl)-pyrrolidine-1-carbonyl]-2-methyl-propyl}-carbamic acid benzyl ester
-
-
{1-[2-(1-Aminooxalyl-2-methyl-propylcarbamoyl)-pyrrolidine-1-carbonyl]-2-methyl-propyl}-carbamic acid benzyl ester
-
-
{1-[2-(1-Formyl-2-methyl-propylcarbamoyl)-pyrrolidine-1-carbonyl]-2-methyl-propyl}-carbamic acid benzyl ester
-
-
{1-[2-(1-Isopropyl-2,3-dioxo-heptylcarbamoyl)-pyrrolidine-1-carbonyl]-2-methyl-propyl}-carbamic acid benzyl ester
-
-
{1-[2-(3,3-Difluoro-1-isopropyl-2,4-dioxo-7-phenyl-heptylcarbamoyl)-pyrrolidine-1-carbonyl]-2-methyl-propyl}-carbamic acid benzyl ester
-
-
{1-[2-(3-Benzylcarbamoyl-3,3-difluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidine-1-carbonyl]-2-methyl-propyl}-carbamic acid benzyl ester
-
-
{2-Methyl-1-[(R)-2-(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidine-1-carbonyl]-propyl}-carbamic acid benzyl ester
-
-
{2-Methyl-1-[(S)-2-(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidine-1-carbonyl]-propyl}-carbamic acid benzyl ester
-
-
{2-Methyl-1-[2-(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-pyrrolidine-1-carbonyl]-propyl}-carbamic acid benzyl ester
-
-
{2-Methyl-1-[2-(3,3,3-trifluoro-2-hydroxy-1-isopropyl-propylcarbamoyl)-pyrrolidine-1-carbonyl]-propyl}-carbamic acid benzyl ester
-
-
2-chloro-4-(1-hydroxyoctadecyl)benzoic acid
-
SC-39026
2-chloro-4-(1-hydroxyoctadecyl)benzoic acid
-
SC-39026, reversible non-competitive inhibition at low concentrations (0.0005-0.00125 mM), mixed type inhibition at higher concentrations
2-chloro-4-(1-hydroxyoctadecyl)benzoic acid
-
SC-39026
2-chloro-4-(1-hydroxyoctadecyl)benzoic acid
-
SC-39026
2-chloro-4-(1-hydroxyoctadecyl)benzoic acid
-
SC-39026
7-(4-chlorophenylsulfonyl-L-glutamyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one
-
TEI-5624, strong, highly specific inhibitor, prevents degradation of insoluble elastin by elastase, prevents pulmonary hemorrhage in animal model
7-(4-chlorophenylsulfonyl-L-glutamyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one
-
TEI-5624, strong, highly specific inhibitor, prevents degradation of insoluble elastin by elastase
7-(4-chlorophenylsulfonyl-L-lysyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one
-
TEI-6344, strong, highly specific inhibitor, prevents degradation of insoluble elastin by elastase, prevents pulmonary hemorrhage in animal model
7-(4-chlorophenylsulfonyl-L-lysyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one
-
TEI-6344, strong, highly specific inhibitor, prevents degradation of insoluble elastin by elastase
alpha-1-antitrypsin
-
incomplete inhibition with the antielastase alpha-1-antitrypsin after binding to heparan sulfate components of syndecan-1
-
alpha-1-antitrypsin
-
-
-
alpha-1-antitrypsin
-
neutrophil elastase is inactivated by 0.005 mg of alpha-1-antitrypsin for 30 min
-
alpha-1-antitrypsin
-
-
-
alpha1-antitrypsin
-
-
-
alpha1-antitrypsin
-
very potent inhibitor, complete inhibition at nanomolar concentrations, colistin is unable to reverse inhibition
-
alpha1-antitrypsin
-
physiological inhibitor of neutrophil elastase. HL-60 cells neutralize neutrophil elastase activity by concomitant secretion of alpha1-antitrypsin
-
Alpha1-proteinase inhibitor
-
-
-
Alpha1-proteinase inhibitor
-
-
-
Aprotinin
-
no inhibition of proteinase 2A and 2B
Eglin c
-
at a therapeutic concentration of 0.0005 mM eglin c will inhibit leukocyte elastase in one second and will bind this enzyme in a pseudo-irreversible manner
Eglin c
-
inhibition by a synthetic trihexacontapeptide corresponding to the sequence 8-70 of eglin c, no inhibition by a synthetic nonapeptide corresponding to the sequence 41-19 of eglin c
elafin
-
a potent, substratelike, but fully reversible inhibitor
-
elafin
-
cationic protease inhibitor of human neutrophil elastase
-
elafin
-
also known as elastase specific inhibitor, skin-derived antileukoprotease, or trappin-2
-
elafin
-
substrate inhibitor of neutrophil elastase, the purified fragments of the cleaved inhibitor elafin, Lys6-Gln57 and Ser10-Gln57, are also still active for inhibiting neutrophil elastase
-
elafin
-
complete inhibition at 0.01 mM
-
EPI-hNE-4
-
potent and specific inhibitor of neutrohil elastase
-
EPI-hNE-4
-
highly specific, potent inhibitor, protective effect in repeated injury animal model
-
GW475151
-
i.e. (3S,3aS,6aR)-3-isopropyl-1-methanesulfonyl-4-(2-pyrrolidin-1-ylmethyl-oxazole-4-carbonyl)hexahydro-pyrrolo-[3,2-b]pyrrol-2-one hydrochloride
GW475151
suicide inhibitor
heparin
-
tight-binding non-competitive inhibitor, 90% inhibition at 0.5 ng/ml, higher chain length of oligosaccharides causes stronger inhibition, desulfated heparins lack inhibitory potential, ionic strength above 0.5 abolishes the inhibitory capacity of heparin
heparin
-
low molecular weight and semi-synthetic heparin samples with homogeneous degree of polymerization and saccharide backbone, mixed hyperbolic binding process, sulfation patterns, overview
heparin
-
strong inhibition, partly reversible by addition of colistin
heparin
-
tight-binding non-competitive inhibitor, 90% inhibition at 0.5 ng/ml, higher chain length of oligosaccharides causes stronger inhibition, desulfated heparins lack inhibitory potential, ionic strength above 0.5 abolishes the inhibitory capacity of heparin
horse leukocyte elastase inhibitor
-
protein with a molecular weight of 35200 Da that forms sodium dodecylsulfate-stable equimolar complexes with elastase
-
horse leukocyte elastase inhibitor
-
protein with a molecular weight of 35200 Da that forms sodium dodecylsulfate-stable equimolar complexes with elastase
-
L-658758
-
-
L-658758
-
the neutrophil elastase inhibitor prevents ischemia/reperfusion-induced decreases of hepatic tissue levels of CGRP and IGF-I
leukocyte elastase inhibitor
-
-
-
leukocyte elastase inhibitor
-
i.e. LEI, inhibits leukocyte elastase, and also influences the automodification of poly(ADP-ribose) polymerase-1, PARP-1, which does not influence the inhibition of elastase by LEI, overview
-
MeO-Suc-Ala-Ala-Pro-Ala-CH2Cl
-
MeO-Suc-Ala-Ala-Pro-Ala-CH2Cl
suicide inhibitor
MeO-Suc-Ala-Ala-Pro-Val-CH2Cl
-
MeO-Suc-Ala-Ala-Pro-Val-CH2Cl
suicide inhibitor
methoxysuccinyl-Ala-Ala-Pro-Val-CH2Cl
-
-
methoxysuccinyl-Ala-Ala-Pro-Val-CH2Cl
-
methoxysuccinyl-Ala-Ala-Pro-Val-chloromethylketone
-
-
methoxysuccinyl-Ala-Ala-Pro-Val-chloromethylketone
-
specific inhibitor
methoxysuccinyl-Ala-Ala-Pro-Val-chloromethylketone
-
-
monocyte/neutrophil elastase inhibitor
-
i.e. MNEI, a 42 kDA serpin protein
-
monocyte/neutrophil elastase inhibitor
-
i.e. MNEI, a 42 kDA serpin protein, 96.5% inhibition at 25 nM of a purified recombinant enzyme, in vivo inhibition of neutrophil elastase in rat lungs by daily administration leading to reduced inflammation and injury and enhanced clearance of Pseudomonas aeruginosa, overview, no in vitro bactericidal effect on Pseudomonas aeruginosa
-
N-(methoxysuccinyl)-Ala-Ala-Pro-Val-chloromethyl ketone
-
complete inhibition at low micromolar concentrations, colistin is unable to reverse the complete inhibition with 0.005 mM but able to reverse the partial inhibition with 0.0005 mM N-(methoxysuccinyl)-Ala-Ala-Pro-Val-chloromethyl ketone
N-(methoxysuccinyl)-Ala-Ala-Pro-Val-chloromethyl ketone
-
-
ONO-5046
-
-
ONO-5046
-
a specific inhibitor
ONO-5046
-
selective NE inhibitor, also known as elastase inhibitor IV
ONO-5046
-
specific neutrophil elastase inhibitor
ovomucoid
-
chicken ovomucoid; turkey ovomucoid
-
ovomucoid
-
turkey ovomucoid
-
serpin B1
-
-
-
sivelestat
-
-
sivelestat
-
also known as Elaspol, a synthetic inhibitor of neutrophil elastase with high specificity
sivelestat
-
selective neutrophil elastase inhibitor
sivelestat
-
a selective neutrophil elastase inhibitor
sivelestat
-
inhibits the enzyme and reduces brain edema and vascular permeability , and subsequently improves the neurological deficits in an acute focal ischemia. The inhibitor rescues the cultured endothelial cells from neutrophil elastase-induced damage. It can protect the blood-brain barrier function in acute cerebral ischemia
sivelestat
-
a specific inhibitor of neutrophil elastase, it reduces the risk for ling dysfunction in patients after undergoing on-pump coronary artery bypass surgery, clinical study, overview
sivelestat
-
ONO-5046, competitive and selective inhibitor
sivelestat
-
i.e. N-[2-[4-(2,2-dimethyl-propionyloxy)phenylsulfonylamino]benzoyl]aminoacetatetetrahydrate or ONO-5046, specific neutrophil elastase inhibitor, intravenous infusion of sivelestat at 3 mg/kg/h 0-22 h after Streptococcus pneumoniae inoculation reduces the increase in neutrophil elastase activity
sivelestat
-
a neutrophil elastase inhibitor, silvelestat-mediated enzyme inhibition is an effective therapeutic option in liver transplantation and other inflammation disease states, it amelioreates the hepatocellular damage and increases local neutrophil activity and infiltration with reduction of expression of proinflammatory cytokines in macrophages
sivelestat
-
selective neutrophil elastase inhibitor
sivelestat
-
a neutrophil elastase inhibitor, effect on leukocyte dynamics in the liver microcirculation after hepatic ischemia-reperfusion, Leukocyte dynamics in sinusoids, overview. The inhibitor significantly decreases the number of adherent leukocytes and prevents perfusion disturbance, overview
sivelestat
-
the neutrophil elastase inhibitor prevents ischemia/reperfusion-induced decreases of hepatic tissue levels of CGRP and IGF-I
sivelestat sodium hydrate
-
a selective inhibitor of neutrophil elastase, the compound is effective in reducing acute lung injury associated with systemic inflammatory response syndrome, SIRS. In patients with thoracic esophageal cancer undergoing thoracoscopic esophagectomy with extended lymph node dissection, the inhibitor treatment prevents postoperative hypercytokinemia and hypoxia secondary to SIRS in a clinical study, overview
sivelestat sodium hydrate
-
i.e. sodium N-[2-w4-(2,2-dimethylpropionyloxy) phenylsulfonylaminox benzoyl] aminoacetate tetrahydrate, a polymorphonuclear neutrophil elastase inhibitor. It may attenuate neutrophil elastase or proinflammatory cytokines, and improve pulmonary dysfunction in patients undergoing a cardiopulmonary bypass and aortic valve replacement
sivelestat sodium hydrate
-
ONO-5046, selective inhibitor
sivelestat sodium hydrate
-
highly specific synthetic inhibitor
sivelestat sodium hydrate
-
-
sivelestat sodium hydrate
-
a selective neutrophil elastase inhibitor. Its postischemic infusion protects against myocardial stunning in swine, overview
SSR69071
-
i.e. 2-(9-(2-piperidinoethoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yloxymethyl)-4-(1-methylethyl)-6-methoxy-1,2-benzisothiazol-3-one-1,1-dioxide, a selective, orally active, and potent inhibitor of leukocyte elastase with good penetration in respiratory tissues
ursolic acid
-
IC50: 0.0337
ursolic acid
-
highest inhibitory potency
additional information
-
peptidyl trifluoromethyl ketone inhibitors can achieve high levels of oral activity and bioavailibility, and therefore they may prove useful as therapeutic agents in the treatment of diseases in which elastase is implicated
-
additional information
-
shows no activity as inhibitor
-
additional information
-
neither leupeptin, E-64, pepstatin A, benzamidine, soybean trypsin inhibitor, Nalpha-tosyl-L-lysine chloromethyl ketone, N-p-tosyl-L-phenylalanine chloromethyl ketone, EDTA, GM6001, nor phosphoramidon have any inhibitory effect
-
additional information
-
extracts from 12 Arnica species show inhibition of 10-97% for platelet-activating factor-induced neutrophil elastase release and 1-100% for N-formyl-L-methionyl-L-leucyl-L-phenylalanine-induced neutrophil elastase release from neutrophils
-
additional information
-
an imbalance between neutrophil elastase and its inhibitors in blood is related to the development of acute respiratory distress syndrome
-
additional information
-
budlein A inhibits neutrophil elastase release from neutrophils at 0.01683 mM for formylated bacterial tripeptide-induced release and at 0.01184 mM for platelet aggregation factor-induced release
-
additional information
-
2-[2-(4-methyl-piperazin-1-yl)-pyridin-3-yl] derivative inhibitor development and synthesis, structure-activity relationship study, overview
-
additional information
-
synthesis of a series of peptide-based transition-state human neutrophil elastase inhibitors with N-terminal acidic moieties, evaluation of in vitro and in vivo inhibitory activities, overview
-
additional information
-
synthesis and evaluation of benzoxazinone derivatives, inhibitory effect on neutrophil elastase, and effects on enzyme release from FMLP-activated human neutrophils, overview
-
additional information
-
MCoTI-II modification and engineering by active site loop exchanges and truncations develop analogues with potent activity against leukocyte elastase, overview. No inhibition by MCoTI-I and MCoTI-II, and by analogues MCoTI-II K10R, MCoTI-II K10Q, and by MCoTI-II truncation analogues
-
additional information
-
4-oxo-beta-lactams are selective and potent inhibitors of leukocyte elastase, 4-oxo-beta-lactams containing a heteroarylthiomethyl group on the para position of an N1-aryl moiety afforded highly potent and selective inhibition of the enzyme, even at a very low inhibitor to enzyme ratio, structure-activity relationship analysis, inhibition mechanisms, molecular modelling, overview
-
additional information
-
not inhibited by 1-(3-methylbenzoyl)-1H-indazole-3-carboxylic acid, (3-methoxyphenyl)-(3-methylindazol-1-yl)-methanone, 1-(pyridine-4-carbonyl)-1H-indazole-3-carboxylic acid ethyl ester, 1-(naphthalene-1-carbonyl)-1H-indazole-3-carboxylic acid ethyl ester, 1-(3,4,5-trimethoxybenzoyl)-1H-indazole-3-carboxylic acid ethyl ester, 1-(pyridine-4-carbonyl)-1H-indazole-3-carboxylic acid phenylamide, 1-(toluene-4-sulfonyl)-1H-indazole-3-carboxylic acid phenylamide, 1-(4-chlorobenzenesulfonyl)-1H-indazole-3-carboxylic acid phenylamide, 1-(4-chlorobenzyl)-1H-indazole-3-carboxylic acid phenylamide, 1-(4-chlorophenyl)-1H-indazole-3-carboxylic acid phenylamide, 1-(2-oxo-2-phenylethyl)-1H-indazole-3-carboxylic acid ethyl ester, 1-(4-chlorophenylcarbamoyl)-1H-indazole-3-carboxylic acid ethyl ester, and 1-(3-methoxyphenylcarbamoyl)-1H-indazole-3-carboxylic acid ethyl ester
-
additional information
-
neutrophil elastase is not inhibited by 4-aminobenzoic acid hydrazide
-
additional information
-
not inhibited by dalbergioidin, 3(S)-2',4'-dihydroxy-5,5'-dimethoxy-(6'',6''-dimethylpyano)-(2'',3'':7,6)-isoflavan, myrsininone A, isosophoranone, myrsininone B, and 3'-geranyl-5,7,2',5'-tetrahydroxyisoflavone
-
additional information
-
neutrophil elastase inhibitor treatment ameliorated hepatocellular damage and decreased local neutrophil infiltration, as assessed by myeloperoxidase assay, naphthol AS-D chloroacetate esterase stains, and immunohistochemistry. Expression of pro-inflammatory cytokines and chemokines is reduced, overview
-
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0.000072
(2-(3,5-bis-trifluoromethyl-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
0.00002
(2-(3,5-difluoro-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
0.0000036
(2-(4-amino-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
0.000018
(2-(4-chloro-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
0.000009 - 0.000101
(2-(4-formylamino-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
0.0000081
(2-(4-methoxy-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
0.000017
(2-(4-nitro-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
0.000057
(2-cyclohexyl-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
0.00017
(2-isopropyl-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
0.0000082
(6-oxo-2-(4-fluorophenyl)-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
0.0000066
(6-oxo-2-phenyl-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
0.000033
(6-oxo-2-pyridin-3-yl-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
0.000043
(6-oxo-2-[4-(2,2,2-trifluoro-acetylamino)-phenyl]-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
0.01634
(E)-3-(3-(3,7-dimethylocta-2,6-dienyl)-2,4-dihydroxyphenyl)-3,5,7-trihydroxy-chroman-4-one
-
at pH 8.0, temperature not specified in the publication
0.0000067
(S)-1-[(S)-2-(4-methoxybenzamido)-3-methylbutyryl]-N-[(S)-2-methyl-1-(trifluoroacetyl)propyl]pyrrolidine-2-carboxamide
-
-
0.000015
1(6H)-Pyrimidineacetamide, 2-(4-aminophenyl)-5-[(methylsulfonyl)amino]-6-oxo-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
-
0.000046
1(6H)-Pyrimidineacetamide, 2-(4-fluorophenyl)-5-(methylamino)-6-oxo-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
-
0.000026
1(6H)-Pyrimidineacetamide, 5-(ethylamino)-6-oxo-2-(2-thienyl)-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
-
0.0001
1(6H)-Pyrimidineacetamide, 5-(formylamino)-6-oxo-2-(2-thienyl)-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
-
0.0000049
1(6H)-Pyrimidineacetamide, 5-amino-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]-6-oxo-2-(2-thienyl)-
-
-
0.0000016 - 0.0000077
1(6H)-Pyrimidineacetamide, 5-[[(cyclohexylamino)sulfonyl]amino]-2-(4-fluorophenyl)-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]-6-oxo-
0.000094
1(6H)-Pyrimidineacetamide, 6-oxo-2-phenyl-5-[(trifluoroacetyl)amino]-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
-
0.00000574
1,2,5-thiadiazolidin-3-one 1,1-dioxide
-
-
0.000004
1-methyl-1H-tetrazole-5-thiol
-
-
0.00052
2-(5-amino-6-oxo-2-thien-2-ylpyrimidin-1(6H)-yl)-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide
-
-
0.000127 - 0.00138
2-(thiophen-2-ylcarbonylthio)-N-(2-oxo-2,3,4,5-tetrahydrothiophen-3-yl)propionamide
0.0015
2-chloro-4-(1-hydroxyoctadecyl)benzoic acid
-
pH 8.0, 30°C
0.0000016
2-[2-(4-fluorophenyl)-6-oxo-5-[(cyclohexylsulfamoyl)-amino]-1,6-dihydro-1-pyrimidinyl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide
-
pH 7.4
0.00027
2-[5-amino-2-(3,5-difluorophenyl)-6-oxopyrimidin-1(6H)-yl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide
-
-
0.0000062 - 0.000052
2-[5-amino-6-oxo-2-(4-fluorophenyl)-1,6-dihydro-1-pyrimidinyl]-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]acetamide
0.000011
2-[5-[(benzyloxycarbonyl)amino]-6-oxo-2-(2-thienyl)-1,6-dihydro-1-pyrimidinyl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide
-
pH 7.4
0.0000006
4-(4-bromophenylsulfonylcarbamoyl)benzoyl-L-valyl-L-proline 1 (RS)-(1-trifluoroacetyl-2-methylpropyl)amide
-
-
0.000025
6-amino-2-(2,2,2-trifluoro-acetylamino)-hexanoic acid [1-(4-trifluoromethyl-phenylcarbamoyl)-ethyl]-amide
-
-
0.000007
7-(4-chlorophenylsulfonyl-L-glutamyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one
0.000016
7-(4-chlorophenylsulfonyl-L-lysyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one
0.0000018
Ala15-reactive site variant of aprotinin
-
0.0000002 - 0.00037
alpha-aminobutyric acid15-reactive site variant of aprotinin
-
0.0000002 - 0.00022
alpha-aminovaleric acid15-reactive site variant of aprotinin
-
0.000027
Carbamic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-(2-thienyl)-5-pyrimidinyl]-, 1-methylethyl ester
-
-
0.000043
Carbamic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-(2-thienyl)-5-pyrimidinyl]-, 2,2,2-trifluoroethyl ester
-
-
0.000042
Carbamic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-(2-thienyl)-5-pyrimidinyl]-, methyl ester
-
-
0.00004
Carbamic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-phenyl-5-pyrimidinyl]-, 2,2,2-trifluoroethyl ester
-
-
0.00000096
Carbamic acid, [2-(4-fluorophenyl)-1,6-dihydro-1-[2-[[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]amino]-2-oxoethyl]-6-oxo-5-pyrimidinyl]-, (3,5-dimethyl-4-pyridinyl)methyl ester
-
-
0.000022
Carbamic acid, [2-(4-fluorophenyl)-1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-5-pyrimidinyl]-, 2-pyridinylmethyl ester
-
-
0.000023
Carbamic acid, [2-(4-fluorophenyl)-1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-5-pyrimidinyl]-, 4-pyridinylmethyl ester
-
-
0.000016
Carbamothioic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-phenyl-5-pyrimidinyl]-, S-methyl ester
-
-
0.000023
Carbamothioic acid, [2-(4-fluorophenyl)-1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-5-pyrimidinyl]-, S-methyl ester
-
-
0.025
CF3-CO-Ala-Ala-4-nitroanilide
-
-
0.17
CF3-CO-Ala-Ala-Ala
-
-
0.000000075
Eglin c
-
pH 7.3, 37°C
0.00000008 - 0.0000067
elafin
-
0.4
glutaryl-Ala-Ala-Pro-NH-C3H7
-
-
0.00000031
GW311616
-
pH 7.4, 30°C
0.000000014
GW447631
-
pH 7.4, 30°C
0.00000173
GW469002
-
pH 7.4, 30°C
0.00000016
GW475151
-
pH 7.4, 30°C
1.8
H-Ala-Ala-Pro-Ala-OH
-
-
0.000036
insulapeptolide D
-
in 50 mM sodium phosphate buffer (100 mM NaCl, pH 7.8), at 25°C
0.000058
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1R)-3,3-difluoro-1-(1-methylethyl)-2,4-dioxo-4-[(2-pyridinylmethyl)amino]butyl]-
-
-
0.0000031
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-3,3-difluoro-1-(1-methylethyl)-2,4-dioxo-4-[(2-pyridinylmethyl)amino]butyl]-
-
-
0.00000035
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-3,3-difluoro-1-(1-methylethyl)-2-oxo-4-[(phenylmethyl)amino]butyl]-
-
-
0.0000038
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-3,3-difluoro-4-(methylamino)-1-(1-methylethyl)-2,4-dioxobutyl]-
-
-
0.0000064
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-4-(benzoylamino)-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
-
0.000015
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-4-amino-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
-
0.0000034
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-4-[[(1,1-dimethylethoxy)carbonyl]amino]-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
-
0.0000033
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
-
0.0000017
L-Prolinamide, N-(phenoxycarbonyl)-L-valyl-N-[(1S)-3,3-difluoro-1-(1-methylethyl)-2,4-dioxo-4-[(2-pyridinylmethyl)amino]butyl]-
-
-
0.00000085
L-Prolinamide, N-(phenoxycarbonyl)-L-valyl-N-[(1S)-3,3-difluoro-4-(methylamino)-1-(1-methylethyl)-2,4-dioxobutyl]-
-
-
0.00000035
L-Prolinamide, N-(phenoxycarbonyl)-L-valyl-N-[(1S)-4-[[(1,1-dimethylethoxy)carbonyl]amino]-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
-
0.0000015
L-Prolinamide, N-(phenoxycarbonyl)-L-valyl-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
-
0.0000016
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-3,3-difluoro-1-(1-methylethyl)-2-oxo-4-[(phenylmethyl)amino]butyl]-
-
-
0.000003
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-3,3-difluoro-4-(methylamino)-1-(1-methylethyl)-2,4-dioxobutyl]-
-
-
0.00000038
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-4-amino-3,3-difluoro-1-(1-methylethyl)-2,4-dioxobutyl]-
-
-
0.00013
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-4-amino-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
-
0.0000011
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-4-[[(1,1-dimethylethoxy)carbonyl]amino]-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
-
0.0000026
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
-
0.004
m-CF3-C6H4-CO-Ala-Ala-4-nitroanilide
-
-
0.000032
MCoTI-II K10A
-
pH not specified in the publication, temperature not specified in the publication
0.0075
MCoTI-II K10F
-
pH not specified in the publication, temperature not specified in the publication
0.000021
MCoTI-II K10V
-
pH not specified in the publication, temperature not specified in the publication
0.06
N-(1-(1-[1-(4-benzoyl-phenylcarbamoyl)-2-methyl-propylcarbamoyl]-3-methyl-butylcarbamoyl)-2-(4-hydroxy-phenyl)-ethyl)-succinamic acid
-
-
0.00011
N-(5-(adamantane-1-sulfonylamino)-5-[1-(1-formyl-2-methyl-propylcarbamoyl)-ethylcarbamoyl]-pentyl)-succinamic acid
-
-
0.00006
N-(5-(adamantane-1-sulfonylamino)-5-[1-(1-formyl-2-methyl-propylcarbamoyl)-ethylcarbamoyl]-pentyl)-terephthalamic acid
-
-
0.000035
N-(5-benzyloxycarbonylamino-1-(1-[2-(1-formyl-2-methyl-propylcarbamoyl)-pyrrolidine-1-carbonyl]-2-methyl-propylcarbamoyl)-pentyl)-succinamic acid
-
-
0.0007
N-galloyl-4-alkyliden-beta-lactam
-
-
0.00007 - 0.0058
oleoyl-Ala-Ala-Pro-Ala
0.004
oleoyl-Ala-Ala-Pro-Val
-
-
0.00000027
Pro44-eglin c
-
-
-
0.000058
semisynthetic glucan sulfate LMWH
-
37°C
-
0.0000185
semisynthetic glucan sulfate PPS
-
37°C
-
0.0000132
semisynthetic glucan sulfate PS3
-
37°C
-
0.000012
semisynthetic glucan sulfate PulS1
-
37°C
-
0.0000215
semisynthetic glucan sulfate PulS2
-
37°C
-
0.000036
semisynthetic glucan sulfate PulS3
-
37°C
-
0.000044
semisynthetic glucan sulfate PulS4
-
37°C
-
0.0000034
semisynthetic glucan sulfate PulS5
-
37°C
-
0.000001
semisynthetic glucan sulfate PulS6
-
37°C
-
0.0000008
semisynthetic glucan sulfate PulS7
-
37°C
-
0.0000056
semisynthetic glucan sulfate UFH
-
37°C
-
0.0000000168 - 0.000058
SSR69071
0.12
succinyl-Tyr-D-Leu-D-Val-4-nitroanilide
-
-
0.0000022
synthetic trihexacontapeptide corresponding to the sequence 8-70 of eglin c
-
-
-
0.00021
tert-butoxycarbonyl-Val-Val-Val-NH-(CH2)11-CH3
-
-
0.00000003
trappin-2
-
neutrophil elastase
-
0.0000003
Val15-aminobutyric acid15-reactive site variant of aprotinin
-
pH 7.4, 25°C
-
0.000004 - 0.00012
Val15-reactive site variant of aprotinin
-
0.000005571 - 0.000139
ZD8321
0.000042
[6-Oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-2-(4-trifluoromethyl-phenyl)-1,6-dihydro-pyrimidin-5-yl]-carbamic acid benzyl ester
-
-
additional information
additional information
-
0.000009
(2-(4-formylamino-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
0.000101
(2-(4-formylamino-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
-
0.0000016
1(6H)-Pyrimidineacetamide, 5-[[(cyclohexylamino)sulfonyl]amino]-2-(4-fluorophenyl)-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]-6-oxo-
-
-
0.0000077
1(6H)-Pyrimidineacetamide, 5-[[(cyclohexylamino)sulfonyl]amino]-2-(4-fluorophenyl)-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]-6-oxo-
-
-
0.000127
2-(thiophen-2-ylcarbonylthio)-N-(2-oxo-2,3,4,5-tetrahydrothiophen-3-yl)propionamide
-
pH 7.4, 37°C, pre-steady-state analysis
0.00138
2-(thiophen-2-ylcarbonylthio)-N-(2-oxo-2,3,4,5-tetrahydrothiophen-3-yl)propionamide
-
pH 7.4, 37°C, graphic analysis
0.0000062
2-[5-amino-6-oxo-2-(4-fluorophenyl)-1,6-dihydro-1-pyrimidinyl]-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]acetamide
-
pH 7.4
0.000052
2-[5-amino-6-oxo-2-(4-fluorophenyl)-1,6-dihydro-1-pyrimidinyl]-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]acetamide
-
pH 7.4
0.000007
7-(4-chlorophenylsulfonyl-L-glutamyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one
-
pH 7.5, 37°C
0.000007
7-(4-chlorophenylsulfonyl-L-glutamyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one
-
pH 7.5, 37°C
0.000016
7-(4-chlorophenylsulfonyl-L-lysyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one
-
pH 7.5, 37°C
0.000016
7-(4-chlorophenylsulfonyl-L-lysyl)amino-5-methyl-2-iso-propylamino-4H-3,1-benzoxazin-4-one
-
pH 7.5, 37°C
0.0000018
Ala15-reactive site variant of aprotinin
-
pH 7.4, 25°C
-
0.0000018
Ala15-reactive site variant of aprotinin
-
pH 7.4, 25°C
-
0.0000018
Ala15-reactive site variant of aprotinin
-
proteinase 2B
-
0.0000002
alpha-aminobutyric acid15-reactive site variant of aprotinin
-
pH 7.4, 25°C
-
0.0000004
alpha-aminobutyric acid15-reactive site variant of aprotinin
-
pH 7.4, 25°C, proteinase 2B
-
0.00037
alpha-aminobutyric acid15-reactive site variant of aprotinin
-
pH 7.4, 25°C, proteinase 2A
-
0.0000002
alpha-aminovaleric acid15-reactive site variant of aprotinin
-
pH 7.4, 25°C
-
0.0000011
alpha-aminovaleric acid15-reactive site variant of aprotinin
-
pH 7.4, 25°C, proteinase 2B
-
0.00022
alpha-aminovaleric acid15-reactive site variant of aprotinin
-
pH 7.4, 25°C, proteinase 2A
-
0.00000008
elafin
-
neutrophil elastase
-
0.00000017
elafin
-
pH 8.0, 25°C
-
0.0000002
elafin
-
pH 9.0, 25°C
-
0.0000067
elafin
-
pH 5.4, 25°C
-
0.00003 - 0.00015
heparin
-
low molecular weight and semi-synthetic heparin samples, inhibition kinetics
0.00004
heparin
-
8 disaccharide units, pH 8.0, 37°C
0.023
heparin
-
5 disaccharide units, pH 8.0, 37°C
0.1
heparin
-
2 disaccharide units, pH 8.0, 37°C
0.00007
oleoyl-Ala-Ala-Pro-Ala
-
-
0.0058
oleoyl-Ala-Ala-Pro-Ala
-
-
0.0000000168
SSR69071
-
pH 7.8
0.00000168
SSR69071
-
pH 7.8
0.00000301
SSR69071
-
pH 7.8
0.000058
SSR69071
-
pH 7.8
0.000004
Val15-reactive site variant of aprotinin
-
-
-
0.000004
Val15-reactive site variant of aprotinin
-
pH 7.4, 25°C, proteinase 2B
-
0.00012
Val15-reactive site variant of aprotinin
-
pH 7.4, 25°C, proteinase 2A
-
0.000005571
ZD8321
-
pH 7.8
0.00003475
ZD8321
-
pH 7.8
additional information
additional information
-
inhibition kinetics
-
additional information
additional information
Ki-values for variants of human pancreatic secretory trypsin inhibitor optimized with respect to the affinity and specificity for human leukocyte elastase relative to trypsin, and in particular chymotrypsin
-
additional information
additional information
-
Ki-values for variants of human pancreatic secretory trypsin inhibitor optimized with respect to the affinity and specificity for human leukocyte elastase relative to trypsin, and in particular chymotrypsin
-
additional information
additional information
-
overview, oligopeptide inhibitors, aldehyde inhibitors, carbamate inhibitors, carbazate inhibitors, trifluoromethylketone inhibitors, difluoromethylene inhibitors, boronic acid inhibitors, isocoumarin inhibitors, cephalosporin inhibitors, azetidinone inhibitors, benzothiazolinone inhibitors and various other classes
-
additional information
additional information
-
detailed inhibition kinetics of 4-oxo-beta-lactams, overview
-
additional information
additional information
-
variants of human secretory trypsin inhibitor are constructed with the aim of producing inhibitors specific for human leukocyte elastase. Models of the human pancreatic secretory trypsin inhibitor/human leukocytic elastase and human pancreatic secretory trypsin inhibitor/chymotrypsin complexes are generated by computer aided protein design and used to plan better human leukocyte elastase inhibitors
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.0128
(-)-epigallocatechin-3-gallate
Homo sapiens
-
pH 7.5, 37°C
0.1
(22E,24R)-ergosta-7,22-dien-2alpha,3alpha,9alpha-triol
Homo sapiens
-
IC50 above 0.1 mM, pH 7.5, 37°C
0.0179
(2R, 3R)-6-methyl-3'-geranyl-2,3-trans-5,7,4'-trihydroxyflavonol
Homo sapiens
-
at pH 8.0, temperature not specified in the publication
0.022
(3-methylindazol-1-yl)-m-tolyl-methanone
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.1
(3beta,5alpha,8alpha,22E)-ergosta-6,22-diene-3-ol-5,8-peroxide
Homo sapiens
-
IC50 above 0.1 mM, pH 7.5, 37°C
0.1
(3beta,5alpha,8alpha,22E)-ergosta-6,22-diene-3-ol-5,8-peroxide 3-O-beta-D-glucoside
Homo sapiens
-
IC50 above 0.1 mM, pH 7.5, 37°C
0.000025
(3R)-1-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-3-carboxylic acid
Homo sapiens
-
pH 7.4, 22°C
0.000019
(3S)-1-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-3-carboxylic acid
Homo sapiens
-
pH 7.4, 22°C
0.0085
(E)-3-(3-(3,7-dimethylocta-2,6-dienyl)-2,4-dihydroxyphenyl)-3,5,7-trihydroxy-chroman-4-one
Homo sapiens
-
at pH 8.0, temperature not specified in the publication
0.1
(E)-6-O-p-coumaroyl scandoside methyl ester
Homo sapiens
-
pH 7.5, 37°C, above
0.1
(E)-6-O-p-feruloyl scandoside methyl ester
Homo sapiens
-
pH 7.5, 37°C, above
0.018
(E)-6-O-p-methoxycinnamoyl scandoside methyl ester
Homo sapiens
-
pH 7.5, 37°C
0.1
(Z)-6-O-p-coumaroyl scandoside methyl ester
Homo sapiens
-
pH 7.5, 37°C, above
0.1
(Z)-6-O-p-methoxycinnamoyl scandoside methyl ester
Homo sapiens
-
pH 7.5, 37°C, above
0.034
1-(2-methylbenzoyl)-1H-indazole-3-carboxylic acid phenylamide
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0016
1-(3-aminobenzoyl)-1H-indazole-3-carboxylic acid ethyl ester
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0031
1-(3-aminobenzoyl)-1H-indazole-3-carboxylic acid phenylamide
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0008
1-(3-methoxybenzoyl)-1H-indazole-3-carboxylic acid ethyl ester
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00055
1-(3-methoxybenzoyl)-1H-indazole-3-carboxylic acid methyl ester
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0018
1-(3-methoxybenzoyl)-1H-indazole-3-carboxylic acid phenylamide
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0019
1-(3-methoxybenzoyl)-1H-indazole-3-carboxylic acid propyl ester
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00013
1-(3-methylbenzoyl)-1H-indazole-3-carboxylic acid methyl ester
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.038
1-(4-cyanobenzoyl)-1H-indazole-3-carboxylic acid ethyl ester
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00093
1-(thiophene-3-carbonyl)-1H-indazole-3-carboxylic acid ethyl ester
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00031
1-(thiophene-3-carbonyl)-1H-indazole-3-carboxylic acid methyl ester
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0031
1-(thiophene-3-carbonyl)-1H-indazole-3-carboxylic acid phenylamide
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0019
1-(thiophene-3-carbonyl)-1H-indazole-3-carboxylic acid propyl ester
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.000089
1-benzoyl-1H-indazole-3-carboxylic acid methyl ester
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00042
1-benzoyl-1H-indazole-3-carboxylic acid phenylamide
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00018
1-butyryl-1H-indazole-3-carboxylic acid ethyl ester
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00048
1-cyclopentanecarbonyl-1H-indazole-3-carboxylic acid ethyl ester
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0004
1-propionyl-1H-indazole-3-carboxylic acid ethyl ester
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0039
1-[(3-chlorophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0059
1-[(3-fluorophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0093
1-[(3-methylphenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.011
1-[(3-nitrophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0061
1-[(4-chlorophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.038
1-[(4-cyanophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0081
1-[(4-fluorophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.029
1-[(4-methylphenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0013
1-[3-(5-cyclobutyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
Homo sapiens
-
pH 7.4, 22°C
0.00014
1-[3-(5-cyclopropyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
Homo sapiens
-
pH 7.4, 22°C
0.0407
1-[3-(5-ethyl-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
Homo sapiens
-
pH 7.4, 22°C
0.000028
1-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
Homo sapiens
-
pH 7.4, 22°C
0.000079
1-[3-(5-methyl-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
Homo sapiens
-
pH 7.4, 22°C
0.00018
1-[3-(7-methoxy-4-oxo-5-propyl-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
Homo sapiens
-
pH 7.4, 22°C
0.00033
1-[3-[7-methoxy-4-oxo-5-(propan-2-yl)-4H-3,1-benzoxazin-2-yl]pyridin-2-yl]piperidine-4-carboxylic acid
Homo sapiens
-
pH 7.4, 22°C
0.0205
14alpha-hydroxy-ergosta-4,7,9(11),22-tetraen-3,6-dione
Homo sapiens
-
pH 7.5, 37°C
0.01
1H-indazol-1-yl(3-methylphenyl)methanone
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00026
2,2,2-trifluoroethyl 1-(phenylcarbonyl)-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00051
2,2,2-trifluoroethyl 1-(thiophen-3-ylcarbonyl)-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00034
2,2,2-trifluoroethyl 1-[(3-aminophenyl)carbonyl]-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00089
2,2,2-trifluoroethyl 1-[(3-methoxyphenyl)carbonyl]-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00046
2,2,2-trifluoroethyl 1-[(3-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.000085
2-(2-methoxypyridin-3-yl)-5-methyl-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.0093
2-(2-phenoxypyridin-3-yl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.000021
2-(2-[4-[2-(dimethylamino)ethyl]piperazin-1-yl]pyridin-3-yl)-5-ethyl-7-methoxy-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.00011
2-(2-[[2-(dimethylamino)ethyl](methyl)amino]pyridin-3-yl)-5-methyl-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.0081
2-(2-[[2-(dimethylamino)ethyl]amino]pyridin-3-yl)-5-methyl-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.000064
2-[2-(1H-imidazol-1-yl)pyridin-3-yl]-5-methyl-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.000027
2-[2-(4-butylpiperazin-1-yl)pyridin-3-yl]-5-ethyl-7-methoxy-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.000034
2-[2-(4-cyclopentylpiperazin-1-yl)pyridin-3-yl]-5-ethyl-7-methoxy-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.000028
2-[2-[4-(cyclopropylmethyl)piperazin-1-yl]pyridin-3-yl]-5-ethyl-7-methoxy-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.0308
3'-geranyl-5,7,2',4'-tetrahydroxyisoflavanone
Homo sapiens
-
at pH 8.0, temperature not specified in the publication
0.000024
3-[4-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperazin-1-yl]propanenitrile
Homo sapiens
-
pH 7.4, 22°C
0.1
3beta,5alpha,9alpha-trihydroxy-ergosta-7,22-dien-6-one
Homo sapiens
-
IC50 above 0.1 mM, pH 7.5, 37°C
0.0146
3beta,5alpha-dihydroxy-6beta-methoxyergosta-7,22-diene
Homo sapiens
-
pH 7.5, 37°C
0.1
3beta,5alpha-dihydroxy-ergosta-7,22-dien-6-one
Homo sapiens
-
IC50 above 0.1 mM, pH 7.5, 37°C
0.1
3beta-hydroxy-ergosta-7,22-dien-6-one
Homo sapiens
-
IC50 above 0.1 mM, pH 7.5, 37°C
0.000016
4-(4-bromophenylsulfonylcarbamoyl)benzoyl-L-valyl-L-proline 1 (RS)-(1-trifluoroacetyl-2-methylpropyl)amide
Homo sapiens
-
ICI 200,355, reversible, tight, and potent inhibitor, prevents the ongoing destruction of insoluble elastin by elastase, IC50: 16 nM, 4fold excess of inhibitor over enzyme causes 83% inhibition
0.000023
4-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperazine-1-carboxylic acid
Homo sapiens
-
pH 7.4, 22°C
0.0234
5-chloro-2-(2-chlorophenyl)-4H-benzo[d][1,3]oxazin-4-one
Homo sapiens
-
pH 7.4, 25°C
0.00121
5-chloro-2-(2-fluorophenyl)-4H-benzo[d][1,3]oxazin-4-one
Homo sapiens
-
pH 7.4, 25°C
0.00648
5-chloro-2-(2-methoxyphenyl)-4H-benzo[d][1,3]oxazin-4-one
Homo sapiens
-
pH 7.4, 25°C
0.00016
5-chloro-2-(2-phenoxypyridin-3-yl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.00015
5-cyclobutyl-7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.00085
5-cyclobutyl-7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.00012
5-cyclopropyl-7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.00011
5-cyclopropyl-7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.04055
5-ethyl-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.04067
5-ethyl-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.000016
5-ethyl-2-[2-[4-(2-hydroxyethyl)piperazin-1-yl]pyridin-3-yl]-7-methoxy-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.000022
5-ethyl-7-methoxy-2-(2-[4-[2-(morpholin-4-yl)ethyl]piperazin-1-yl]pyridin-3-yl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.00002
5-ethyl-7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.000028
5-ethyl-7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.000016
5-ethyl-7-methoxy-2-[2-[4-(2-methoxyethyl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.000021
5-ethyl-7-methoxy-2-[2-[4-(2-methylpropyl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.00039
5-methoxy-2-(2-phenoxypyridin-3-yl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.000087
5-methyl-2-(2-methylpyridin-3-yl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.00017
5-methyl-2-(2-phenoxyphenyl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.000061
5-methyl-2-(2-phenoxypyridin-3-yl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.006
5-methyl-2-(2-[[2-(morpholin-4-yl)ethyl]amino]pyridin-3-yl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.00071
5-methyl-2-(6-methylpyridin-3-yl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.0009
5-methyl-2-(pyridin-3-yl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.00093
5-methyl-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.000074
5-methyl-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.000015
5-tert-butyl-7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.0352
5alpha,6alpha,8alpha,9alpha-diepoxy-ergost-22-en-3beta,7alpha-diol
Homo sapiens
-
pH 7.5, 37°C
0.0282
5alpha,6alpha-epoxy-ergosta-8(14),22-diene-3beta,7alpha-diol
Homo sapiens
-
pH 7.5, 37°C
0.0751
5alpha,6alpha-epoxy-ergosta-8(9),22-dien-7-one-3beta-ol
Homo sapiens
-
pH 7.5, 37°C
0.0053
7-(dimethylamino)-5-ethyl-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.0026
7-(dimethylamino)-5-ethyl-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.002
7-chloro-2-(2-bromophenyl)-4H-benzo[d][1,3]oxazin-4-one
Homo sapiens
-
pH 7.4, 25°C
0.00268
7-chloro-2-(2-chlorophenyl)-4H-benzo[d][1,3]oxazin-4-one
Homo sapiens
-
pH 7.4, 25°C
0.00138
7-chloro-2-(2-fluorophenyl)-4H-benzo[d][1,3]oxazin-4-one
Homo sapiens
-
pH 7.4, 25°C
0.00021
7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-5-(propan-2-yl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.00025
7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-5-propyl-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.00014
7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-5-(propan-2-yl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.000071
7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-5-propyl-4H-3,1-benzoxazin-4-one
Homo sapiens
-
pH 7.4, 22°C
0.0178
clitocybin D
Homo sapiens
-
pH 7.5, 37°C
0.0552
ergosta-4,7,22-trien-3,6-dione
Homo sapiens
-
pH 7.5, 37°C
0.1
ergosta-7,22-dien-2beta,3alpha,9alpha-triol
Homo sapiens
-
IC50 above 0.1 mM, pH 7.5, 37°C
0.0775
ergosta-7,22-dien-3beta,5alpha,6beta,9alpha-tetraol
Homo sapiens
-
pH 7.5, 37°C
0.0645
ergosterol
Homo sapiens
-
pH 7.5, 37°C
0.028
ethyl 1-(1,3-benzodioxol-5-ylcarbonyl)-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0004
ethyl 1-(phenylcarbonyl)-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0048
ethyl 1-acetyl-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.052
ethyl 1-[(2-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0017
ethyl 1-[(3-chlorophenyl)carbonyl]-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0017
ethyl 1-[(3-fluorophenyl)carbonyl]-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00041
ethyl 1-[(3-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.019
ethyl 1-[(4-chlorophenyl)carbonyl]-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0057
ethyl 1-[(4-fluorophenyl)carbonyl]-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.036
ethyl 1-[(4-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00014
insulapeptolide A
Homo sapiens
-
in 50 mM sodium phosphate buffer (100 mM NaCl, pH 7.8), at 25°C
0.0001
insulapeptolide B
Homo sapiens
-
in 50 mM sodium phosphate buffer (100 mM NaCl, pH 7.8), at 25°C
0.00009
insulapeptolide C
Homo sapiens
-
in 50 mM sodium phosphate buffer (100 mM NaCl, pH 7.8), at 25°C
0.000085
insulapeptolide D
Homo sapiens
-
in 50 mM sodium phosphate buffer (100 mM NaCl, pH 7.8), at 25°C
0.0032
insulapeptolide E
Homo sapiens
-
in 50 mM sodium phosphate buffer (100 mM NaCl, pH 7.8), at 25°C
0.0016
insulapeptolide F
Homo sapiens
-
in 50 mM sodium phosphate buffer (100 mM NaCl, pH 7.8), at 25°C
0.0035
insulapeptolide G
Homo sapiens
-
in 50 mM sodium phosphate buffer (100 mM NaCl, pH 7.8), at 25°C
0.0027
insulapeptolide H
Homo sapiens
-
in 50 mM sodium phosphate buffer (100 mM NaCl, pH 7.8), at 25°C
0.001 - 0.002
N-galloyl-4-alkyliden-beta-lactam
Homo sapiens
-
-
0.00377
nigranoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.02168
oleanolic acid
Homo sapiens
-
at pH 8.0, temperature not specified in the publication
0.000044
ONO-5046
Mus musculus
-
-
0.00024
propan-2-yl 1-(phenylcarbonyl)-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00069
propan-2-yl 1-(thiophen-3-ylcarbonyl)-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00051
propan-2-yl 1-[(3-aminophenyl)carbonyl]-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00076
propan-2-yl 1-[(3-methoxyphenyl)carbonyl]-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00065
propan-2-yl 1-[(3-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0004
propyl 1-(phenylcarbonyl)-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0007
propyl 1-[(3-aminophenyl)carbonyl]-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.00078
propyl 1-[(3-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
Homo sapiens
-
in 200 mM Tris-HCl, pH 7.5, at 25°C
0.0000181
semisynthetic glucan sulfates
Homo sapiens
-
with pullulan as basic polysaccharide: PulS1, PulS2, PulS3 (IC50: 0.0000181 mM), PulS4, PulS5, PulS6 and PulS7, with glucuronoxylan as basic polysaccharide: PPS, and with phycarine as basic polysaccharide: PS3
-
0.00551 - 0.0337
ursolic acid
0.00551
ursolic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0337
ursolic acid
Homo sapiens
-
IC50: 0.0337 mM
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