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Information on EC 3.4.21.39 - chymase and Organism(s) Homo sapiens and UniProt Accession P23946

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     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.21 Serine endopeptidases
                3.4.21.39 chymase
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Select one or more organisms in this record:
This record set is specific for:
Homo sapiens
UNIPROT: P23946 not found.
Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Reaction Schemes
preferential cleavage: Phe-/- > Tyr-/- > Trp-/- > Leu-/-
Synonyms
alpha-chymase, beta-chymase, CAGE, Chy, chymase, chymase 1, chymostatin sensitive angiotensin generating enzyme, chymotrypsin-like protease, chymotryptic mast cell peptidase, CLP, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
chymase
chymostatin sensitive angiotensin generating enzyme
247
-
chymotrypsin-like protease
247
-
chymotryptic mast cell peptidase
247
-
CLP
247
-
CMA
247
-
mast cell chymase
mast cell protease
247
-
mast cell protease I
-
-
-
-
mast cell-derived chymase
247
-
mast-cell-derived chymase
247
-
MC chymase
MC-derived chymase
247
-
MC-specific chymase
296838
-
Mcpt
247
-
MMCP-1
-
-
-
-
proteinase, mast cell serine, chymase
-
-
-
-
RMCP I
-
-
-
-
skeletal muscle protease
-
-
-
-
skin chymotryptic proteinase
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY hide
97501-92-3
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
angiotensin I + H2O
angiotensin II + His-Leu
show the reaction diagram
biglycan + H2O
?
show the reaction diagram
-
-
-
?
heat shock protein 70 + H2O
?
show the reaction diagram
-
-
-
?
HMGB1 + H2O
?
show the reaction diagram
-
-
-
?
interleukin-33 + H2O
?
show the reaction diagram
-
-
-
?
N-succinyl-L-Leu-L-Leu-L-Val-L-Tyr-4-nitroanilide + H2O
N-succinyl-L-Leu-L-Leu-L-Val-L-Tyr + 4-nitroaniline
show the reaction diagram
-
-
-
?
pro-collagen + H2O
collagen + ?
show the reaction diagram
-
-
-
-
?
pro-interleukin-1beta + H2O
interleukin-1beta + ?
show the reaction diagram
-
-
-
-
?
pro-matrix metalloproteinase-1 + H2O
matrix metalloproteinase-1 + ?
show the reaction diagram
-
-
-
-
?
pro-matrix metalloproteinase-3 + H2O
matrix metalloproteinase-3 + ?
show the reaction diagram
-
-
-
-
?
pro-matrix metalloproteinase-9 + H2O
matrix metalloproteinase-9 + ?
show the reaction diagram
-
-
-
-
?
pro-transforming growth factor-beta + H2O
transforming growth factor-beta + ?
show the reaction diagram
-
-
-
-
?
pro-transforming growth factor-beta1 + H2O
transforming growth factor-beta1 + ?
show the reaction diagram
-
-
-
-
?
succinyl-L-Leu-L-Leu-L-Val-L-Tyr-4-nitroanilide + H2O
succinyl-L-Leu-L-Leu-L-Val-L-Tyr + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
Vitronectin + H2O
?
show the reaction diagram
-
-
-
-
?
2-aminobenzoyl-Asp-Arg-Val-Tyr-Ile-His-Pro-Phe-His-Dab(DNP) + H2O
2-aminobenzoyl-Asp-Arg-Val-Tyr-Ile-His-Pro-Phe + His-Dab(DNP)
show the reaction diagram
-
the enzyme cleaves between Phe and His of modified angiotensin I permitting the release of His-[2-amino-4-(2,3-dinitrophenylamino)-butyrate]
-
-
?
Abz-GIAPFCDLMPEQ-EDDnp + H2O
?
show the reaction diagram
-
-
-
-
?
Abz-GIATFCDLMPEQ-EDDnp + H2O
?
show the reaction diagram
-
-
-
-
?
Abz-GIATFCMLMPEQ-EDDnp + H2O
?
show the reaction diagram
-
-
-
-
?
Abz-GIATFCPLMPEQ-EDDnp + H2O
?
show the reaction diagram
-
-
-
-
?
Abz-GIATFCRLMPEQ-EDDnp + H2O
?
show the reaction diagram
-
-
-
-
?
Abz-GIATFDMLMPEQ-EDDnp + H2O
?
show the reaction diagram
-
-
-
-
?
Abz-GIATFRMLMPEQ-EDDnp + H2O
?
show the reaction diagram
-
-
-
-
?
Abz-GIATFSMLMPEQ-EDDnp + H2O
?
show the reaction diagram
-
-
-
-
?
Abz-GIATFWMLMPEQ-EDDnp + H2O
?
show the reaction diagram
-
-
-
-
?
Abz-GIEPFSDPMPEQ-EDDnp + H2O
?
show the reaction diagram
-
-
-
-
?
Abz-TPFSALQ-EDDnp + H2O
?
show the reaction diagram
-
-
-
-
?
Abz-TPWSALQ-YNO2 + H2O
?
show the reaction diagram
-
-
-
-
?
acetyltyrosine ethyl ester + H2O
acetyl-Tyr + ethanol
show the reaction diagram
-
-
-
-
?
Ala-Ala-Pro-Leu-4-nitroanilide + H2O
Ala-Ala-Pro-Leu + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
Ala-Ala-Pro-Met-4-nitroanilide + H2O
Ala-Ala-Pro-Met + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
Ala-Ala-Pro-Phe-4-nitroanilide + H2O
Ala-Ala-Pro-Phe + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
angiotensin I + H2O
angiotensin II + ?
show the reaction diagram
-
-
-
-
?
angiotensin I + H2O
angiotensin II + His-Leu
show the reaction diagram
angotensin I + H2O
angiotensin II
show the reaction diagram
-
-
-
-
?
Big endothelin-1 + H2O
?
show the reaction diagram
-
-
-
-
?
big-endothelin-1 (1-38) + H2O
endothelin-1 (1-31) + ?
show the reaction diagram
-
chymase cleaves the tyrosine31-glycine32 peptide bond of big-endothelin-1 (1-38)
-
-
?
CAAPFW + H2O
?
show the reaction diagram
-
-
-
-
?
chemerin + H2O
?
show the reaction diagram
-
mast cell chymase abolishes chemerin activity by the removal of additional amino acids from its C-terminus, this effect is specific to bioactive chemerin (chemerin-157 and to a lesser extent chemerin-156)
-
-
?
cholesteryl ester transfer protein + H2O
?
show the reaction diagram
-
-
-
-
?
cholesteryl ester transfer protein-high density lipoprotein complex + H2O
?
show the reaction diagram
-
-
-
-
?
collagen type IV + H2O
?
show the reaction diagram
-
-
-
-
?
connective tissue-activating peptide III + H2O
neutrophil-activating peptide 2 + precursorpeptide
show the reaction diagram
-
i.e. CTAP-II
i.e. NAP-2
-
?
DRVWIHPFHL + H2O
?
show the reaction diagram
-
-
-
-
?
DRVWIHPLHL + H2O
?
show the reaction diagram
-
-
-
-
?
DRVWIHPWHL + H2O
?
show the reaction diagram
-
-
-
-
?
Fibronectin + H2O
?
show the reaction diagram
-
-
-
-
?
interleukin 1beta precursor + H2O
?
show the reaction diagram
-
-
-
-
?
latent transforming growth factor-beta + H2O
active transforming growth factor-beta + ?
show the reaction diagram
-
-
-
-
?
MeO-succinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
MeO-succinyl-Ala-Ala-Pro-Val + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
methoxy-succinyl-Arg-Ala-Tyr-4-nitroanilide + H2O
methoxy-succinyl-Arg-Ala-Tyr + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
methoxysuccinyl-Arg-Ala-Tyr-4-nitroanilide + H2O
methoxysuccinyl-Arg-Ala-Tyr + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
MR121-CAAPFW + H2O
?
show the reaction diagram
-
-
-
-
?
N-succinyl-Ala-His-Pro-Phe-4-nitroanilide + H2O
N-succinyl-Ala-His-Pro-Phe + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
N-succinyl-L-alanyl-L-alanyl-L-prolyl-L-phenylalanine-p-nitroanilide + H2O
N-succinyl-L-alanyl-L-alanyl-L-prolyl-L-phenylalanine + p-nitroaniline
show the reaction diagram
-
-
-
-
?
neurotensin + H2O
?
show the reaction diagram
-
-
-
-
?
plasmin + H2O
?
show the reaction diagram
-
-
-
-
?
pro-interleukin-18 + H2O
interleukin-18 fragments
show the reaction diagram
-
cleaves recombinant pro-interleukin-18 at 56-Phe
16 and 20 kDa fragments, the 16 kDa fragment is biologically active
-
?
promatrix metalloproteinase 9 + H2O
matrix metalloproteinase 9
show the reaction diagram
-
-
-
-
?
promatrix metalloproteinase-2 + H2O
matrix metalloproteinase-2
show the reaction diagram
-
-
-
-
?
promatrix metalloproteinase-9 + H2O
matrix metalloproteinase-9
show the reaction diagram
-
-
-
-
?
secretory leucocyte protease inhibitor + H2O
?
show the reaction diagram
-
cleaved secretory leucocyte protease inhibitor is a biomarker of chymase activity
-
-
?
secretory leukocyte protease inhibitor + H2O
?
show the reaction diagram
-
the cleavage of recombinant human secretory leukocyte protease inhibitor by human chymase occurres at Leu72-Met73
the cleaved form of SLPI can be used as a biomarker of chymase activity
-
?
succinyl-AAPF-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Ala-Ala-Pro-Leu-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Ala-Ala-Pro-Met-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Ala-Ala-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Ala-Ala-Pro-Phe-4-nitroanilide + H2O
succinyl-Ala-Ala-Pro-Phe + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
succinyl-Ala-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-epsilon-(2-picolinyl)Lys-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-epsilon-(2-picolinyl)Lys-Val-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Gln-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Glu-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Glu-Val-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Gly-Gly-Phe-p-nitroanilide + H2O
succinyl-Gly-Gly-Phe + p-nitroaniline
show the reaction diagram
-
-
-
-
?
succinyl-L-Ala-L-Ala-L-Pro-L-Phe-4-nitroanilide + H2O
succinyl-L-Ala-L-Ala-L-Pro-L-Phe + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
succinyl-L-Ala-L-Ala-L-Pro-L-Phe-thiobenzyl ester + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Leu-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Leu-Val-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Lys-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Lys-Val-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Met-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Met-Val-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Phe-Ala-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Phe-epsilon-(2-picolinyl)Lys-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Phe-Gln-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Phe-Glu-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Phe-Leu-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Phe-Met-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Phe-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Phe-Thr-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Phe-Val-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Phe-Val-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Ser-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Thr-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Val-Pro-Leu-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Val-Pro-Met-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Val-Pro-Phe-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Val-Pro-Pro-Phe-SCH2C6H5 + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Val-Pro-Trp-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Val-Pro-Tyr-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
thrombin + H2O
?
show the reaction diagram
-
-
-
-
?
Vitronectin + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
angiotensin I + H2O
angiotensin II + His-Leu
show the reaction diagram
biglycan + H2O
?
show the reaction diagram
P23946
-
-
-
?
heat shock protein 70 + H2O
?
show the reaction diagram
P23946
-
-
-
?
HMGB1 + H2O
?
show the reaction diagram
P23946
-
-
-
?
interleukin-33 + H2O
?
show the reaction diagram
P23946
-
-
-
?
pro-collagen + H2O
collagen + ?
show the reaction diagram
-
-
-
-
?
pro-interleukin-1beta + H2O
interleukin-1beta + ?
show the reaction diagram
-
-
-
-
?
pro-matrix metalloproteinase-1 + H2O
matrix metalloproteinase-1 + ?
show the reaction diagram
-
-
-
-
?
pro-matrix metalloproteinase-3 + H2O
matrix metalloproteinase-3 + ?
show the reaction diagram
-
-
-
-
?
pro-matrix metalloproteinase-9 + H2O
matrix metalloproteinase-9 + ?
show the reaction diagram
-
-
-
-
?
pro-transforming growth factor-beta + H2O
transforming growth factor-beta + ?
show the reaction diagram
-
-
-
-
?
pro-transforming growth factor-beta1 + H2O
transforming growth factor-beta1 + ?
show the reaction diagram
-
-
-
-
?
Vitronectin + H2O
?
show the reaction diagram
-
-
-
-
?
angiotensin I + H2O
angiotensin II + His-Leu
show the reaction diagram
angotensin I + H2O
angiotensin II
show the reaction diagram
-
-
-
-
?
big-endothelin-1 (1-38) + H2O
endothelin-1 (1-31) + ?
show the reaction diagram
-
chymase cleaves the tyrosine31-glycine32 peptide bond of big-endothelin-1 (1-38)
-
-
?
Fibronectin + H2O
?
show the reaction diagram
-
-
-
-
?
plasmin + H2O
?
show the reaction diagram
-
-
-
-
?
promatrix metalloproteinase-2 + H2O
matrix metalloproteinase-2
show the reaction diagram
-
-
-
-
?
promatrix metalloproteinase-9 + H2O
matrix metalloproteinase-9
show the reaction diagram
-
-
-
-
?
thrombin + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
-
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1-[(5-fluoro-1-benzothiophen-3-yl)methyl]-3-{[(methoxycarbonyl)(methyl)amino]methyl}-1H-indole-2-carboxylate
-
-
2-{1-[(1,4-dimethyl-1H-indol-3-yl)methyl]-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl}hexanoic acid
-
-
4-({1-[(4-methyl-1-benzothiophen-3-yl)methyl]-1H-benzimidazol-2-yl}sulfanyl)butanoic acid
-
-
chymostatin
-
-
NK3201
-
-
SF-8257
-
-
-
TY51184
-
-
[1-(5-chloro-1-methyl-1H-indol-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonate
-
-
(6E)-4-[(4-chlorophenyl)sulfonyl]-6-(phenylmethylidene)-1,4-diazepane-2,5-dione
-
-
(6R)-6-(5-chloro-2-methoxybenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
-
(6S)-6-(5-chloro-2-methoxybenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
potent inhibitor
1-(2-Amino-3-methyl-butyryl)-pyrrolidine-2-carboxylic acid (1-benzyl-3,3,3-trifluoro-2-oxo-propyl)-amide
-
-
2-(2-[2-[5-amino-2-(3-amino-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester
-
-
2-(2-[2-[5-amino-2-(3-methoxy-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester
-
i.e. Y40079, novel, potent and orally active chymase inhibitor which would be a useful tool in elucidating the pathophysiological roles of chymase
2-(2-[2-[5-amino-2-(3-nitro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester
-
-
2-(2-{2-[5-amino-2-(3-amino-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester
-
-
2-(2-{2-[5-amino-2-(3-chloro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester
-
-
2-(2-{2-[5-amino-2-(3-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester
-
-
2-(2-{2-[5-amino-2-(3-nitro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester
-
-
2-(2-{2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazol-5-carboxylic acid diethylamide
-
-
2-(2-{2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazol-5-carboxylic acid ethyl ester
-
-
2-(2-{2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazol-5-carboxylic acid ethylamide
-
-
2-(2-{2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazol-6-carboxylic acid methyl ester
-
-
2-(2-{2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido}-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester
-
-
2-(5-Acetylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-(5-Amino-6-oxo-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-(5-Amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-hydroxypropyl)acetamide
-
-
2-(5-Amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-(5-amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(2-phenethyl)acetamide
-
-
2-(5-amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-methylacetamide
-
-
2-(5-Benzenesulfonylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-(5-Benzoylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-(5-Benzyloxycarbonylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[3,4-dioxo-1-phenyl-7-(2-pyridyloxy)]-2-heptyl]acetamide
-
NK3201
2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[3,4-dioxo-1-phenyl-7-(2-pyridyloxy)]-heptyl] acetamide
-
NK3201
2-(5-Hydroxysuccinylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-(5-Mehoxysuccinylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-(5-Methanesulfonylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-(5-Oxaloamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-(benzylamino)-4H-3,1-benzoxazin-4-one
-
-
2-(benzyloxycarbonyl-NH(CH2)2CONH)C6H4SO2F
-
-
2-(benzyloxycarbonyl-NH(CH2)5CONH)C6H4SO2F
-
-
2-(benzyloxycarbonyl-NHCH2CONH)C6H4SO2F
-
-
2-(N-benzyl-N-methylamino)-4H-3,1-benzoxazin-4-one
-
inhibitor forms a stable acyl-enzyme with half-life of 53 min
2-(N-benzyl-N-methylamino)-6-methyl-4H-3,1-benzoxazin-4-one
-
-
2-(N-methyl-N-phenylamino)-4H-3,1-benzoxazin-4-one
-
inhibitor forms a stable acyl-enzyme with half-life of 25 min
2-amino-4-[(1R)-1-([[(6R)-6-(5-chloro-2-methoxybenzyl)-3,7-dioxo-1,4-diazepan-1-yl]carbonyl]amino)propyl]benzoic acid
-
-
2-amino-4-[(1R)-1-([[(6S)-6-(5-chloro-2-methoxybenzyl)-3,7-dioxo-1,4-diazepan-1-yl]carbonyl]amino)propyl]benzoic acid
-
-
2-amino-5-[(1R)-1-([[(6R)-6-(5-chloro-2-methoxybenzyl)-3,7-dioxo-1,4-diazepan-1-yl]carbonyl]amino)propyl]benzoic acid
-
-
2-[2-(4-Fluorophenyl)-5-hydroxysuccinylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-[2-[2-(5-amino-6-oxo-2-m-tolyl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
-
-
2-[2-[2-(5-amino-6-oxo-2-phenyl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
-
-
2-[2-[2-(5-amino-6-oxo-2-pyridin-3-yl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
-
-
2-[2-[2-(5-amino-6-oxo-2-pyridin-4-yl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
-
-
2-[2-[2-[5-amino-2-(3-chloro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
-
-
2-[2-[2-[5-amino-2-(3-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
-
-
2-[2-[2-[5-amino-2-(3-methoxy-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
-
-
2-[2-[2-[5-amino-2-(3-nitro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
-
-
2-[2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazol-5-carboxylic acid diethylamide
-
-
2-[2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazol-5-carboxylic acid ethyl ester
-
-
2-[2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazol-5-carboxylic acid ethylamide
-
-
2-[2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazol-6-carboxylic acid methyl ester
-
-
2-[2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
-
-
2-[4-(5-fluoro-3-methylbenzo[b] thiophen-2-yl)sulfonamido-3-methansulfonylphenyl]oxazole-4-carboxylic acid
-
TY-1184
2-[4-chloro-2-([1-[(4-chlorophenyl)sulfonyl]-3,7-dioxo-1,4-diazepan-6-yl]methyl)phenoxy]-N-methylacetamide
-
-
2-[5-Amino-2-(3-chlorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-[5-Amino-2-(3-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-[5-Amino-2-(4-aminophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-[5-Amino-2-(4-chlorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-(1-benzyl-2-oxazolo[4,5-b]pyridin-2-yl-2-oxo-ethyl)-acetamide
-
-
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-(1-benzyl-2-oxo-2-thiazol-2-yl-ethyl)-acetamide
-
-
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-(2-benzothiazol-2-yl-1-benzyl-2-oxo-ethyl)-acetamide
-
-
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-[1-benzyl-2-(4,5-dihydro-oxazol-2-yl)-2-oxo-ethyl]-acetamide
-
-
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-[1-benzyl-2-(5-fluoro-benzooxazol-2-yl)-2-oxo-ethyl]-acetamide
-
-
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-[1-benzyl-2-(5-methoxy-benzooxazol-2-yl)-2-oxo-ethyl]-acetamide
-
-
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-[1-benzyl-2-oxo-2-(5-phenyl-benzooxazol-2-yl)-ethyl]-acetamide
-
-
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(2-benzoxazolyl)carbonyl]-2-phenylethyl]-acetamide
-
-
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(5-aminobenzoxazol-2-yl)carbonyl]-2-phenylethyl]acetamide
-
-
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(5-carbamoylbenzoxazol-2-yl)carbonyl]-2-phenylethyl]acetamide
-
-
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(5-carboxybenzoxazol-2-yl)carbonyl]-2-phenylethyl]acetamide
-
-
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(5-hydroxybenzoxazol-2-yl)carbonyl]-2-phenylethyl]acetamide
-
-
2-[5-Amino-2-(4-hydroxyphenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-[5-Amino-2-(4-methoxyphenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-[5-Amino-2-(4-nitrophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-[5-Amino-6-oxo-2-(2-thienyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-[5-Amino-6-oxo-2-(3-pyridyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-[5-Amino-6-oxo-2-(4-pyridyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-[5-Amino-6-oxo-2-(m-tolyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-[5-Amino-6-oxo-2-(p-tolyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
2-{2-[2-(5-Amino-6-oxo-2-m-tolyl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl}-benzooxazole-5-carboxylic acid methyl ester
-
-
2-{2-[2-(5-Amino-6-oxo-2-phenyl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl}-benzooxazole-5-carboxylic acid methyl ester
-
-
2-{2-[2-(5-Amino-6-oxo-2-pyridin-3-yl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl}-benzooxazole-5-carboxylic acid methyl ester
-
novel, potent, and orally active inhibitor. Rapidly after oral administration and has satisfactory bioavailability
2-{2-[2-(5-Amino-6-oxo-2-pyridin-4-yl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl}-benzooxazole-5-carboxylic acid methyl ester
-
-
3-([1-[(4-chlorophenyl)sulfonyl]-3,7-dioxo-1,4-diazepan-6-yl]methyl)-4-methoxybenzonitrile
-
-
3-C6H5CONHC6H4SO2F
-
-
3-CF3C6H4SO2F
-
-
3-[(1R)-1-([[(6R)-6-(5-chloro-2-methoxybenzyl)-3,7-dioxo-1,4-diazepan-1-yl]carbonyl]amino)propyl]benzoic acid
-
-
3-[(1R)-1-([[(6S)-6-(5-chloro-2-methoxybenzyl)-3,7-dioxo-1,4-diazepan-1-yl]carbonyl]amino)propyl]benzoic acid
-
-
3-[(3,4-dimethoxyphenyl)sulfonyl]-1-(3,4-dimethylphenyl)imidazoline-2,4-dione
-
C41
3-[(3-amino-4-carboxy)phenylsulfonyl]-7-chloroquinazorine
-
SUNC8257
3-[5-Amino-6-oxo-2-(m-tolyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)propanamide
-
-
3[(3-amino-4-carboxy) phenylsulfonyl]-7-chloroquinazolone-2,4(1H,3H)-dione
-
N-C8257
4-[(1R)-1-([[(6R)-6-(5-chloro-2-methoxybenzyl)-3,7-dioxo-1,4-diazepan-1-yl]carbonyl]amino)propyl]-2-hydroxybenzoic acid
-
-
4-[(1R)-1-([[(6R)-6-(5-chloro-2-methoxybenzyl)-3,7-dioxo-1,4-diazepan-1-yl]carbonyl]amino)propyl]benzoic acid
-
-
4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
-
4-[(4-chlorophenyl)sulfonyl]-6-(2,5-dimethoxybenzyl)-1,4-diazepane-2,5-dione
-
-
4-[(4-chlorophenyl)sulfonyl]-6-(2-ethoxybenzyl)-1,4-diazepane-2,5-dione
-
-
4-[(4-chlorophenyl)sulfonyl]-6-(2-fluorobenzyl)-1,4-diazepane-2,5-dione
-
-
4-[(4-chlorophenyl)sulfonyl]-6-(2-methoxybenzyl)-1,4-diazepane-2,5-dione
-
-
4-[(4-chlorophenyl)sulfonyl]-6-(4,5-dichloro-2-methoxybenzyl)-1,4-diazepane-2,5-dione
-
-
4-[(4-chlorophenyl)sulfonyl]-6-(5-chloro-2-propoxybenzyl)-1,4-diazepane-2,5-dione
-
-
4-[(4-chlorophenyl)sulfonyl]-6-(5-fluoro-2-methoxybenzyl)-1,4-diazepane-2,5-dione
-
-
4-[(4-chlorophenyl)sulfonyl]-6-(5-hydroxy-2-methoxybenzyl)-1,4-diazepane-2,5-dione
-
-
4-[(4-chlorophenyl)sulfonyl]-6-(cyclohexylmethyl)-1,4-diazepane-2,5-dione
-
-
4-[(4-chlorophenyl)sulfonyl]-6-(naphthalen-2-ylmethyl)-1,4-diazepane-2,5-dione
-
-
4-[(4-chlorophenyl)sulfonyl]-6-(pyridin-3-ylmethyl)-1,4-diazepane-2,5-dione
-
-
4-[(4-chlorophenyl)sulfonyl]-6-(pyridin-4-ylmethyl)-1,4-diazepane-2,5-dione
-
-
4-[1-(naphthylmethyl)benzimidazol-2-ylthio]butanoic acid
-
TEI-E548
4-[1-[bis-(4-methyl-phenyl)-methyl]-carbamoyl]-3-(2-ethoxy-benzyl)-4-oxo-azetidine-2-yloxy-benzoic acid
-
BCEAB
4-[1-[[bis-(4-methyl-phenyl)-methyl]-carbamoyl]-3-(2-ethoxy-benzyl)-4-oxo-azetidine-2-yloxy]-benzoic acid
-
-
5-[(1R)-1-([[(6R)-6-(5-chloro-2-methoxybenzyl)-3,7-dioxo-1,4-diazepan-1-yl]carbonyl]amino)propyl]-2-hydroxybenzoic acid
-
-
6-(2-butoxy-5-chlorobenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
-
6-(2-chlorobenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
-
6-(3-chloro-5-fluoro-2-methoxybenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
-
6-(3-chlorobenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
-
6-(4-chlorobenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
-
6-(5-chloro-2-ethoxybenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
-
6-(5-chloro-2-methoxybenzyl)-3,7-dioxo-N-(1-phenylbutyl)-1,4-diazepane-1-carboxamide
-
-
6-(5-chloro-2-methoxybenzyl)-3,7-dioxo-N-(1-phenylethyl)-1,4-diazepane-1-carboxamide
-
-
6-(5-chloro-2-methoxybenzyl)-3,7-dioxo-N-(1-phenylpropyl)-1,4-diazepane-1-carboxamide
-
-
6-(5-chloro-2-methoxybenzyl)-3,7-dioxo-N-(2-phenylethyl)-1,4-diazepane-1-carboxamide
-
-
6-(5-chloro-2-methoxybenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
-
6-(5-chloro-2-methoxybenzyl)-N-(2-methyl-1-phenylpropyl)-3,7-dioxo-1,4-diazepane-1-carboxamide
-
-
6-(5-chloro-2-methoxybenzyl)-N-(diphenylmethyl)-3,7-dioxo-1,4-diazepane-1-carboxamide
-
-
6-benzyl-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
-
6-methyl-2-(N-methyl-N-phenylamino)-4H-3,1-benzoxazin-4-one
-
-
acetyl-Ala-Gly-Phe-CH2Cl
-
-
alpha1-Aantichymotrypsin
-
-
-
Alpha1-proteinase inhibitor
-
-
-
antichymotrypsin
-
-
-
antitrypsin
-
-
-
Aprotinin
-
-
benzyloxycarbonyl-Ile-Glu-Pro-Phe-COOCH3
-
-
benzyloxycarbonyl-Leu-Phe-chloromethyl ketone
-
-
C6H5CH2SO3F
-
-
chymostatin
dipyridyl
-
IC50: above 0.4 mM
Eglin c
-
potent inhibitor
JNJ-10311795
-
-
L-Valyl-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)-L-prolinamide hydrochloride
-
-
lisinopril
-
IC50: above 0.4 mM
methyl 3-[(1R)-1-([[(6R)-6-(5-chloro-2-methoxybenzyl)-3,7-dioxo-1,4-diazepan-1-yl]carbonyl]amino)propyl]benzoate
-
-
methyl[1-naphthalen-2-yl-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphinic acid
-
-
N-(1-Benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
N-benzyl-6-(5-chloro-2-methoxybenzyl)-3,7-dioxo-1,4-diazepane-1-carboxamide
-
-
N-benzyl-6-(5-chloro-2-methoxybenzyl)-N-methyl-3,7-dioxo-1,4-diazepane-1-carboxamide
-
-
N-substituted saccharin derivatives
-
-
-
N-tosyl-L-phenylalanyl-chloromethyl ketone
-
-
NK3201
phenylmethylsulfonyl fluoride
-
-
platelet factor 4
-
i.e. PF-4, competitive inhibition of enzyme and cathepsin G
-
RO5066852
-
-
RWJ-355871
-
-
SD906
-
-
secretory leucocyte protease inhibitor
-
-
-
secretory leukocyte protease inhibitor
-
-
-
SF2809-I
-
the inhibitor is isolated from the fermentation broth of Dactylosporangium sp., specific chymase inhibitor with little or no inhibitory activity against chymotrypsin or cathepsin G, IC50: 0.0073 mM
SF2809-II
-
the inhibitor is isolated from the fermentation broth of Dactylosporangium sp., specific chymase inhibitor with little or no inhibitory activity against chymotrypsin or cathepsin G, IC50: 0.000041 mM
SF2809-III
-
the inhibitor is isolated from the fermentation broth of Dactylosporangium sp., specific chymase inhibitor with little or no inhibitory activity against chymotrypsin or cathepsin G, IC50: 0.0021 mM
SF2809-IV
-
the inhibitor is isolated from the fermentation broth of Dactylosporangium sp., specific chymase inhibitor with little or no inhibitory activity against chymotrypsin or cathepsin G, IC50: 0.000081
SF2809-V
-
the inhibitor is isolated from the fermentation broth of Dactylosporangium sp., specific chymase inhibitor with little or no inhibitory activity against chymotrypsin or cathepsin G, IC50: 0.000043 mM
SF2809-VI
-
the inhibitor is isolated from the fermentation broth of Dactylosporangium sp., specific chymase inhibitor with little or no inhibitory activity against chymotrypsin or cathepsin G, IC50: 0.000014 mM
soybean tryosin inhibitor
-
-
Soybean trypsin inhibitor
-
substituted 3-phenylsulfonylquinazoline-2,4-dione derivatives
-
-
-
Suc-Val-Pro-PheP-(OPh)2
-
noncompetitive inhibitor
succinyl-Pro-Leu-Phe-CH2Cl
-
-
succinyl-Val-Pro-PheP(OPh)2
-
-
succinyl-Val-Pro-PheP-(OPh)2
-
highly specific and metabolically stable chymase inhibitor with a biological half-life of more than 20 h
SUN C8257
-
-
SUN-C8007
-
i.e. 3-(3-aminophenylsulfonyl)-7-chloroquinazorine-2,4(1H,3H)-dione
SUN-C8257
-
i.e. 3-[(3-amino-4-carboxy)phenylsulfonyl]-7-chloroquinazorine 2,4(1H,3H)-dione
SUN13350
-
-
-
SUNC8257
-
-
suramin
-
i.e. 8,8'-[carbonylbis[imino-3,1-phenylenecarbonylimino(4-methyl-3,1-phenylene)carbonylimino]]bis-1,3,5-naphthalenetrisulfonic acid
t-butyloxycarbonyl-Gly-Leu-Phe
-
-
TY-51184
-
highly-specific and orally active chymase inhibitor; i.e. 2-[4-(5-fluoro-3-methylbenzo[b]thiophen-2-yl)sulfonamide-3-methanesulfonylphenyl]oxazole-4-carboxylic acid
TY-51469
-
i.e. 2-[4-(5-fluoro-3-methylbenzo[b]thiophen-2-yl)sulfonamido-3-methanesulfonylphenyl]thiazole-4-carboxylic acid; inhibitor with very high affinity (IC50 0.1 nmol/kg) against chymase
TY51184
-
-
Y-40018
-
i.e. 4-[5-amino-2-(3-chlorophenyl)-6-oxo-1,6-dihydropyrimidin-1-ylacetamido]-N-benzyl-2,2-difluoro-3-oxo-5-phenylpentanamide
Y-40079
-
i.e. 2-[2-[2-[5-amino-2-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-1-yl]acetamido]-3-phenylpropionyl]benzoxazole-5-carboxylic acid methyl ester
Z-Ile-Glu-Pro-Phe-CO2Me
-
-
[1-(1-benzofuran-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
-
-
[1-(1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
-
-
[1-(1-methyl-1H-indol-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
-
-
[1-(1H-indol-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
-
-
[1-(2,3-dihydro-1H-benzotriazol-1-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
-
less than 50% inhibition at 0.01 mM
[1-(5-chloro-1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl](2-phenylethyl)phosphinic acid
-
-
[1-(5-chloro-1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]ethylphosphinic acid
-
-
[1-(5-chloro-1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]methylphosphinic acid
-
-
[1-(5-chloro-1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phenylphosphinic acid
-
-
[1-(5-chloro-1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
-
-
[1-(5-chloro-1-benzothiophen-3-yl)-2-oxo-2-[[(E)-2-phenylethenyl]amino]ethyl]methylphosphinic acid
-
-
[1-(5-chloro-1-benzothiophen-3-yl)-2-oxo-2-[[(E)-2-phenylethenyl]amino]ethyl]phosphonic acid
-
-
[1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(3,4-difluorophenyl)ethenyl]amino]-2-oxoethyl]ethylphosphinic acid
-
-
[1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(3,4-difluorophenyl)ethenyl]amino]-2-oxoethyl]methylphosphinic acid
-
-
[1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(3,4-difluorophenyl)ethenyl]amino]-2-oxoethyl]phosphonic acid
-
-
[1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(3-chloro-5-fluorophenyl)ethenyl]amino]-2-oxoethyl]methylphosphinic acid
-
-
[1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(3-chlorophenyl)ethenyl]amino]-2-oxoethyl]methylphosphinic acid
-
-
[1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(4-fluorophenyl)ethenyl]amino]-2-oxoethyl]phosphonic acid
-
-
[1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(4-methoxyphenyl)ethenyl]amino]-2-oxoethyl]phosphonic acid
-
-
[1-(5-chloro-1-benzothiophen-3-yl)-2-[[2-(3,4-difluorophenyl)ethyl]amino]-2-oxoethyl]methylphosphinic acid
-
-
[1-(5-chloro-1-methyl-1H-indol-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]methylphosphinic acid
-
-
[1-(5-chloro-1-methyl-1H-indol-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
-
-
[1-(5-chloro-1-methyl-1H-indol-3-yl)-2-[[(E)-2-(3,4-difluorophenyl)ethenyl]amino]-2-oxoethyl]methylphosphinic acid
-
-
[1-(5-chloro-1-methyl-1H-indol-3-yl)-2-[[(E)-2-(4-fluorophenyl)ethenyl]amino]-2-oxoethyl]phosphonic acid
-
-
[1-naphthalen-1-yl-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
-
-
[1-[(1-Benzyl-2-hydroxy-2-oxazolo[5,4-b]pyridin-2-yl-ethylcarbamoyl)-methyl]-2-(4-fluoro-phenyl)-6-oxo-1,6-dihydro-pyrimidin-5-yl]-carbamic acid benzyl ester
-
-
[2-(3-[methyl[1-(naphthalen-2-ylcarbonyl)piperidin-4-yl]carbamoyl]naphthalen-2-yl)-1-naphthalen-1-yl-2-oxoethyl]phosphonic acid
-
-
[4-chloro-2-([1-[(4-chlorophenyl)sulfonyl]-3,7-dioxo-1,4-diazepan-6-yl]methyl)phenoxy]acetic acid
-
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2.96
(25R)-3beta-hydroxycholest-5-en-27-oate
-
pH 7.5, 22°C
1.02
Ala-Ala-Pro-Leu-4-nitroanilide
-
wild type enzyme
3
Ala-Ala-Pro-Met-4-nitroanilide
-
wild type enzyme
0.47
Ala-Ala-Pro-Phe-4-nitroanilide
-
wild type enzyme
0.0223 - 0.398
angiotensin I
0.0141
big endothelin
-
deglycosylated enzyme
-
0.0145
Big endothelin-1
-
glycosylated enzyme
0.31
DRVWIHOLHL
-
-
-
0.06
DRVWIHPFHL
-
-
0.11
DRVWIHPWHL
-
-
3
succinyl-Ala-Ala-Pro-Leu-4-nitroanilide
-
-
2.6
succinyl-Ala-Ala-Pro-Met-4-nitroanilide
-
-
0.8
succinyl-Ala-Ala-Pro-Phe-4-nitroanilide
-
-
0.67
succinyl-Ala-Pro-Phe-4-nitroanilide
-
-
1
succinyl-epsilon-(2-picolinyl)Lys-Val-Pro-Phe-4-nitroanilide
-
-
0.88
succinyl-Gln-Pro-Phe-4-nitroanilide
-
-
0.32
succinyl-Glu-Pro-Phe-4-nitroanilide
-
-
0.36
succinyl-Glu-Val-Pro-Phe-4-nitroanilide
-
-
0.514 - 0.935
succinyl-L-Ala-L-Ala-L-Pro-L-Phe-4-nitroanilide
0.0157 - 0.0355
succinyl-L-Ala-L-Ala-L-Pro-L-Phe-thiobenzyl ester
0.82
succinyl-Leu-Pro-Phe-4-nitroanilide
-
-
0.13
succinyl-Leu-Val-Pro-Phe-4-nitroanilide
-
-
0.65
succinyl-Lys-Pro-Phe-4-nitroanilide
-
-
0.078
succinyl-Lys-Val-Pro-Phe-4-nitroanilide
-
-
0.44
succinyl-Met-Pro-Phe-4-nitroanilide
-
-
0.055
succinyl-Met-Val-Pro-Phe-4-nitroanilide
-
-
0.24 - 0.7
succinyl-Phe-Ala-Phe-4-nitroanilide
0.21
succinyl-Phe-Gln-Phe-4-nitroanilide
-
-
1.4
succinyl-Phe-Glu-Phe-4-nitroanilide
-
-
0.091
succinyl-Phe-Leu-Phe-4-nitroanilide
-
-
0.29
succinyl-Phe-Met-Phe-4-nitroanilide
-
-
0.29
succinyl-Phe-Pro-Phe-4-nitroanilide
-
-
0.49
succinyl-Phe-Ser-Phe-4-nitroanilide
-
-
0.44
succinyl-Phe-Thr-Phe-4-nitroanilide
-
-
0.071
succinyl-Phe-Val-Phe-4-nitroanilide
-
-
0.056
succinyl-Phe-Val-Pro-Phe-4-nitroanilide
-
-
0.51
succinyl-Ser-Pro-Phe-4-nitroanilide
-
-
0.25
succinyl-Thr-Pro-Phe-4-nitroanilide
-
-
0.88 - 0.9
succinyl-Val-Pro-Leu-4-nitroanilide
1.2
succinyl-Val-Pro-Met-4-nitroanilide
-
-
0.093 - 0.1
succinyl-Val-Pro-Phe-4-nitroanilide
0.048
succinyl-Val-Pro-Pro-Phe-SCH2C6H5
-
-
0.17
succinyl-Val-Pro-Tyr-4-nitroanilide
-
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
17.5
(25R)-3beta-hydroxycholest-5-en-27-oate
-
pH 7.5, 22°C
19.3
Ala-Ala-Pro-Leu-4-nitroanilide
-
wild type enzyme
23
Ala-Ala-Pro-Met-4-nitroanilide
-
wild type enzyme
143
Ala-Ala-Pro-Phe-4-nitroanilide
-
wild type enzyme
65 - 143
angiotensin I
24.7 - 25.6
Big endothelin-1
46
DRVWIHOLHL
-
-
-
160
DRVWIHPFHL
-
-
210
DRVWIHPWHL
-
-
6.7
succinyl-Ala-Ala-Pro-Leu-4-nitroanilide
-
-
2.5
succinyl-Ala-Ala-Pro-Met-4-nitroanilide
-
-
65
succinyl-Ala-Ala-Pro-Phe-4-nitroanilide
-
-
51
succinyl-Ala-Pro-Phe-4-nitroanilide
-
-
480
succinyl-epsilon-(2-picolinyl)Lys-Val-Pro-Phe-4-nitroanilide
-
-
56 - 86
succinyl-Gln-Pro-Phe-4-nitroanilide
61
succinyl-Glu-Pro-Phe-4-nitroanilide
-
-
68
succinyl-Glu-Val-Pro-Phe-4-nitroanilide
-
-
2.5 - 3.6
succinyl-L-Ala-L-Ala-L-Pro-L-Phe-4-nitroanilide
12.6 - 17.8
succinyl-L-Ala-L-Ala-L-Pro-L-Phe-thiobenzyl ester
77
succinyl-Leu-Pro-Phe-4-nitroanilide
-
-
79
succinyl-Leu-Val-Pro-Phe-4-nitroanilide
-
-
14
succinyl-Lys-Pro-Phe-4-nitroanilide
-
-
58
succinyl-Lys-Val-Pro-Phe-4-nitroanilide
-
-
100
succinyl-Met-Pro-Phe-4-nitroanilide
-
-
53
succinyl-Met-Val-Pro-Phe-4-nitroanilide
-
-
10
succinyl-Phe-Ala-Phe-4-nitroanilide
-
-
3.9
succinyl-Phe-Gln-Phe-4-nitroanilide
-
-
8.4
succinyl-Phe-Glu-Phe-4-nitroanilide
-
-
7.5
succinyl-Phe-Leu-Phe-4-nitroanilide
-
-
5.9
succinyl-Phe-Met-Phe-4-nitroanilide
-
-
6.2
succinyl-Phe-Ser-Phe-4-nitroanilide
-
-
10
succinyl-Phe-Thr-Phe-4-nitroanilide
-
-
4
succinyl-Phe-Val-Phe-4-nitroanilide
-
-
56
succinyl-Phe-Val-Pro-Phe-4-nitroanilide
-
-
38
succinyl-Ser-Pro-Phe-4-nitroanilide
-
-
120
succinyl-Thr-Pro-Phe-4-nitroanilide
-
-
21
succinyl-Val-Pro-Leu-4-nitroanilide
-
-
1.2 - 8.7
succinyl-Val-Pro-Met-4-nitroanilide
75
succinyl-Val-Pro-Phe-4-nitroanilide
-
-
400
succinyl-Val-Pro-Pro-Phe-SCH2C6H5
-
-
19
succinyl-Val-Pro-Tyr-4-nitroanilide
-
-
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1963
Abz-GIAPFCDLMPEQ-EDDnp
-
pH 7.4, 37°C
1035
Abz-GIATFCDLMPEQ-EDDnp
-
pH 7.4, 37°C
238
Abz-GIATFCMLMPEQ-EDDnp
-
pH 7.4, 37°C
287
Abz-GIATFCPLMPEQ-EDDnp
-
pH 7.4, 37°C
144
Abz-GIATFCRLMPEQ-EDDnp
-
pH 7.4, 37°C
221
Abz-GIATFDMLMPEQ-EDDnp
-
pH 7.4, 37°C
203
Abz-GIATFRMLMPEQ-EDDnp
-
pH 7.4, 37°C
209
Abz-GIATFSMLMPEQ-EDDnp
-
pH 7.4, 37°C
96
Abz-GIATFWMLMPEQ-EDDnp
-
pH 7.4, 37°C
1648
Abz-GIEPFSDPMPEQ-EDDnp
-
pH 7.4, 37°C
136
Abz-TPFSALQ-EDDnp
-
pH 7.4, 37°C
97
Abz-TPWSALQ-YNO2
-
pH 7.4, 37°C
3.85 - 4.86
succinyl-L-Ala-L-Ala-L-Pro-L-Phe-4-nitroanilide
355 - 1130
succinyl-L-Ala-L-Ala-L-Pro-L-Phe-thiobenzyl ester
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000005 - 0.0000821
1-(2-Amino-3-methyl-butyryl)-pyrrolidine-2-carboxylic acid (1-benzyl-3,3,3-trifluoro-2-oxo-propyl)-amide
0.0000261
2-(2-[2-[5-amino-2-(3-chloro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester
-
-
0.0000143
2-(2-[2-[5-amino-2-(3-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester
-
-
0.0000418
2-(2-[2-[5-amino-2-(3-nitro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester
-
-
0.0000595
2-(2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl)-benzooxazol-5-carboxylic acid diethylamide
-
-
0.00003
2-(2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl)-benzooxazol-5-carboxylic acid ethyl ester
-
-
0.0000686
2-(2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl)-benzooxazol-5-carboxylic acid ethylamide
-
-
0.0000563
2-(2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl)-benzooxazol-6-carboxylic acid methyl ester
-
-
0.0000226 - 0.000026
2-(2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl)-benzooxazole-5-carboxylic acid methyl ester
0.000105
2-(5-Acetylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.06
2-(5-Amino-6-oxo-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.03
2-(5-Amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-hydroxypropyl)acetamide
-
-
0.000389
2-(5-Amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.11
2-(5-amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(2-phenethyl)acetamide
-
-
0.08
2-(5-amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-methylacetamide
-
-
0.000369
2-(5-Benzenesulfonylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.000306
2-(5-Benzoylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.000146
2-(5-Benzyloxycarbonylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.0000656
2-(5-Hydroxysuccinylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.000229
2-(5-Mehoxysuccinylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.00103
2-(5-Methanesulfonylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.00447
2-(5-Oxaloamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl)-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.000005
2-(benzylamino)-4H-3,1-benzoxazin-4-one
-
pH 8.0, 25°C
0.000011
2-(N-benzyl-N-methylamino)-4H-3,1-benzoxazin-4-one
-
pH 8.0, 25°C
0.000017
2-(N-benzyl-N-methylamino)-6-methyl-4H-3,1-benzoxazin-4-one
-
pH 8.0, 25°C
0.000014
2-(N-methyl-N-phenylamino)-4H-3,1-benzoxazin-4-one
-
pH 8.0, 25°C
0.000237
2-[2-(4-Fluorophenyl)-5-hydroxysuccinylamino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.0000289 - 0.0000442
2-[2-[2-(5-amino-6-oxo-2-m-tolyl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
0.00000356 - 0.00000557
2-[2-[2-(5-amino-6-oxo-2-phenyl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
0.00000262 - 0.0000774
2-[2-[2-(5-amino-6-oxo-2-pyridin-3-yl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
0.0000138 - 0.0000435
2-[2-[2-(5-amino-6-oxo-2-pyridin-4-yl-6H-pyrimidin-1-yl)-acetylamino]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
0.0000056 - 0.0004
2-[2-[2-[5-amino-2-(3-amino-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
0.0000169
2-[2-[2-[5-amino-2-(3-chloro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
-
pH 7.5, 37°C
0.0000185
2-[2-[2-[5-amino-2-(3-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
-
pH 7.5, 37°C
0.0000325 - 0.0000485
2-[2-[2-[5-amino-2-(3-methoxy-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
0.0000157
2-[2-[2-[5-amino-2-(3-nitro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
-
pH 7.5, 37°C
0.00000932
2-[2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazol-5-carboxylic acid diethylamide
-
pH 7.5, 37°C
0.0000102
2-[2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazol-5-carboxylic acid ethyl ester
-
pH 7.5, 37°C
0.00000771
2-[2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazol-5-carboxylic acid ethylamide
-
pH 7.5, 37°C
0.0000102
2-[2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazol-6-carboxylic acid methyl ester
-
pH 7.5, 37°C
0.0000166
2-[2-[2-[5-amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-acetylamido]-3-phenyl-propionyl]-benzooxazole-5-carboxylic acid methyl ester
-
pH 7.5, 37°C
0.000124
2-[5-Amino-2-(3-chlorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.000141
2-[5-Amino-2-(3-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.00012
2-[5-Amino-2-(4-aminophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.000471
2-[5-Amino-2-(4-chlorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.0000606
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-(1-benzyl-2-oxazolo[4,5-b]pyridin-2-yl-2-oxo-ethyl)-acetamide
-
-
0.00385
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-(1-benzyl-2-oxo-2-thiazol-2-yl-ethyl)-acetamide
-
-
0.000182
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-(2-benzothiazol-2-yl-1-benzyl-2-oxo-ethyl)-acetamide
-
-
0.00589
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-[1-benzyl-2-(4,5-dihydro-oxazol-2-yl)-2-oxo-ethyl]-acetamide
-
-
0.0000907 - 0.0000931
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-[1-benzyl-2-(5-fluoro-benzooxazol-2-yl)-2-oxo-ethyl]-acetamide
0.0000733 - 0.000489
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-[1-benzyl-2-(5-methoxy-benzooxazol-2-yl)-2-oxo-ethyl]-acetamide
0.0000097 - 0.000174
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-[1-benzyl-2-oxo-2-(5-phenyl-benzooxazol-2-yl)-ethyl]-acetamide
0.000305
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.0000133 - 0.000125
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(2-benzoxazolyl)carbonyl]-2-phenylethyl]-acetamide
0.000489
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(5-aminobenzoxazol-2-yl)carbonyl]-2-phenylethyl]acetamide
-
pH 7.5, 37°C
0.000012 - 0.000094
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(5-carbamoylbenzoxazol-2-yl)carbonyl]-2-phenylethyl]acetamide
0.0000169 - 0.00076
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(5-carboxybenzoxazol-2-yl)carbonyl]-2-phenylethyl]acetamide
0.0000097 - 0.00212
2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1-[(5-hydroxybenzoxazol-2-yl)carbonyl]-2-phenylethyl]acetamide
0.000479
2-[5-Amino-2-(4-hydroxyphenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.000487
2-[5-Amino-2-(4-methoxyphenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.000547
2-[5-Amino-2-(4-nitrophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.000377
2-[5-Amino-6-oxo-2-(2-thienyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.000658
2-[5-Amino-6-oxo-2-(3-pyridyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.00122
2-[5-Amino-6-oxo-2-(4-pyridyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.0000506
2-[5-Amino-6-oxo-2-(m-tolyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.000186
2-[5-Amino-6-oxo-2-(p-tolyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.03
3-[5-Amino-6-oxo-2-(m-tolyl)-1,6-dihydro-1-pyrimidinyl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)propanamide
-
-
0.000029
6-methyl-2-(N-methyl-N-phenylamino)-4H-3,1-benzoxazin-4-one
-
pH 8.0, 25°C
0.0000131
chymostatin
0.00008
L-Valyl-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)-L-prolinamide hydrochloride
-
-
0.02
N-(1-Benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
-
-
0.0000506
[1-[(1-Benzyl-2-hydroxy-2-oxazolo[5,4-b]pyridin-2-yl-ethylcarbamoyl)-methyl]-2-(4-fluoro-phenyl)-6-oxo-1,6-dihydro-pyrimidin-5-yl]-carbamic acid benzyl ester
-
pH 7.5, 37°C