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Information on EC 3.4.21.22 - coagulation factor IXa and Organism(s) Homo sapiens and UniProt Accession P00740

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     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.21 Serine endopeptidases
                3.4.21.22 coagulation factor IXa
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Select one or more organisms in this record: ?
This record set is specific for:
Homo sapiens
UNIPROT: P00740 not found.
Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria
Reaction Schemes
Selective cleavage of Arg-/-Ile bond in factor X to form factor Xa
Synonyms
factor ix, factor ixa, coagulation factor ix, activated factor ix, intrinsic xase, activated fix, coagulation factor ixa, factor ixabeta, factor ixan, blood coagulation factor ixa, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
activated Christmas factor
-
-
-
0
activated coagulation factor IX
247
-
activated factor IX
activated FIX
247
-
blood coagulation factor IXa
247
-
Christmas factor
-
-
-
0
circulating factor IXa
247
-
coagulation factor IX
coagulation factor IXa
292417
-
factor IX
247
-
factor IXa
factor IXaAL
247
variant protein, D47G
factor IXabeta
247
-
factor IXaCH
247
variant protein, R145H
factor IXalphabeta
247
-
factor IXaN
247
normal protein
factor XIa
292417
-
FIXC
292417
-
human coagulation factor IXa
247
-
intrinsic Xase
292417
-
additional information
292417
the enzyme is a member of the serine protease family and shares a high degree of homology with trypsin
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis
-
-
additional information
-
amidolytic activity
CAS REGISTRY NUMBER
COMMENTARY hide
37316-87-3
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
(methylsulfonyl)-D-cyclohexylalanine-Gly-Arg-7-amido-4-methylcoumarin + H2O
(methylsulfonyl)-D-cyclohexylalanine-Gly-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
Pefa10
-
-
?
(methylsulfonyl)-D-cyclohexylglycine-Gly-Arg-7-amido-4-methylcoumarin + H2O
(methylsulfonyl)-D-cyclohexylglycine-Gly-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
Pefa9
-
-
?
4-methylsulfonyl-D-Leu-Gly-Arg-p-nitroanilide + H2O
4-methylsulfonyl-D-Leu-Gly-Arg + p-nitroaniline
show the reaction diagram
-
-
-
?
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
-
-
?
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
N-alpha-benzyloxycarbonyl-D-arginylglycyl-L-arginine-para-nitroanilide + H2O
N-alpha-benzyloxycarbonyl-D-arginylglycyl-L-arginine + para-nitroaniline
show the reaction diagram
-
-
-
?
p-aminobenzamidine + H2O
p-aminobenzoic acid + NH3
show the reaction diagram
-
-
-
?
Spectrofluor FIXa + H2O
(methylsulfonyl)-D-cyclohexylglycine-Gly-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
i.e. (methylsulfonyl)-D-cyclohexylglycine-Gly-Arg-7-amido-4-methylcoumarin
-
-
?
tert-butoxycarbonyl-Ile-Glu-Gly-Arg-7-amido-4-methylcoumarin + H2O
tert-butoxycarbonyl-Ile-Glu-Gly-Arg + 7-amino-4-methylcoumarin
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
-
amidolytic activity
-
-
?
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
-
a chymotrypsin homologue, and one of the gamma-carboxyglutamic acid-containing blood coagulation factors. The proenzyme factor IX is activated by factor XIa
-
-
?
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
-
CBS 31.39
-
-
?
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 37°C
-
-
?
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
-
-
-
-
?
Nalpha-benzyloxycarbonyl-D-Arg-Gly-Arg-4-nitroanilide + H2O
Nalpha-benzyloxycarbonyl-D-Arg-Gly-Arg + 4-nitroaniline
show the reaction diagram
-
S-2765
-
-
?
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 SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
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
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
-
a chymotrypsin homologue, and one of the gamma-carboxyglutamic acid-containing blood coagulation factors. The proenzyme factor IX is activated by factor XIa
-
-
?
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 37°C
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
Factor VIIIa
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Na+
no requirement for Na+ in presence of Ca2+, can partially substite for Ca2+
lithium ion
-
activates slightly
additional information
factor IXa is not a Na+-binding protease
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,5-dansyl-Glu-Gly-Arg chloromethylketone
-
2-chloro-N-[3-methyl-1-(4-methyl-2-nitrophenyl)pyrrolidin-3-yl]-4-(4H-1,2,4-triazol-4-yl)benzamide
-
4-aminobenzamidine
-
antithrombin
-
BPTI
Kunitz-type inhibitor, competitive, reversible inhbition, low molecular weight heparin binding to fIXa enhances reactivity of fIXa with the Kunitz-type inhibitor BPTI
-
D-Phe-Pro-Arg chloromethylketone
-
EDTA
complete inhibition at 20 mM
enoxaparin
competitive, reversible inhbition
Glu-Gly-Arg chloromethylketone
-
N-[(3R)-1-(3-amino-4,5-dichloro-1,2-benzoxazol-7-yl)pyrrolidin-3-yl]-2-chloro-4-(4H-1,2,4-triazol-4-yl)benzamide
-
N-[(3R)-1-(3-amino-4-chloro-1,2-benzoxazol-7-yl)pyrrolidin-3-yl]-2-chloro-4-(4H-1,2,4-triazol-4-yl)benzamide
-
N-[(3R)-1-(3-amino-4-chloro[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-(1-methyl-2-oxo-1,2-dihydropyrimidin-5-yl)benzamide
-
N-[(3R)-1-(3-amino-4-chloro[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-(1-methyl-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl)benzamide
-
N-[(3R)-1-(3-amino-4-chloro[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)benzamide
-
N-[(3R)-1-(3-amino-4-chloro[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-(1H-imidazo[4,5-b]pyridin-1-yl)benzamide
-
N-[(3R)-1-(3-amino-4-chloro[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
N-[(3R)-1-(3-amino-4-chloro[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-(4H-1,2,4-triazol-4-yl)benzamide
-
N-[(3R)-1-(3-amino-4-chloro[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-(pyrimidin-2-yl)benzamide
-
N-[(3R)-1-(3-amino-4-chloro[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-(pyrimidin-5-yl)benzamide
-
N-[(3R)-1-(3-amino-4-chloro[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-[3-(difluoromethyl)-4H-1,2,4-triazol-4-yl]benzamide
-
N-[(3R)-1-(3-amino-4-chloro[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-[4-(2-hydroxyethyl)-1H-imidazol-1-yl]benzamide
-
N-[(3R)-1-(3-amino-4-chloro[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-4-(1H-benzimidazol-1-yl)-2-chlorobenzamide
-
N-[(3R)-1-(3-amino-4-fluoro-1,2-benzoxazol-7-yl)pyrrolidin-3-yl]-2-chloro-4-(4H-1,2,4-triazol-4-yl)benzamide
-
N-[(3R)-1-(3-amino-5-methyl[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-(4H-1,2,4-triazol-4-yl)benzamide
-
N-[1-(3-amino-1,2-benzoxazol-7-yl)pyrrolidin-3-yl]-2-chloro-4-(4H-1,2,4-triazol-4-yl)benzamide
-
N-[1-(3-amino-5-methyl-1,2-benzoxazol-7-yl)pyrrolidin-3-yl]-2-chloro-4-(4H-1,2,4-triazol-4-yl)benzamide
-
N-[1-(3-amino[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-(4H-1,2,4-triazol-4-yl)benzamide
-
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
-
TFPI-K1
Kunitz-type inhibitor, competitive, reversible inhbition
-
(2-carbamimidoylbenzo[b]thiophen-4-yloxy)phenylacetic acid methyl ester
-
-
(2-carbamimidoylbenzo[b]thiophen-6-yloxy)thiophen-2-ylacetic acid ethyl ester
-
-
(2E)-3-[(7S)-7-[2-chloro-4-(4H-1,2,4-triazol-4-yl)benzamido]-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]prop-2-enoic acid
-
-
(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
-
-
(7S)-2-methyl-7-phenyl-7-[4-(4H-1,2,4-triazol-4-yl)benzamido]-6,7,8,9-tetrahydropyrido[1,2-a]indole-10-carboxylic acid
-
-
(7S)-2-methyl-7-phenyl-7-[[5-(4H-1,2,4-triazol-4-yl)pyridine-2-carbonyl]amino]-6,7,8,9-tetrahydropyrido[1,2-a]indole-10-carboxylic acid
-
-
(7S)-7-[2-chloro-4-(1H-tetrazol-1-yl)benzamido]-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indole-10-carboxylic acid
-
-
(7S)-7-[2-chloro-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamido]-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indole-10-carboxylic acid
-
-
(7S)-7-[2-chloro-4-(4H-1,2,4-triazol-4-yl)benzamido]-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indole-10-carboxamide
-
-
1-(3-chloro-4-[[(2R)-2,8-dimethyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]carbamoyl]phenyl)-1H-benzimidazole-5-carboxylic acid
-
-
2,6-dichloro-4-(3-methyl-1H-1,2,4-triazol-1-yl)-N-[(2R)-8-methyl-2-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]benzamide
-
-
2,6-dichloro-N-((R)-2-((S)-1-hydroxyethyl)-8-methyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl)-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
-
2,6-dichloro-N-[(2R)-10-hydroxy-2,7-dimethyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
-
2,6-dichloro-N-[(2R)-2,8-dimethyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
-
2,6-dichloro-N-[(2R)-2-(3,4-difluorophenyl)-8-methyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
-
2,6-dichloro-N-[(2R)-2-(3-fluorophenyl)-8-methyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
-
2,6-dichloro-N-[(2R)-2-(4-fluorophenyl)-8-methyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
-
2,6-dichloro-N-[(2R)-8-methyl-2-(3-methylphenyl)-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
-
2,6-dichloro-N-[(2R)-8-methyl-2-[1-(propan-2-yl)-1H-1,2,3-triazol-4-yl]-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
-
2,6-dichloro-N-[(3R)-3,7-dimethyl-2,3,4,9-tetrahydro-1H-carbazol-3-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
-
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-chloro-N-[(2R)-2-(3-methoxyphenyl)-8-methyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
-
2-chloro-N-[(2R)-8-methyl-2-phenyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
-
2-chloro-N-[(7S)-10-cyclopropyl-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-4-(4H-1,2,4-triazol-4-yl)benzamide
-
-
2-chloro-N-[(7S)-10-[(E)-(hydroxyimino)methyl]-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-4-(4H-1,2,4-triazol-4-yl)benzamide
-
-
2-chloro-N-[(7S)-2-methyl-7-phenyl-10-(2,2,2-trifluoro-1-hydroxyethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-4-(4H-1,2,4-triazol-4-yl)benzamide
-
-
2-chloro-N-[(7S)-2-methyl-7-phenyl-10-(2H-tetrazol-5-yl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-4-(4H-1,2,4-triazol-4-yl)benzamide
-
-
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-[(7R)-7-[2-chloro-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamido]-2-methyl-7-phenyl-4a,6,7,8,9,10a-hexahydropyrido[1,2-a]indol-10-yl]propanoic acid
-
-
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-cyano-2-fluoro-N-(10-hydroxy-2,7-dimethyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl)benzamide
-
-
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
-
-
-
EDTA
-
complete inhibition at 20 mM
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-[(7S)-10-(5-aminopyridin-3-yl)-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-2-chloro-4-(4H-1,2,4-triazol-4-yl)benzamide
-
-
N-[2-(5,6-dimethyl-1H-benzimidazol-2-yl)ethyl]-4-(4H-1,2,4-triazol-4-yl)benzamide
-
-
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
-
-
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
-
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
anionic phospholipid
highly activating
-
factor FVIIa
in complex with tissue factor and Ca2+
-
factor FVIIIa
-
-
factor FXIa
in presence of 5 mM CaCl2
-
Factor VIIIa
-
Phospholipid
provided by platelet surface
phospholipid membrane
-
-
vitamin K
dependent on
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
1,4-Butanediol
-
affect the activity only to a slight extent, rFIXa
cofactor VIIIa
-
-
-
diethylene glycol
-
increases the activity 2fold
emicizumab
-
factorIXa/factorX bispecific antibody. Emicizumab functions as a cofactor to promote the factor IXa-catalyzed factor X activation
-
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 FVIIIa
-
-
-
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