Information on EC 3.4.21.22 - coagulation factor IXa

Word Map on EC 3.4.21.22
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Specify your search results
Select one or more organisms in this record:
Show additional data
Do not include text mining results
Include (text mining) results (more...)
Include results (AMENDA + additional results, but less precise; more...)

The enzyme appears in viruses and cellular organisms

EC NUMBER
COMMENTARY hide
3.4.21.22
-
RECOMMENDED NAME
GeneOntology No.
coagulation factor IXa
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
Selective cleavage of Arg-/-Ile bond in factor X to form factor Xa
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis
-
-
hydrolysis of peptide bond
-
-
endopeptidase
-
additional information
-
amidolytic activity
CAS REGISTRY NUMBER
COMMENTARY hide
37316-87-3
-
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
-
factor IXa deficiency results in hemophilia
physiological function
-
factor IXa is a critical enzyme for the formation of stable blood clots
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
4-methylsulfonyl-D-Leu-Gly-Arg-p-nitroanilide + H2O
4-methylsulfonyl-D-Leu-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
-
?
acetyl-L-Ala-Gly-Arg-Ser-Leu-amide + H2O
?
show the reaction diagram
-
-
-
-
?
CBS 31.39 + H2O
?
show the reaction diagram
-
i.e. CH3SO2-D-Leu-Gly-L-Arg-4-nitroanilide
-
-
?
CBS 48.03 + H2O
?
show the reaction diagram
-
i.e. CH3OCO-D-Leu-Gly-L-Arg-4-nitroanilide
-
-
?
CH3SO2-D-Leu-Gly-Arg-4-nitroanilide + H2O
?
show the reaction diagram
CH3SO2-D-Leu-Gly-L-Arg-p-nitroanilide + H2O
CH3SO2-D-Leu-Gly-L-Arg + p-nitroaniline
show the reaction diagram
D-cyclohexylglycyl-Gly-Arg-7-amido-4-methylcoumarin + H2O
D-cyclohexylglycyl-Gly-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
D-cyclohexylglycyl-Gly-Arg-p-nitroanilide + H2O
D-cyclohexylglycyl-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
D-Leu-Phe-Gly-Arg-4-nitroanilide + H2O
D-Leu-Phe-Gly-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
D-Leu-Phg-Arg-4-nitroanilide + H2O
D-Leu-Phg-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
factor X
?
show the reaction diagram
-
activation of factor X to factor Xa
-
-
?
factor X + H2O
?
show the reaction diagram
factor X + H2O
activated factor X + ?
show the reaction diagram
factor X + H2O
factor Xa
show the reaction diagram
Factor X + H2O
Factor Xa + ?
show the reaction diagram
factor X + H2O
fragments of factor X
show the reaction diagram
-
-
-
?
L-Leu-Gly-L-Arg-4-nitroanilide + H2O
L-Leu-Gly-L-Arg + 4-nitroaniline
show the reaction diagram
methoxycarbonyl-D-cyclohexylglycyl-glycyl-L-arginyl-p-nitroanilide + H2O
methoxycarbonyl-D-cyclohexylglycyl-glycyl-L-arginine + p-nitroaniline
show the reaction diagram
-
-
-
-
?
methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
rFIXa, ethanol, 25% v/v enhances the activity 6fold, methanol 4fold, ethylene glycol, 25-40% v/v enhances the activity up to 20fold, glycerol, 50% v/v enhances the activity 6fold
-
-
?
methylsulfonyl-D-cyclohexylglycyl-Arg-7-amido-4-methylcoumarin + H2O
methylsulfonyl-D-cyclohexylglycyl-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
assay at 37C
-
-
?
methylsulfonyl-D-cyclohexylglycyl-Gly-Arg-p-nitroanilide + H2O
methylsulfonyl-D-cyclohexylglycyl-Gly-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
methylsulfonyl-D-hexahydrotyrosyl-Gly-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
N-alpha-benzyloxycarbonyl-D-arginylglycyl-L-arginine-para-nitroanilide + H2O
N-alpha-benzyloxycarbonyl-D-arginylglycyl-L-arginine + para-nitroaniline
show the reaction diagram
-
-
-
-
?
Nalpha-benzyloxycarbonyl-D-Arg-Gly-Arg-4-nitroanilide + H2O
Nalpha-benzyloxycarbonyl-D-Arg-Gly-Arg + 4-nitroaniline
show the reaction diagram
-
S-2765
-
-
?
p-aminobenzamidine + H2O
p-aminobenzoic acid + NH3
show the reaction diagram
-
-
-
-
?
Pefa-5523 + H2O
?
show the reaction diagram
-
-
-
-
?
Pefachrome IXa + H2O
?
show the reaction diagram
S-2366 + H2O
?
show the reaction diagram
-
-
-
-
?
Spectrozyme FIXa + H2O
?
show the reaction diagram
-
i.e. D-Leu-phenylated Gly-L-Arg-4-nitroanilide
-
-
?
Spectrozyme FXIIa
?
show the reaction diagram
-
i.e. D-cyclohexyl-Thr-Gly-L-Arg-4-nitroanilide
-
-
?
Spectrozyme t-PA + H2O
?
show the reaction diagram
-
i.e. CH3SO2-D-cyclohexyl-Thr-Gly-L-Arg-4-nitroanilide
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
D-Leu-Phg-Arg-4-nitroanilide + H2O
D-Leu-Phg-Arg + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
factor X
?
show the reaction diagram
-
activation of factor X to factor Xa
-
-
?
factor X + H2O
?
show the reaction diagram
factor X + H2O
activated factor X + ?
show the reaction diagram
factor X + H2O
factor Xa
show the reaction diagram
Factor X + H2O
Factor Xa + ?
show the reaction diagram
factor X + H2O
fragments of factor X
show the reaction diagram
-
-
-
?
methylsulfonyl-D-cyclohexylglycyl-Arg-7-amido-4-methylcoumarin + H2O
methylsulfonyl-D-cyclohexylglycyl-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
assay at 37C
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
Factor VIIIa
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
lithium ion
-
activates slightly
additional information
-
factor IXa is not a Na+-binding protease
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2-carbamimidoylbenzo[b]thiophen-4-yloxy)phenylacetic acid methyl ester
-
-
(2-carbamimidoylbenzo[b]thiophen-6-yloxy)thiophen-2-ylacetic acid ethyl ester
-
-
(2R)-N-1,3-benzothiazol-5-yl-2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanamide
-
-
(2R)-N-[4-(1H-benzimidazol-1-yl)-2-fluorophenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenylpropanamide
-
-
(2S)-N-1,3-benzothiazol-5-yl-2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanamide
-
-
(2S)-N-[4-(1H-benzimidazol-1-yl)-2-fluorophenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenylpropanamide
-
-
2-(2-carbamimidoylbenzo[b]thiophen-4-yloxy)propionic acid methyl ester
-
-
2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenyl-N-(4-[3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl)propanamide
-
-
2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenyl-N-[4-(4-phenyl-1H-imidazol-1-yl)phenyl]propanamide
-
-
2-(5-carbamimidoyl-1-benzothiophen-3-yl)-N-(4-cyanophenyl)-3-phenylpropanamide
-
-
2-(5-carbamimidoyl-1-benzothiophen-3-yl)-N-(4-methylphenyl)-3-phenylpropanamide
-
-
2-(5-carbamimidoyl-1-benzothiophen-3-yl)-N-(4-phenoxyphenyl)-3-phenylpropanamide
-
-
2-(5-carbamimidoyl-1-benzothiophen-3-yl)-N-(4-[(6-chloropyridazin-3-yl)sulfamoyl]phenyl)-3-phenylpropanamide
-
-
2-(5-carbamimidoyl-1-benzothiophen-3-yl)-N-(5-fluoro-2-methylphenyl)-3-phenylpropanamide
-
-
2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenyl-N-(2'-sulfamoylbiphenyl-4-yl)propanamide
-
-
2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenyl-N-[4-(5-phenyl-1H-imidazol-4-yl)phenyl]propanamide
-
-
2-(5-carbamimidoyl-1H-indol-3-yl)-N-(2'-sulfamoylbiphenyl-4-yl)acetamide
-
-
2-(5-carbamimidoyl-1H-indol-3-yl)-N-(4-ethylphenyl)-3-phenylpropanamide - 1H-benzimidazole
-
(1:1)
2-(7-carbamimidoylnaphthalen-1-yl)-N-[2-(1-ethoxyethenyl)cyclohexyl]-3-phenylpropanamide
-
-
2-([2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]amino)-N-ethylcyclohexanecarboxamide
-
-
2-([2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]amino)cyclohexanecarboxylic acid
-
-
2-amidino-4-iodobenzothiophene
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenyl-N-[4-(pyrrolidin-1-ylcarbonyl)phenyl]acetamide
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (1,3-dimethyl-1H-pyrazol-5-yl)carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (2,4-difluorophenyl)carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (2,6-difluorophenyl)carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (2-fluorophenyl)carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (2-methylphenyl)carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (2-[[(2-methylpropyl)amino]methyl]phenyl)carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (3,5-dimethyl-1,2-oxazol-4-yl)carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (3,5-dimethyl-1H-pyrazol-4-yl)carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (3-fluorophenyl)carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (4-fluorophenyl)carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (4-methoxyphenyl)carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl phenylcarbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [1,3-dimethyl-5-[(propan-2-ylamino)methyl]-1H-pyrazol-4-yl]carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [1-methyl-3-[(methylamino)methyl]-1H-pyrazol-5-yl]carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [2-(aminomethyl)phenyl]carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [2-(piperazin-1-ylmethyl)phenyl]carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [2-[(dimethylamino)methyl]phenyl]carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [2-[(methylamino)methyl]phenyl]carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [3-(methoxymethyl)-1-methyl-1H-pyrazol-5-yl]carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [4-[(4-methylpiperazin-1-yl)methyl]phenyl]carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [4-[2-(dimethylamino)ethoxy]phenyl]carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [5-[(ethylamino)methyl]-1,3-dimethyl-1H-pyrazol-4-yl]carbamate
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-N,2-diphenylacetamide
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-N-(2-methoxyphenyl)-2-phenylacetamide
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-N-(3-methoxyphenyl)-2-phenylacetamide
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-N-(4-methoxyphenyl)-2-phenylacetamide
-
-
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-N-[2-(dimethylamino)ethyl]-2-phenylacetamide
-
-
2-[(2-carbamimidoyl-1-benzothiophen-6-yl)oxy]-2-(4-fluorophenyl)acetamide
-
-
2-[(2-carbamimidoyl-6-fluoro-1-benzothiophen-4-yl)oxy]-2-phenylethyl phenylcarbamate
-
-
2-[(2-carbamimidoyl-6-fluoro-1-benzothiophen-4-yl)oxy]-2-phenylethyl [2-(aminomethyl)phenyl]carbamate
-
-
2-[(2-carbamimidoyl-6-fluoro-1-benzothiophen-4-yl)oxy]-2-phenylethyl [2-[(dimethylamino)methyl]phenyl]carbamate
-
-
3-(1-[4-(1H-benzimidazol-1-yl)phenyl]-2-oxopyrrolidin-3-yl)-1-benzothiophene-5-carboximidamide
-
-
3-(2-carbamimidoylbenzo[b]thiophen-6-yloxy)-3-(4-chlorophenyl)propionic acid methyl ester
-
-
3-(2-[4-(1H-benzimidazol-1-yl)phenyl]-1-benzyl-2-oxoethyl)-1-benzothiophene-5-carboximidamide
-
-
3-(4-aminophenyl)-N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1-benzothiophen-3-yl)propanamide
-
-
3-(4-aminophenyl)-N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)propanamide
-
-
3-[3-([4-(1H-benzimidazol-1-yl)phenyl]amino)-2-(5-carbamimidoyl-1H-indol-3-yl)-3-oxopropyl]benzoic acid
-
-
4-(([2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenylpropanoyl]amino)methyl)-N-[5-(methylsulfonyl)-1H-benzimidazol-2-yl]benzamide
-
-
4-(2-carbamimidoylbenzo[b]thiophen-6-yloxy)-4-(4-chlorophenyl) butyric acid methyl ester
-
-
4-(benzyloxy)-1-benzothiophene-2-carboximidamide
-
-
4-([[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy](phenyl)acetyl]amino)-N,N-dimethylbenzamide
-
-
4-phenyl-1-benzothiophene-2-sulfinimidamide
-
-
4-[phenyl(3-phenyl[1,2,4]oxadiazol-5-yl)methoxy]benzo[b]thiophene-2-carboxamidine
-
-
5-(3,4-dimethoxyphenyl)benzo[b]thiophene-2-carboxamidine
-
-
5-(benzyloxy)-1-benzothiophene-2-carboximidamide
-
-
5-phenyl-1-benzothiophene-2-carboximidamide
-
-
6-(2-phenylethoxy)-1-benzothiophene-2-carboximidamide
-
-
6-(3,4-dimethoxyphenyl)-1-benzothiophene-2-carboximidamide
-
-
6-(3-chloro-4-fluorobenzyloxy)benzo[b]thiophene-2-carboxamidine
-
-
6-(pyridin-3-ylmethoxy)-1-benzothiophene-2-carboximidamide
-
-
6-(thiophen-2-ylmethoxy)benzo[b]thiophene-2-carboxamidine
-
-
6-benzyloxybenzo[b]thiophene-2-carboxamidine
-
-
6-[(2-chlorobenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
-
6-[(2-fluorobenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
-
6-[(2-methoxybenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
-
6-[(3,4-difluorobenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
-
6-[(3-chlorobenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
-
6-[(3-fluorobenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
-
6-[(3-methoxybenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
-
6-[(4-chloro-3-fluorobenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
-
6-[(4-chlorobenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
-
6-[(4-fluorobenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
-
6-[(4-methoxybenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
-
6-[(4-methylbenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
-
6-[1-(4-fluorophenyl)ethoxy]-1-benzothiophene-2-carboximidamide
-
-
antithrombin
-
antithrombin III
-
aptamer
-
RNA aptamers isolated by iterative in vitro selection technique, complete inhibition at 0.00004 mM, inhibition is reversed by specific antidotes, i.e. oligonucleotides, complementary to the aptamers
-
Bovine pancreatic trypsin inhibitor
-
-
-
BPTI
-
Kunitz-type inhibitor, competitive, reversible inhbition, low molecular weight heparin binding to fIXa enhances reactivity of fIXa with the Kunitz-type inhibitor BPTI
-
Ca2+
-
5 mM
EDTA
-
complete inhibition at 20 mM
enoxaparin
-
competitive, reversible inhbition
ethyl 1-[4-([[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy](phenyl)acetyl]amino)phenyl]-1H-imidazole-2-carboxylate
-
-
ethyl 2-([2-(5-carbamimidoyl-1,1-dioxido-1-benzothiophen-3-yl)-3-phenylpropanoyl]amino)cyclohexanecarboxylate
-
-
ethyl 2-([2-(5-carbamimidoyl-1-benzofuran-3-yl)-3-phenylpropanoyl]amino)cyclohexanecarboxylate
-
-
ethyl 2-([2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]amino)cyclohexanecarboxylate
-
-
ethyl [(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]acetate
-
-
ethyl [(2-carbamimidoyl-1-benzothiophen-6-yl)oxy]acetate
-
-
ethyl [4-[([2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethoxy]carbonyl)amino]-3,5-dimethyl-1H-pyrazol-1-yl]acetate
-
-
FIX1-47 peptide
-
benzoylphenylalanine containing peptide, 0.038 mM, 50% inhibition
-
heparin
-
in the presence of 0.3 mM bovine pancreatic trypsin inhibitor
methyl (1R)-2-(2-[2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]hydrazino)cyclohexanecarboxylate
-
-
methyl (1S,2R)-2-(2-[(2R)-2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]hydrazino)cyclohexanecarboxylate
-
-
methyl (1S,2R)-2-(2-[(2S)-2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]hydrazino)cyclohexanecarboxylate
-
-
methyl (1S,2R)-2-(2-[2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]hydrazino)cyclohexanecarboxylate
-
-
methyl 2-([2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]amino)cyclohexanecarboxylate
-
-
methyl 2-([2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenylpropanoyl]amino)cyclohexanecarboxylate
-
-
methyl 3-([[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy](phenyl)acetyl]amino)propanoate
-
-
methyl 4-[[(2-carbamimidoyl-1-benzothiophen-6-yl)oxy]methyl]benzoate
-
-
methyl [(2-carbamimidoyl-1-benzothiophen-6-yl)oxy](4-chlorophenyl)acetate
-
-
methyl [(2-carbamimidoyl-1-benzothiophen-6-yl)oxy](4-fluorophenyl)acetate
-
-
N-(2-amino-2-oxoethyl)-2-([2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]amino)cyclohexanecarboxamide
-
-
N-(4-[3-([4-(1H-benzimidazol-1-yl)phenyl]amino)-2-(5-carbamimidoyl-1H-indol-3-yl)-3-oxopropyl]phenyl)benzamide
-
-
N-1,3-benzothiazol-5-yl-2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanamide
-
-
N-1H-benzimidazol-2-yl-3-([2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenylpropanoyl]amino)benzamide
-
-
N-1H-benzimidazol-2-yl-4-([2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenylpropanoyl]amino)benzamide
-
-
N-benzyl-2-([2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]amino)cyclohexanecarboxamide
-
-
N-benzyl-2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylacetamide
-
-
N-[4-(1H-benzimidazol-1-yl)-2-fluorophenyl]-2-(5-carbamimidoyl-1-methyl-1H-indol-3-yl)-3-phenylpropanamide
-
-
N-[4-(1H-benzimidazol-1-yl)-2-fluorophenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenylpropanamide
-
-
N-[4-(1H-benzimidazol-1-yl)-2-fluorophenyl]-2-(6-carbamimidoyl-1H-indol-1-yl)-3-phenylpropanamide
-
-
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-naphthalen-1-ylpropanamide
-
-
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanamide
-
-
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1-benzothiophen-3-yl)butanamide
-
-
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-2-methylpropanamide
-
-
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-3-(4-[(phenylsulfonyl)amino]phenyl)propanamide
-
-
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-3-cyclohexylpropanamide
-
-
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-3-naphthalen-2-ylpropanamide
-
-
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-3-pyridin-3-ylpropanamide
-
-
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-4-phenylbutanamide
-
-
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)butanamide
-
-
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)propanamide
-
-
N-[4-(1H-benzimidazol-2-yl)phenyl]-2-benzyl-3-(5-carbamimidoyl-1H-indol-3-yl)propanamide
-
-
N-[4-(1H-benzimidazol-2-yl)phenyl]-3-(5-carbamimidoyl-1H-indol-3-yl)-4-phenylbutanamide
-
-
Na+
-
200 mM in the absence of Ca2+, 185 mM in the presence of 5 mM Ca2+
PN2-KPI
-
Kunitz-type inhibitor, competitive, reversible inhbition
-
Polyethylene glycol
-
inhibition with increasing concentration
Rb+
-
slightly inhibiting in presence of Ca2+
RB006
-
-
-
recombinant full-length tissue factor pathway inhibitor
-
-
-
supersulfated low molecular weight heparin
-
inhibits the intrinsic tenase (factor IXa-factor VIIIa) complex in an antithrombin-independent manner by 90% when using factor X as substrate. Supersulfated low molecular weight heparin is 32fold more potent than unmodified low molecular weight heparin in the inhibition of factor X activation by the intrinsic tenase complex
-
TFPI-K1
-
Kunitz-type inhibitor, competitive, reversible inhbition
-
unmodified low molecular weight heparin
-
-
-
[(2-carbamimidoyl-1-benzothiophen-6-yl)oxy](4-fluorophenyl)acetic acid
-
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,2-dicaproyl-sn-glycero-3-phospho-L-serine
-
up-regulates the catalytic activity of the enzyme
1,2-propanediol
-
25-40% v/v, up to 20fold increase of the activity, methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide as substrate, rFIXa
1,3-Propanediol
-
affect the activity only to a slight extent; affect the activity only to a slight extent, rFIXa
1,4-Butanediol
-
affect the activity only to a slight extent, rFIXa
anionic phospholipid
-
highly activating
-
cofactor VIIIa
-
-
-
diethylene glycol
-
increases the activity 2fold
enoxaparin
-
in the presence of bovine pancreatic trypsin inhibitor
ethanol
-
25% v/v, 6fold increase of the activity, methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide as substrate, rFIXa, alcohols modify the conformation of FIXa rendering the active-site cleft more easily accessible to tripeptide substrates with a hydrophobic residue in the P3-position
ethylene glycol
factor FVIIa
-
in complex with tissue factor and Ca2+
-
factor FVIIIa
-
-
-
factor FXIa
-
in presence of 5 mM CaCl2
-
Factor IX
-
concentrations of approximately 100 nM, physiological levels in plasma, increases the activation of factor X catalyzed by factor IXa by increasing the affinity of the factor X for the intrinsic factor X activation complex
-
factor IX-specific antibodies
-
antibosies specific for human factor I, e.g. 198A1, 198B3, and 224F3, enhance the factor IXa activity mimicking the stimulatory effect of FVIIIa, and thus can replace FVIIIa as cofactor in the FX activation reaction, overview
-
factor VIIa/tissue factor
-
-
-
factor VIII
-
in modified form, established in the activation of factor X
-
Factor VIIIa
-
Factor XIa
-
factor XIa proteolytically activates factor IX by an exosite- and Ca2+-mediated release-rebind mechanism. XIa cleaves IX after Arg145, forming IXalpha, and then after Arg180, forming IXabeta
-
FIXa
-
12.5 nM in Tris buffered saline/Ca2+ for 2 h at 37 C
-
FVIII
-
in absence of FVIIIa decreased catalytic activity of enzyme FIXa
-
GIGAVLKVLTTGLPALISSWIKRKRQQ
-
approx. 600fold lower km, slight increase in kcat
glycerol
-
50% v/v, 6fold increase of the activity, methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide as substrate, rFIXa
heparin
i-erythritol
-
50% v/v, 1.5fold increase of the activity, methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide as substrate, rFIXa
low molecular weight heparin
-
enhances the activity of factor IXa (0.01 mM used in assay conditions)
-
methanol
-
25% v/v, 4fold increase of the activity, methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide as substrate, rFIXa, alcohols modify the conformation of FIXa rendering the active-site cleft more easily accessible to tripeptide substrates with a hydrophobic residue in the P3-position
phosphatidylserine
-
up-regulates the catalytic activity of the enzyme
Phospholipid
phospholipid membrane
-
Phospholipids
platelet factor 3
-
in vivo, established in the activation of factor X
-
tert-butanol
-
up to 10% v/v, increase of the activity, higher concentrations lead to a drastic activity decrease, methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide as substrate, rFIXa, alcohols modify the conformation of FIXa rendering the active-site cleft more easily accessible to tripeptide substrates with a hydrophobic residue in the P3-position
tissue factor
-
-
-
TRYLRIHPQSWVHQIALRMEV
-
approx. 600fold lower km, slight increase in kcat, optimal activation in the presence of 0.5-1 mM Ca2+
vitamin K
-
dependent on
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.5 - 8.7
4-methylsulfonyl-D-Leu-Gly-Arg-p-nitroanilide
1.7 - 3.2
CH3SO2-D-Leu-Gly-Arg-4-nitroanilide
2.3
CH3SO2-D-Leu-Gly-L-Arg-p-nitroanilide
-
-
0.000001 - 0.38
Factor X
-
1.2 - 2.3
L-Leu-Gly-L-Arg-4-nitroanilide
3.62
methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide
-
rFIXa, at pH 7.4, in the presence of 33% v/v ethylene glycol
1.43
methylsulfonyl-D-cyclohexylglycyl-Gly-Arg-p-nitroanilide
-
rFIXa, at pH 7.4, in the presence of 33% v/v ethylene glycol
5.99
methylsulfonyl-D-hexahydrotyrosyl-Gly-Arg-p-nitroanilide
-
rFIXa, at pH 7.4, in the presence of 33% v/v ethylene glycol
additional information
additional information
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.005 - 3.38
4-methylsulfonyl-D-Leu-Gly-Arg-p-nitroanilide
18.5 - 21.9
CH3SO2-D-Leu-Gly-Arg-4-nitroanilide
13.2
CH3SO2-D-Leu-Gly-L-Arg-p-nitroanilide
Homo sapiens
-
-
0.00011 - 1999
Factor X
-
17.5 - 21.4
L-Leu-Gly-L-Arg-4-nitroanilide
2.01
methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide
Homo sapiens
-
rFIXa, at pH 7.4, in the presence of 33% v/v ethylene glycol
5.67
methylsulfonyl-D-cyclohexylglycyl-Gly-Arg-p-nitroanilide
Homo sapiens
-
rFIXa, at pH 7.4, in the presence of 33% v/v ethylene glycol
6.11
methylsulfonyl-D-hexahydrotyrosyl-Gly-Arg-p-nitroanilide
Homo sapiens
-
rFIXa, at pH 7.4, in the presence of 33% v/v ethylene glycol
additional information
2-[5-Amino-2-(4-fluoro-phenyl)-6-oxo-6H-pyrimidin-1-yl]-N-(1-benzyl-2-oxo-2-thiazol-2-yl-ethyl)-acetamide
Homo sapiens
-
the catalytic efficiency kcat/Km, of phospholipid vesicles containing 20 or 35% phosphatidylethanolamine and no phosphatidylserine is 5.5fold higher than that of vesicles containing 1% phosphatidylserine and no phosphatidylethanolamine
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00011 - 0.00037
D-Leu-Phg-Arg-4-nitroanilide
160397
0.83 - 49000
Factor X
346
9.3 - 14.6
L-Leu-Gly-L-Arg-4-nitroanilide
19573
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0005
(2-carbamimidoylbenzo[b]thiophen-4-yloxy)phenylacetic acid methyl ester
-
pH and temperature not specified in the publication
0.000003
(2-carbamimidoylbenzo[b]thiophen-6-yloxy)thiophen-2-ylacetic acid ethyl ester
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.00048
(2R)-N-1,3-benzothiazol-5-yl-2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanamide
-
-
0.000018
(2R)-N-[4-(1H-benzimidazol-1-yl)-2-fluorophenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenylpropanamide
-
-
0.01422
(2S)-N-1,3-benzothiazol-5-yl-2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanamide
-
-
0.00082
(2S)-N-[4-(1H-benzimidazol-1-yl)-2-fluorophenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenylpropanamide
-
-
0.00515
2-(2-carbamimidoylbenzo[b]thiophen-4-yloxy)propionic acid methyl ester
-
pH and temperature not specified in the publication
0.0001
2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenyl-N-(4-[3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl)propanamide
-
-
0.00039
2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenyl-N-[4-(4-phenyl-1H-imidazol-1-yl)phenyl]propanamide
-
-
0.00173
2-(5-carbamimidoyl-1-benzothiophen-3-yl)-N-(4-cyanophenyl)-3-phenylpropanamide
-
-
0.00058
2-(5-carbamimidoyl-1-benzothiophen-3-yl)-N-(4-methylphenyl)-3-phenylpropanamide
-
-
0.00025
2-(5-carbamimidoyl-1-benzothiophen-3-yl)-N-(4-phenoxyphenyl)-3-phenylpropanamide
-
-
0.00093
2-(5-carbamimidoyl-1-benzothiophen-3-yl)-N-(4-[(6-chloropyridazin-3-yl)sulfamoyl]phenyl)-3-phenylpropanamide
-
-
0.0096
2-(5-carbamimidoyl-1-benzothiophen-3-yl)-N-(5-fluoro-2-methylphenyl)-3-phenylpropanamide
-
-
0.00066
2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenyl-N-(2'-sulfamoylbiphenyl-4-yl)propanamide
-
-
0.00027
2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenyl-N-[4-(5-phenyl-1H-imidazol-4-yl)phenyl]propanamide
-
-
0.0067
2-(5-carbamimidoyl-1H-indol-3-yl)-N-(2'-sulfamoylbiphenyl-4-yl)acetamide
-
-
0.00031
2-(5-carbamimidoyl-1H-indol-3-yl)-N-(4-ethylphenyl)-3-phenylpropanamide - 1H-benzimidazole
-
(1:1)
0.00024
2-(7-carbamimidoylnaphthalen-1-yl)-N-[2-(1-ethoxyethenyl)cyclohexyl]-3-phenylpropanamide
-
-
0.00043
2-([2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]amino)-N-ethylcyclohexanecarboxamide
-
-
0.0035
2-([2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]amino)cyclohexanecarboxylic acid
-
-
0.00095
2-amidino-4-iodobenzothiophene
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.00029
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenyl-N-[4-(pyrrolidin-1-ylcarbonyl)phenyl]acetamide
-
pH and temperature not specified in the publication
0.00001
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (1,3-dimethyl-1H-pyrazol-5-yl)carbamate
-
pH and temperature not specified in the publication
0.000007
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (2,4-difluorophenyl)carbamate
-
pH and temperature not specified in the publication
0.000007
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (2,6-difluorophenyl)carbamate
-
pH and temperature not specified in the publication
0.000005
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (2-fluorophenyl)carbamate
-
pH and temperature not specified in the publication
0.000008
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (2-methylphenyl)carbamate
-
pH and temperature not specified in the publication
0.000002
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (2-[[(2-methylpropyl)amino]methyl]phenyl)carbamate
-
pH and temperature not specified in the publication
0.000012
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (3,5-dimethyl-1,2-oxazol-4-yl)carbamate
-
pH and temperature not specified in the publication
0.000008
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (3,5-dimethyl-1H-pyrazol-4-yl)carbamate
-
pH and temperature not specified in the publication
0.000025
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (3-fluorophenyl)carbamate
-
pH and temperature not specified in the publication
0.000008
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (4-fluorophenyl)carbamate
-
pH and temperature not specified in the publication
0.000005
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl (4-methoxyphenyl)carbamate
-
pH and temperature not specified in the publication
0.00001
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl phenylcarbamate
-
pH and temperature not specified in the publication
0.000003
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [1,3-dimethyl-5-[(propan-2-ylamino)methyl]-1H-pyrazol-4-yl]carbamate
-
pH and temperature not specified in the publication
0.000005
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [1-methyl-3-[(methylamino)methyl]-1H-pyrazol-5-yl]carbamate
-
pH and temperature not specified in the publication
0.000004
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [2-(aminomethyl)phenyl]carbamate
-
pH and temperature not specified in the publication
0.000003
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [2-(piperazin-1-ylmethyl)phenyl]carbamate
-
pH and temperature not specified in the publication
0.000008
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [2-[(dimethylamino)methyl]phenyl]carbamate
-
pH and temperature not specified in the publication
0.000003
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [2-[(methylamino)methyl]phenyl]carbamate
-
pH and temperature not specified in the publication
0.000009
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [3-(methoxymethyl)-1-methyl-1H-pyrazol-5-yl]carbamate
-
pH and temperature not specified in the publication
0.00001
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [4-[(4-methylpiperazin-1-yl)methyl]phenyl]carbamate
-
pH and temperature not specified in the publication
0.000004
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [4-[2-(dimethylamino)ethoxy]phenyl]carbamate
-
pH and temperature not specified in the publication
0.000005
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl [5-[(ethylamino)methyl]-1,3-dimethyl-1H-pyrazol-4-yl]carbamate
-
pH and temperature not specified in the publication
0.00017
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-N,2-diphenylacetamide
-
pH and temperature not specified in the publication
0.00014
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-N-(2-methoxyphenyl)-2-phenylacetamide
-
pH and temperature not specified in the publication
0.00013
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-N-(3-methoxyphenyl)-2-phenylacetamide
-
pH and temperature not specified in the publication
0.00014
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-N-(4-methoxyphenyl)-2-phenylacetamide
-
pH and temperature not specified in the publication
0.001
2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-N-[2-(dimethylamino)ethyl]-2-phenylacetamide
-
pH and temperature not specified in the publication
0.00198
2-[(2-carbamimidoyl-1-benzothiophen-6-yl)oxy]-2-(4-fluorophenyl)acetamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.0000155
2-[(2-carbamimidoyl-6-fluoro-1-benzothiophen-4-yl)oxy]-2-phenylethyl phenylcarbamate
-
pH and temperature not specified in the publication
0.0000044
2-[(2-carbamimidoyl-6-fluoro-1-benzothiophen-4-yl)oxy]-2-phenylethyl [2-(aminomethyl)phenyl]carbamate
-
pH and temperature not specified in the publication
0.0000081
2-[(2-carbamimidoyl-6-fluoro-1-benzothiophen-4-yl)oxy]-2-phenylethyl [2-[(dimethylamino)methyl]phenyl]carbamate
-
pH and temperature not specified in the publication
0.0049
3-(1-[4-(1H-benzimidazol-1-yl)phenyl]-2-oxopyrrolidin-3-yl)-1-benzothiophene-5-carboximidamide
-
-
0.000028
3-(2-carbamimidoylbenzo[b]thiophen-6-yloxy)-3-(4-chlorophenyl)propionic acid methyl ester
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.000063
3-(2-[4-(1H-benzimidazol-1-yl)phenyl]-1-benzyl-2-oxoethyl)-1-benzothiophene-5-carboximidamide
-
-
0.000074
3-(4-aminophenyl)-N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1-benzothiophen-3-yl)propanamide
-
-
0.000075
3-(4-aminophenyl)-N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)propanamide
-
-
0.000059
3-[3-([4-(1H-benzimidazol-1-yl)phenyl]amino)-2-(5-carbamimidoyl-1H-indol-3-yl)-3-oxopropyl]benzoic acid
-
-
0.00066
4-(([2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenylpropanoyl]amino)methyl)-N-[5-(methylsulfonyl)-1H-benzimidazol-2-yl]benzamide
-
-
0.000036
4-(2-carbamimidoylbenzo[b]thiophen-6-yloxy)-4-(4-chlorophenyl) butyric acid methyl ester
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.0015
4-(benzyloxy)-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.00037
4-([[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy](phenyl)acetyl]amino)-N,N-dimethylbenzamide
-
pH and temperature not specified in the publication
0.0016
4-phenyl-1-benzothiophene-2-sulfinimidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.00027
4-[phenyl(3-phenyl[1,2,4]oxadiazol-5-yl)methoxy]benzo[b]thiophene-2-carboxamidine
-
pH and temperature not specified in the publication
0.0059
5-(3,4-dimethoxyphenyl)benzo[b]thiophene-2-carboxamidine
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.0019
5-(benzyloxy)-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.008
5-phenyl-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.0216
6-(2-phenylethoxy)-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.0008 - 0.0242
6-(3,4-dimethoxyphenyl)-1-benzothiophene-2-carboximidamide
0.000031
6-(3-chloro-4-fluorobenzyloxy)benzo[b]thiophene-2-carboxamidine
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.00035
6-(pyridin-3-ylmethoxy)-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.00035
6-(thiophen-2-ylmethoxy)benzo[b]thiophene-2-carboxamidine
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.0038
6-benzyloxybenzo[b]thiophene-2-carboxamidine
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.0072
6-[(2-chlorobenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.023
6-[(2-fluorobenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.0269
6-[(2-methoxybenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.00045
6-[(3,4-difluorobenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.0009
6-[(3-chlorobenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.00068
6-[(3-fluorobenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.00045
6-[(3-methoxybenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.000075
6-[(4-chloro-3-fluorobenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.00045
6-[(4-chlorobenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.0007
6-[(4-fluorobenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.00025
6-[(4-methoxybenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.0009
6-[(4-methylbenzyl)oxy]-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.0113
6-[1-(4-fluorophenyl)ethoxy]-1-benzothiophene-2-carboximidamide
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.037 - 0.7
Bovine pancreatic trypsin inhibitor
-
0.00042
ethyl 1-[4-([[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy](phenyl)acetyl]amino)phenyl]-1H-imidazole-2-carboxylate
-
pH and temperature not specified in the publication
0.00853
ethyl 2-([2-(5-carbamimidoyl-1,1-dioxido-1-benzothiophen-3-yl)-3-phenylpropanoyl]amino)cyclohexanecarboxylate
-
-
0.0019
ethyl 2-([2-(5-carbamimidoyl-1-benzofuran-3-yl)-3-phenylpropanoyl]amino)cyclohexanecarboxylate
-
-
0.00012
ethyl 2-([2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]amino)cyclohexanecarboxylate
-
-
0.0119
ethyl [(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]acetate
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.0038
ethyl [(2-carbamimidoyl-1-benzothiophen-6-yl)oxy]acetate
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.000011
ethyl [4-[([2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethoxy]carbonyl)amino]-3,5-dimethyl-1H-pyrazol-1-yl]acetate
-
pH and temperature not specified in the publication
0.0005
methyl (1R)-2-(2-[2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]hydrazino)cyclohexanecarboxylate
-
-
0.00028
methyl (1S,2R)-2-(2-[(2R)-2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]hydrazino)cyclohexanecarboxylate
-
-
0.0413
methyl (1S,2R)-2-(2-[(2S)-2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]hydrazino)cyclohexanecarboxylate
-
-
0.00031
methyl (1S,2R)-2-(2-[2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]hydrazino)cyclohexanecarboxylate
-
-
0.00014
methyl 2-([2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]amino)cyclohexanecarboxylate
-
-
0.00034
methyl 2-([2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenylpropanoyl]amino)cyclohexanecarboxylate
-
-
0.0084
methyl 3-([[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy](phenyl)acetyl]amino)propanoate
-
pH and temperature not specified in the publication
0.0113
methyl 4-[[(2-carbamimidoyl-1-benzothiophen-6-yl)oxy]methyl]benzoate
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.00002
methyl [(2-carbamimidoyl-1-benzothiophen-6-yl)oxy](4-chlorophenyl)acetate
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.00004
methyl [(2-carbamimidoyl-1-benzothiophen-6-yl)oxy](4-fluorophenyl)acetate
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
0.00028
N-(2-amino-2-oxoethyl)-2-([2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]amino)cyclohexanecarboxamide
-
-
0.00027
N-(4-[3-([4-(1H-benzimidazol-1-yl)phenyl]amino)-2-(5-carbamimidoyl-1H-indol-3-yl)-3-oxopropyl]phenyl)benzamide
-
-
0.00078
N-1,3-benzothiazol-5-yl-2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanamide
-
-
0.0019
N-1H-benzimidazol-2-yl-3-([2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenylpropanoyl]amino)benzamide
-
-
0.00093
N-1H-benzimidazol-2-yl-4-([2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenylpropanoyl]amino)benzamide
-
-
0.032
N-benzyl-2-([2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanoyl]amino)cyclohexanecarboxamide
-
-
0.00039
N-benzyl-2-[(2-carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylacetamide
-
pH and temperature not specified in the publication
0.00036
N-[4-(1H-benzimidazol-1-yl)-2-fluorophenyl]-2-(5-carbamimidoyl-1-methyl-1H-indol-3-yl)-3-phenylpropanamide
-
-
0.000063
N-[4-(1H-benzimidazol-1-yl)-2-fluorophenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-3-phenylpropanamide
-
-
0.0003
N-[4-(1H-benzimidazol-1-yl)-2-fluorophenyl]-2-(6-carbamimidoyl-1H-indol-1-yl)-3-phenylpropanamide
-
-
0.00023
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-naphthalen-1-ylpropanamide
-
-
0.000098
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1-benzothiophen-3-yl)-3-phenylpropanamide
-
-
0.00024
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1-benzothiophen-3-yl)butanamide
-
-
0.00075
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-2-methylpropanamide
-
-
0.00013
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-3-(4-[(phenylsulfonyl)amino]phenyl)propanamide
-
-
0.0038
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-3-cyclohexylpropanamide
-
-
0.000098
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-3-naphthalen-2-ylpropanamide
-
-
0.0012
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-3-pyridin-3-ylpropanamide
-
-
0.00024
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)-4-phenylbutanamide
-
-
0.00016
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)butanamide
-
-
0.00048
N-[4-(1H-benzimidazol-1-yl)phenyl]-2-(5-carbamimidoyl-1H-indol-3-yl)propanamide
-
-
0.00013
N-[4-(1H-benzimidazol-2-yl)phenyl]-2-benzyl-3-(5-carbamimidoyl-1H-indol-3-yl)propanamide
-
-
0.00025
N-[4-(1H-benzimidazol-2-yl)phenyl]-3-(5-carbamimidoyl-1H-indol-3-yl)-4-phenylbutanamide
-
-
0.025 - 0.813
Na+
0.0000025 - 0.00017
supersulfated low molecular weight heparin
-
0.00001 - 0.00147
unmodified low molecular weight heparin
-
0.000021
[(2-carbamimidoyl-1-benzothiophen-6-yl)oxy](4-fluorophenyl)acetic acid
-
in 50 mM Tris, 100 mM NaCl, 5 mM CaCl2, 0.5% (w/v) PEG6000 (pH 7.4), at 22C
additional information
additional information
-
inhibition kinetics
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.3 - 7.4
-
assay at
7.4
-
assay at
7.5
-
assay at
8
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22
-
assay at room temperature
25
-
assay at
37
-
assay at
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
factor IXa binds specifically to the surface of endothelial cells
Manually annotated by BRENDA team
additional information
-
binding of a subpopulation of platelets to the enzyme is activated by the protease-activated receptor-1, PAR-1, requirring both release of calcium from internal stores and influx of extracellular calcium, overview
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
PDB
SCOP
CATH
ORGANISM
UNIPROT
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6000
-
x * 6000, SDS-PAGE
16600
-
1 * 27300 + 1 * 16600, SDS-PAGE
17000
-
1 * 27000 + 1 * 17000, SDS-PAGE
18000
-
1 * 28000 + 1 * 18000, SDS-PAGE
27000
-
1 * 27000 + 1 * 17000, SDS-PAGE
27300
-
1 * 27300 + 1 * 16600, SDS-PAGE
28000
-
1 * 28000 + 1 * 18000, SDS-PAGE
46500
-
SDS-PAGE
47000
-
factor IXabeta', non reducing PAGE
55000
-
factor IXaalpha, non reducing PAGE
56000
-
x * 56000, SDS-PAGE
70000
-
value about, SDS-PAGE
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
the fully active enzyme consists of a light and a heavy chain held together by a single disulfie bond
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glycoprotein
-
-
proteolytic modification
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
hanging drop vapor diffusion method, using 0.25 M ammonium acetate, 19.5% (w/v) PEG 3350
-
of a recombinant two-domain construct of fIXa in complex with p-benzamidine. The 99-loop on Tyr99 plays a major role in substrate interaction, it may be rearranged in the factor X activation complex
-
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-20C, 0.05 M imidazole buffer, pH 6.0, 0.2 M NaCl, no loss of activity after several months
-
22C, recombinant human FIX in soybean seeds, 6 years, no loss of activity
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
combination of anion exchange and affinity/cation exchange chromatography
-
DEAE-Sepharose column chromatography and HiTrap Q column chromatography
-
factor IXabeta'
-
gel filtration
-
heparin Sepharose column chromatography and Q Sepharose column chromatography
-
ion exchange chromatography on Q-Sepharose
-
ion-exchange chromatography
-
method not mentioned
-
Ni-NTA column chromatography, gel filtration
-
Q-Sepharose of column, affinity purification with heparin sepharose, gel filtration
-
recombinant factor IXa
-
recombinant fIXa
-
recombinant wild-type and mutant enzymes from HEK-293 cells by anion exchange and heparin affinity chromatography
-
recombinant wild-type and mutant enzymes from HEK-293 cells by immunoaffinity and anion exchange chromatogaphy
-
recombinant wild-type and mutant factor IXa, immunoaffinity chromatography using HPC4 monoclonal antibodies
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
expressed in Escherichia coli BL21 Star (DE3) cells
-
expressed in Escherichia coli BL21(DE3) cells
-
expressed in Escherichia coli DH5alpha cells
-
expressed in HEK-293 cells
-
expressed in HEK293 cells
-
expressed in human embryonic kidney 293 cell line
-
expressed in modified HEK-293 cell line Flp-In-293
-
expressed in transgenic seeds of Glycine max
-
expression in CHO cells
-
expression in Escherichia coli BL21
-
expression in HEK 293 cells
-
expression in HEK293 cells
-
expression of wild-type and mutant enzymes in HEK-293 cells
-
stable expression of wild-type and mutant enzymes in HEK-293 cells
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
D47G
-
factor IXaAL, causes lower rates of factor X activation, Asp47 and the cleavage of Arg145-Ala146 are important structural features required for specific, high affinity factor IXa binding to platelets in the presence of factors VIIIa and factor X
E186A
-
site-directed mutagenesis, the fIXa mutant exhibits normal activity towards a fIXa-specific chromogenic substrate in the presence of Ca2+ with no obvious requirement for Na+ in the reaction, the mutant interacts with factor VIIIa with near normal affinity and catalyzes the activation of factor X in the intrinsic Xase complex with a normal catalytic efficiency
FIXagamma225P
-
mutant enzyme
G94R
-
33% of wild-type vmax
Gla-domainless factor IXa
-
20000times lower kacat for factor X hydrolysis than wild-type
H185A
-
site-directed mutagenesis, the fIXa mutant exhibits normal activity towards a fIXa-specific chromogenic substrate in the presence of Ca2+ with no obvious requirement for Na+ in the reaction, the mutant interacts with factor VIIIa with near normal affinity and catalyzes the activation of factor X in the intrinsic Xase complex with a normal catalytic efficiency
K265A
-
no change in binding of anti fIX monoclonal antibodies CLB-fIX 14 and CLB-fIX 13
K98A
-
site-directed mutagenesis,
N346D
-
no change in binding of anti fIX monoclonal antibodies CLB-fIX 14, no binding of anti fIX monoclonal antibody CLB-fIX 13
R143A
-
4times lower kcat for factor X hydrolysis than wild-type Gla-domainless factor IXa
R145H
-
factor IXaCH, causes lower rates of factor X activation, Asp47 and the cleavage of Arg145-Ala146 are important structural features required for specific, high affinity factor IXa binding to platelets in the presence of factors VIIIa and factor X
R147A
-
3times lower kcat for factor X hydrolysis than wild-type Gla-domainless factor IXa
R150
-
similar kcat for factor X hydrolysis as wild-type Gla-domainless factor IXa
R170A
-
the mutation slightly (0.5fold) reduces supersulfated low molecular weight heparin affinity
R188A
-
site-directed mutagenesis, the fIXa mutant exhibits normal activity towards a fIXa-specific chromogenic substrate in the presence of Ca2+ with no obvious requirement for Na+ in the reaction, the mutant interacts with factor VIIIa with near normal affinity and catalyzes the activation of factor X in the intrinsic Xase complex with a normal catalytic efficiency
R233A
-
the mutation dramatically (14fold) reduces supersulfated low molecular weight heparin affinity
R333Q
-
activation of factor X is not impaired
R94D
-
slight increase in vmax
rFIXa104A
-
recombinant FIXa alanine point mutation in loop 2 of the EGF2 domain
rFIXa105A
-
recombinant FIXa alanine point mutation in loop 2 of the EGF2 domain
rFIXa107A
-
recombinant FIXa alanine point mutation in loop 2 of the EGF2 domain
rFIXa89A
-
recombinant FIXa alanine point mutation in loop 1 of the EGF2 domain
rFIXa90A
-
recombinant FIXa alanine point mutation in loop 1 of the EGF2 domain
rFIXa91A
-
recombinant FIXa alanine point mutation in loop 1 of the EGF2 domain
rFIXa94A
-
recombinant FIXa alanine point mutation in loop 1 of the EGF2 domain
Y450C
-
the mutant shows about 5% activity compared to the wild type enzyme
Y450F
-
the mutant shows about 25% activity compared to the wild type enzyme
Y450S
-
the mutant shows about 5% activity compared to the wild type enzyme
Y94F/A95aK/K98T/Y177F
-
mutation, higher clotting activity than wild type FIXa
Y94F/A95aK/K98T/Y177F/I213V/E219G
-
about 6fold increased catalytic efficence compared to plasma-derived activated coagulation factor IX, higher clotting activity than wild type FIXa
Y94F/K98T
-
increased catalytic efficence compared to plasma-derived activated coagulation factor IX, higher clotting activity than wild type FIXa
Y94F/K98T/Y177F
-
increased catalytic efficence compared to plasma-derived activated coagulation factor IX, higher clotting activity than wild type FIXa
Y94F/K98T/Y177F/I213V/E219G
-
about 17fold increased catalytic efficence compared to plasma-derived activated coagulation factor IX, higher clotting activity than wild type FIXa
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine