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3.4.21.21: coagulation factor VIIa

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

Word Map on EC 3.4.21.21

Reaction

Selective cleavage of Arg-/-Ile bond in factor X to form factor Xa =

Synonyms

activated blood coagulation factor VII, activated coagulation factor VII, activated factor VII, blood coagulation factor VIIa, blood-coagulation factor VII, activated, blood-coagulation factor VIIa, coagulation factor VII, coagulation factor VII(a), coagulation FVII, Eptacog alfa, Factor VII, factor VIIa, factor VIIa-sTF, factor VIIa-TF, factor VIIa/tissue factor complex, FIIa, free factor VIIa, FVII, FVIIa, FVIIa-sTF, fVIIa/TF, FVIIc, human factor VIIa + TF, More, NovoSeven, procoagulant protein factor VII, recombinant factor VIIa, recombinant factor-activated VII, rFVII, rFVIIa, serine protease factor VIIa, Serum prothrombin conversion accelerator, soluble tissue factor/factor VIIa complex, sTF/VIIa, TF-FVIIa, TF/VIIa, tissue factor/factor VIIa, tissue factor/factor VIIa complex, vitamin K dependent clotting factor

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.21 Serine endopeptidases
                3.4.21.21 coagulation factor VIIa

IC50 Value

IC50 Value on EC 3.4.21.21 - coagulation factor VIIa

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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00034
2-(3'-amino-3-fluoro-4-(isopropylamino)-1,1'-biphenyl-2-yl)-N-(4-(amino(imino)methyl)benzyl)acetamide
Homo sapiens
-
IC50: 340 nM
0.0005
2-(3'-amino-4-(benzylamino)-3-fluoro-1,1'-biphenyl-2-yl)-N-(4-(amino(imino)methyl)benzyl)acetamide
Homo sapiens
-
IC50: 500 nM
0.0007
2-(3-allylamino-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl)-N-(4-carbamimidoyl-benzyl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 700 nM
0.00077
2-(3-benzylamino-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl)-N-(4-carbamimidoyl-benzyl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 770 nM
0.0064
2-(3-benzylsulfanyl-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl)-N-(4-carbamimidoyl-benzyl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0064 mM
0.0032
2-(3-butylamino-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl)-N-(4-carbamimidoyl-benzyl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0032 mM
0.0021
2-[3-(2-amino-ethylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0021 mM
0.00089
2-[3-(3-amino-propylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 890 nM
0.00098
2-[3-(4-amino-butylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 980 nM
0.003
2-[3-(4-tert-butyl-cyclohexylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.003 mM
0.013
2-[3-(adamantan-1-ylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.013 mM
0.00161
2-[6-(3-acetylamino-phenyl)-5-chloro-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.00161 mM
0.00007
2-[6-(3-amino-phenyl)-5-chloro-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 70 nM
0.00002
2-[6-(3-amino-phenyl)-5-chloro-3-cyclobutylamino-2-oxo-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 20 nM
0.00002
2-[6-(3-amino-phenyl)-5-chloro-3-isopropylamino-2-oxo-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 20 nM
0.0042
2-[6-(3-bromo-phenyl)-5-chloro-3-cyclobutylamino-2-oxo-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0042 mM
0.000039
3-(3-[(R)-2-[(S)-1-(4-carbamimidoyl-benzylcarbamoyl)-3-carbamoylpropylcarbamoyl]-2-ethanesulfonylamino-ethyl]-1H-indol-5-yloxymethyl)-benzoic acid
Homo sapiens
in 500 mM Tris-HCl, pH 7.5, 1.5 M NaCl, 50 mM CaCl2, temperature not specified in the publication
0.000118
3-amino-5-(1-(1-((4-(amino(imino)methyl)benzyl)-amino)-2-oxoethyl)-5-(isopropylamino)-6-oxo-1,6-dihydropyridin-2-yl)benzoic acid
Homo sapiens
-
IC50: 118 nM
0.000016
3-amino-5-[1-[2-([4-[amino(imino)methyl]benzyl]amino)-2-oxoethyl]-3-chloro-5-(isopropylamino)-6-oxo-1,6-dihydropyrazin-2-yl]benzoic acid
Homo sapiens
-
pH 8.0, IC50: 16 nM, potent and highly selective inhibitor, selectivity versus factor Xa and thrombin
0.0003
3-methyl-2-(3-phenyl-2-phenylmethanesulfonylamino-propionylamino)-pentanoic acid [4-guanidino-1-(thiazole-2-carbonyl)-butyl]-amide
Homo sapiens
-
IC50: 300 nM, reversible, covalent
0.00145
3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 0.00145 mM, reversible, covalent
0.00036
3-[1-[(4-carbamimidoyl-benzylcarbamoyl)-methyl]-3-chloro-5-isopropylamino-6-oxo-1,6-dihydro-pyrazin-2-yl]-benzoic acid
Homo sapiens
-
pH 8.0, IC50: 360 nM
0.00078
3-[1-[(4-carbamimidoyl-benzylcarbamoyl)-methyl]-3-chloro-5-isopropylamino-6-oxo-1,6-dihydro-pyrazin-2-yl]-benzoic acid methyl ester
Homo sapiens
-
pH 8.0, IC50: 780 nM
0.0007
4,4-dimethyl-2-(3-phenyl-2-phenylmethanesulfonylamino-propionylamino)-pentanoic acid [4-guanidino-1-(thiazole-2-carbonyl)-butyl]-amide
Homo sapiens
-
IC50: 700 nM, reversible, covalent
0.000204
5-(4-carboxybutoxy)-N-(ethylsulfonyl)-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
Homo sapiens
in 500 mM Tris-HCl, pH 7.5, 1.5 M NaCl, 50 mM CaCl2, temperature not specified in the publication
0.000056
5-[(3-carboxybenzyl)oxy]-N-(ethylsulfonyl)-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
Homo sapiens
in 500 mM Tris-HCl, pH 7.5, 1.5 M NaCl, 50 mM CaCl2, temperature not specified in the publication
0.00282
6-dimethylamino-2-(3-phenyl-2-phenylmethanesulfonylamino-propionylamino)-hexanoic acid [4-guanidino-1-(thiazole-2-carbonyl)-butyl]-amide
Homo sapiens
-
IC50: 0.00282 mM, reversible, covalent
0.0024
D-prolyl-N-(4-carbamimidoylbenzyl)-L-prolinamide
Homo sapiens
in 500 mM Tris-HCl, pH 7.5, 1.5 M NaCl, 50 mM CaCl2, temperature not specified in the publication
0.0000015 - 0.0000016
EEWEVLCWTWETCER
0.0000038
EEWEVLCWTWETCERGEG-(Z-domain of protein A)
Homo sapiens
-
IC50: 3.8 nM
-
0.0000015
EEWEVLCWTWETCERGEG-NH2
Homo sapiens
-
IC50: 1.5 nM
0.00000023
EEWEVLCWTWETCERGEGVEEELWEWR
Homo sapiens
-
maximal inhibition to 99%, IC50: 230 pM
0.00047
EVLCWTWETCER-NH2
Homo sapiens
-
IC50: 470 nM
0.0000048
EWEVLCWTWETCERGE-(Z-domain of protein A)
Homo sapiens
-
IC50: 4.8 nM
-
0.019
FFR-FVIIa
Homo sapiens
-
derivate of FVIIa with a stably buried N-terminus representing the active conformation of FVIIa, IC50: 0.019 mM
-
0.0001
hemextin AB complex
Homo sapiens
-
IC50: 100 nM
-
0.0000059
MEEWEVLCWTWETCERGEGQ-(Z-domain of protein A)
Homo sapiens
-
IC50: 5.9 nM
-
0.00045
N-(3-[1-[(4-carbamimidoyl-benzylcarbamoyl)-methyl]-3-chloro-6-oxo-5-phenethylamino-1,6-dihydro-pyrazin-2-yl]-phenyl)-2,2,2-trifluoro-acetamide
Homo sapiens
-
pH 8.0, IC50: 450 nM
0.0164
N-(4-(amino(imino)methyl)benzyl)-2-(2,6-difluoro-3-((2-phenylethyl)amino)phenyl)acetamide
Homo sapiens
-
IC50: 0.0164 mM
0.00398
N-(4-(amino(imino)methyl)benzyl)-2-(3-fluoro-4-((2-phenylethyl)amino)-1,1'-biphenyl-2-yl)acetamide
Homo sapiens
-
IC50: 0.00398 mM
0.0027
N-(4-(amino(imino)methyl)benzyl)-2-(3-hydroxy-4-((2-phenylethyl)amino)-1,1'-biphenyl-2-yl)acetamide
Homo sapiens
-
IC50: 0.0027 mM
0.0025
N-(4-(amino(imino)methyl)benzyl)-2-(3-hydroxy-4-(isopropylamino)-1,1'-biphenyl-2-yl)acetamide
Homo sapiens
-
IC50: 0.0025 mM
0.025
N-(4-(amino(imino)methyl)benzyl)-2-(3-methoxy-4-((2-phenylethyl)amino)-1,1'-biphenyl-2-yl)acetamide
Homo sapiens
-
IC50: 0.025 mM
0.0147
N-(4-(amino(imino)methyl)benzyl)-2-(4-(isopropylamino)-3-methoxy-1,1'-biphenyl-2-yl)acetamide
Homo sapiens
-
IC50: 0.0147 mM
0.0028
N-(4-(amino(imino)methyl)benzyl)-2-(5-(isopropylamino)-3,6-dioxo-2-phenylcyclohexa-1,4-dien-1-yl)acetamide
Homo sapiens
-
IC50: 0.0028 mM
0.000052
N-(4-(amino(imino)methyl)benzyl)-2-(6-(3,5-diaminophenyl)-3-(isopropylamino)-2-oxopyridin-1(2H)-yl)acetamide
Homo sapiens
-
IC50: 52 nM
0.00034
N-(4-carbamimidoyl-benzyl)-2-(2-oxo-3-phenethylamino-6-phenyl-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 340 nM
0.001
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-3-phenethylamino-6-m-tolyl-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.001 mM
0.00043
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-3-phenethylamino-6-o-tolyl-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 430 nM
0.00414
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-3-phenethylamino-6-p-tolyl-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.00414 mM
0.00063
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-3-phenethylamino-6-phenyl-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 630 nM
0.0112
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-6-phenyl-3-phenylamino-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0112 mM
0.00072
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-6-phenyl-3-prop-2-ynylamino-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 720 nM
0.0004
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-6-phenyl-3-propylamino-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 400 nM
0.0063
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-6-phenyl-3-pyrrolidin-1-yl-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0063 mM
0.0004
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-cyclobutylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 400 nM
0.0014
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-cyclohexylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0014 mM
0.0004
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-ethylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 400 nM
0.0002
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-isopropylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 200 nM
0.0007
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-methylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 700 nM
0.00345
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-6-ethyl-2-oxo-3-phenethylamino-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.00345 mM
0.00428
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-6-methyl-2-oxo-3-phenethylamino-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.00428 mM
0.0027
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-3-phenethylamino-6-(2-trifluoromethyl-phenyl)-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0027 mM
0.0029
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-3-phenethylamino-6-(3-trifluoromethyl-phenyl)-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0029 mM
0.0018
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-6-phenyl-3-(1-propyl-butylamino)-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0018 mM
0.0126
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-6-phenyl-3-(3-phenyl-propylamino)-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0126 mM
0.0063
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-6-phenyl-3-(3-trifluoromethyl-benzylamino)-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0063 mM
0.0041
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-6-phenyl-3-(4-phenyl-butylamino)-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0041 mM
0.001
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1,1-dioxo-tetrahydro-16-thiophen-3-ylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.001 mM
0.0098
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1-ethyl-hexylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0098 mM
0.00043
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1-ethyl-propylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 430 nM
0.00084
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1-methyl-butylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 840 nM
0.0009
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1-methyl-pentylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 900 nM
0.0038
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2,5-difluoro-benzylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0038 mM
0.0209
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2-dimethylamino-ethylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0209 mM
500
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2-hydroxy-ethylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 500 mM
880
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2-methoxy-ethylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 880 mM
0.008
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2-morpholin-4-yl-ethylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.008 mM
0.006
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(3,5-difluoro-benzylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.006 mM
0.0176
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(3-dimethylamino-propylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0176 mM
0.0005
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(3-hydroxy-propylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 500 nM
0.0043
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(4-chloro-benzylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0043 mM
0.0006
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(4-hydroxy-butylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 600 nM
0.00047
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(6-hydroxy-hexylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 470 nM
0.0091
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(isopropyl-methyl-amino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0091 mM
0.00034
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-cyclobutylamino-6-(2-hydroxy-phenyl)-2-oxo-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 340 nM
0.0002
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-cyclobutylamino-6-(3-hydroxy-phenyl)-2-oxo-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 200 nM
0.003
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(2-chloro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.003 mM
0.0018
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(2-fluoro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0018 mM
0.0016
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(2-methoxy-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0016 mM
0.00198
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-chloro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.00198 mM
0.0012
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-dimethylamino-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0012 mM
0.0023
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-fluoro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0023 mM
0.0006
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-methanesulfonylamino-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 600 nM
0.0052
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-methoxy-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0052 mM
0.0006
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-methylamino-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 600 nM
0.00252
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-nitro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.00252 mM
0.00888
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(4-chloro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.00888 mM
0.0081
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(4-fluoro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0081 mM
0.02345
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(4-methoxy-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.02345 mM
0.03
N-(4-carbamimidoyl-benzyl)-2-{5-chloro-2-oxo-6-phenyl-3-[2-(3-trifluoromethyl-phenyl)-ethylamino]-2H-pyrazin-1-yl}-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.03 mM
0.00018
N-(4-carbamimidoyl-benzyl)-2-{5-chloro-3-[2-(3-chloro-phenyl)-ethylamino]-2-oxo-6-phenyl-2H-pyrazin-1-yl}-acetamide
Homo sapiens
-
pH 8.0, IC50: 180 nM
0.0006
N-(4-carbamimidoyl-benzyl)-2-{5-chloro-3-[2-(4-chloro-phenyl)-ethylamino]-2-oxo-6-phenyl-2H-pyrazin-1-yl}-acetamide
Homo sapiens
-
pH 8.0, IC50: 600 nM
0.0167
N-(5-carbamimidoyl-pyridin-2-ylmethyl)-2-(2-oxo-3-phenethylamino-6-phenyl-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0167 mM
0.0014
N-(6-carbamimidoyl-pyridin-3-ylmethyl)-2-(2-oxo-3-phenethylamino-6-phenyl-2H-pyrazin-1-yl)-acetamide
Homo sapiens
-
pH 8.0, IC50: 0.0014 mM
0.000069
N-(ethylsulfonyl)-1-methyl-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
Homo sapiens
in 500 mM Tris-HCl, pH 7.5, 1.5 M NaCl, 50 mM CaCl2, temperature not specified in the publication
0.00014
N-(ethylsulfonyl)-5-hydroxy-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
Homo sapiens
in 500 mM Tris-HCl, pH 7.5, 1.5 M NaCl, 50 mM CaCl2, temperature not specified in the publication
0.000065
N-(ethylsulfonyl)-5-methoxy-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
Homo sapiens
in 500 mM Tris-HCl, pH 7.5, 1.5 M NaCl, 50 mM CaCl2, temperature not specified in the publication
0.000062
N-(ethylsulfonyl)-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-L-glutamamide
Homo sapiens
in 500 mM Tris-HCl, pH 7.5, 1.5 M NaCl, 50 mM CaCl2, temperature not specified in the publication
0.0002
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-(3,4,5-trifluoro-phenyl)-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 200 nM, reversible, covalent
0.0008
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-(3-trifluoromethyl-phenyl)-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 800 nM, reversible, covalent
0.00156
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-(4-iodo-phenyl)-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 0.00156 mM, reversible, covalent
0.00588
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-(4-nitro-phenyl)-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 0.00588 mM, reversible, covalent
0.00011
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-hydroxy-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 110 nM, reversible, covalent
0.00017
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-m-tolyl-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 170 nM, reversible, covalent
0.0056
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-naphthalen-1-yl-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 0.0056 mM, reversible, covalent
0.00195
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-naphthalen-2-yl-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 0.00195 mM, reversible, covalent
0.00024
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-o-tolyl-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 240 nM, reversible, covalent
0.00129
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-p-tolyl-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 0.00129 mM, reversible, covalent
0.000042
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-phenyl-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 42 nM, reversible, covalent
0.0002
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-pyridin-3-yl-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 200 nM, reversible, covalent
0.00997
N-[2-(1-benzyl-1H-imidazol-4-yl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 0.00997 mM, reversible, covalent
0.0007
N-[2-(2,6-dimethyl-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 700 nM, reversible, covalent
0.00009
N-[2-(2-fluoro-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 90 nM, reversible, covalent
0.00016
N-[2-(3,4-difluoro-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 160 nM, reversible, covalent
0.00019
N-[2-(3,5-difluoro-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 190 nM, reversible, covalent
0.00023
N-[2-(3-chloro-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 230 nM, reversible, covalent
0.0002
N-[2-(3-fluoro-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 200 nM, reversible, covalent
0.00057
N-[2-(4-acetylamino-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 570 nM, reversible, covalent
0.00076
N-[2-(4-bromo-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 760 nM, reversible, covalent
680
N-[2-(4-chloro-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 680 mM, reversible, covalent
0.00034
N-[2-(4-cyano-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 340 nM, reversible, covalent
0.00017
N-[2-(4-fluoro-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 170 nM, reversible, covalent
0.0005
N-[2-benzo[b]thiophen-3-yl-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 0.0005 mM, reversible, covalent
0.00153
N-[2-benzyloxy-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 0.00153 mM, reversible, covalent
0.00183
N-[2-biphenyl-3-yl-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 0.00183 mM, reversible, covalent
0.0178
N-[2-biphenyl-4-yl-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 0.0178 mM, reversible, covalent
0.0033
N-[2-cyclohexyl-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 0.0033 mM, reversible, covalent
0.00082
N-[2-cyclopropyl-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
Homo sapiens
-
IC50: 820 nM, reversible, covalent
0.00318
N-[4-guanidino-1-(thiazole-2-carbonyl)-butyl]-3-(3-phenyl-2-phenylmethanesulfonylamino-propionylamino)-succinamic acid cyclohexyl ester
Homo sapiens
-
IC50: 0.00318 mM, reversible, covalent
0.0137
N-[4-guanidino-1-(thiazole-2-carbonyl)-butyl]-4-methanesulfonyl-2-(3-phenyl-2-phenylmethanesulfonylamino-propionylamino)-butyramide
Homo sapiens
-
IC50: 0.0137 mM, reversible, covalent
0.0009
N-[4-guanidino-1-(thiazole-2-carbonyl)-butyl]-4-phenyl-2-(3-phenyl-2-phenylmethanesulfonylamino-propionylamino)-butyramide
Homo sapiens
-
IC50: 900 nM, reversible, covalent
0.00103
N1-[4-guanidino-1-(thiazole-2-carbonyl)-butyl]-2-(3-phenyl-2-phenylmethanesulfonylamino-propionylamino)-succinamide
Homo sapiens
-
IC50: 0.00103 mM, reversible, covalent
0.0044
SAEWEVLCWTWEGCGSVGL-(Z-domain of protein A)
Homo sapiens
-
IC50: 4400 nM
0.000093
SEEWEVLCWTWEDCRLEGLE-(Z-domain of protein A)
Homo sapiens
-
IC50: 93 nM
-
0.014
V154G-FVIIa
Homo sapiens
-
derivate of FVIIa with a fully exposed N-terminus representing the zymogen-like conformation of FVIIa, IC50: 0.014 mM
-
0.000000022
VLCWTWETCER-NH2
Homo sapiens
-
IC50: 0.022 nM
0.013
WEVLCWTWETC-NH2
Homo sapiens
-
IC50: 0.013 mM
0.007
WEVLCWTWETCE-NH2
Homo sapiens
-
IC50: 0.007 mM
0.0000025
WEVLCWTWETCER-NH2
Homo sapiens
-
IC50: 2.5 nM