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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

Inhibitors

Inhibitors on EC 3.4.21.21 - coagulation factor VIIa

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6(21),7,9,16,19-hexaene-3,12-dione
-
-
(2R)-2-[(1-aminoisoquinolin-6-yl)amino]-7-(propane-2-sulfonyl)-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6(21),7,9,16,19-hexaene-3,12-dione
-
-
(2R,15R)-2-[(1-amino-4-fluoroisoquinolin-6-yl)amino]-7-(cyclopropanesulfonyl)-4,15,17-trimethyl-13-oxa-4,11-diazatricyclo-[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione
-
highly potent, selective inhibitor
(2R,15R)-2-[(1-amino-7-fluoroisoquinolin-6-yl)amino]-7-(cyclopropanesulfonyl)-4,15,17-trimethyl-13-oxa-4,11-diazatricyclo-[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione
-
-
(2R,15R)-2-[(1-amino-8-fluoroisoquinolin-6-yl)amino]-7-(cyclopropanesulfonyl)-4,15,17- trimethyl-13-oxa-4,11-diazatricyclo-[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione
-
-
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,17-trimethyl-13-oxa-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6,8,10-(21),16,19-hexaene-3,12-dione
-
-
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,17-trimethyl-3,12-dioxo-13-oxa-4,11- diazatricyclo[14.2.2.16,10]henicosa-1-(18),6,8,10(21),16,19-hexaene-7-carboxamide
-
-
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,17-trimethyl-7-(trifluoromethoxy)-13-oxa-4,11-diazatricyclo[14.2.2.16,10]-henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione
-
-
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,20-trimethyl-7-(1-methyl-1H-pyrazol-5-yl)-13-oxa-4,11-diazatricyclo-[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione
-
-
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-7-(cyclopropanesulfonyl)-4,15,20-trimethyl-13-oxa-4,11-diazatricyclo[14.2.2.16,10]-henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione
-
-
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-N,N,4,15,17-pentamethyl-3,12-dioxo-13-oxa-4,11-diazatricyclo[14.2.2.16,10]-henicosa-1(18),6,8,10(21),16,19-hexaene-7-carboxamide
-
-
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-N,N-diethyl-4,15,17-trimethyl-3,12-dioxo-13-oxa-4,11-diazatricyclo[14.2.2.16,10]-henicosa-1(18),6,8,10(21),16,19-hexaene-7-carboxamide
-
-
(2S)-2-[(1-aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6(21),7,9,16,19-hexaene-3,12-dione
-
-
(R)-2-(1-aminoisoquinolin-6-ylamino)-7-ethanesulfonyl-20-methyl-4,11-diaza-tricyclo[14.2.2.16,10]henicosa-1(19),6,8,10-(21),16(20),17-hexaene-3,12-dione
-
-
(R)-2-(1-aminoisoquinolin-6-ylamino)-7-ethanesulfonyl-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(19),6,8,10(21),16-(20),17-hexaene-3,12-dione
-
-
([5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]methyl)propanedioic acid
-
-
2-(1-aminoisoquinolin-6-ylamino)-16-oxa-4,11-diazatricyclo-[15.2.2.16,10]docosa-1(20),6,8,10(22),17(21),18-hexaene-3,12-dione trifluoroacetic acid
-
-
2-(3'-amino-3-fluoro-4-(isopropylamino)-1,1'-biphenyl-2-yl)-N-(4-(amino(imino)methyl)benzyl)acetamide
-
IC50: 340 nM
2-(3'-amino-4-(benzylamino)-3-fluoro-1,1'-biphenyl-2-yl)-N-(4-(amino(imino)methyl)benzyl)acetamide
-
IC50: 500 nM
2-(3-allylamino-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl)-N-(4-carbamimidoyl-benzyl)-acetamide
-
pH 8.0, IC50: 700 nM
2-(3-benzylamino-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl)-N-(4-carbamimidoyl-benzyl)-acetamide
-
pH 8.0, IC50: 770 nM
2-(3-benzylsulfanyl-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl)-N-(4-carbamimidoyl-benzyl)-acetamide
-
pH 8.0, IC50: 0.0064 mM
2-(3-butylamino-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl)-N-(4-carbamimidoyl-benzyl)-acetamide
-
pH 8.0, IC50: 0.0032 mM
2-([5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-5'-fluoro-2',6-dihydroxybiphenyl-3-yl]methyl)butanedioic acid
-
-
2-[(1-aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[13.2.2.16,10]icosa-1(17),6(20),7,9,15,18-hexaene-3,12-dione
-
-
2-[(1-aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6(21),7,9,16,19-hexaene-3,12-dione
-
-
2-[(1-aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[15.2.2.16,10]docosa-1(19),6(22),7,9,17,20-hexaene-3,12-dione
-
-
2-[3-(2-amino-ethylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
-
pH 8.0, IC50: 0.0021 mM
2-[3-(3-amino-propylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
-
pH 8.0, IC50: 890 nM
2-[3-(4-amino-butylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
-
pH 8.0, IC50: 980 nM
2-[3-(4-tert-butyl-cyclohexylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
-
pH 8.0, IC50: 0.003 mM
2-[3-(adamantan-1-ylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
-
pH 8.0, IC50: 0.013 mM
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-5'-fluoro-2',6-dihydroxybiphenyl-3-yl]butanedioic acid
-
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]butanedioic acid
-
-
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]pentanedioic acid
-
-
2-[5-(5-carbamimidoyl-1H-indol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]butanedioic acid
-
-
2-[6-(3-acetylamino-phenyl)-5-chloro-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
-
pH 8.0, IC50: 0.00161 mM
2-[6-(3-amino-phenyl)-5-chloro-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
-
pH 8.0, IC50: 70 nM
2-[6-(3-amino-phenyl)-5-chloro-3-cyclobutylamino-2-oxo-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
-
pH 8.0, IC50: 20 nM
2-[6-(3-amino-phenyl)-5-chloro-3-isopropylamino-2-oxo-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
-
pH 8.0, IC50: 20 nM
2-[6-(3-bromo-phenyl)-5-chloro-3-cyclobutylamino-2-oxo-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide
-
pH 8.0, IC50: 0.0042 mM
3-(3-[(R)-2-[(S)-1-(4-carbamimidoyl-benzylcarbamoyl)-3-carbamoylpropylcarbamoyl]-2-ethanesulfonylamino-ethyl]-1H-indol-5-yloxymethyl)-benzoic acid
-
3-amino-5-(1-(1-((4-(amino(imino)methyl)benzyl)-amino)-2-oxoethyl)-5-(isopropylamino)-6-oxo-1,6-dihydropyridin-2-yl)benzoic acid
-
IC50: 118 nM
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
-
pH 8.0, IC50: 16 nM, potent and highly selective inhibitor, selectivity versus factor Xa and thrombin
3-methyl-2-(3-phenyl-2-phenylmethanesulfonylamino-propionylamino)-pentanoic acid [4-guanidino-1-(thiazole-2-carbonyl)-butyl]-amide
-
IC50: 300 nM, reversible, covalent
3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 0.00145 mM, reversible, covalent
3-[1-[(4-carbamimidoyl-benzylcarbamoyl)-methyl]-3-chloro-5-isopropylamino-6-oxo-1,6-dihydro-pyrazin-2-yl]-benzoic acid
-
pH 8.0, IC50: 360 nM
3-[1-[(4-carbamimidoyl-benzylcarbamoyl)-methyl]-3-chloro-5-isopropylamino-6-oxo-1,6-dihydro-pyrazin-2-yl]-benzoic acid methyl ester
-
pH 8.0, IC50: 780 nM
3-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]pentanedioic acid
-
-
3-[5-(5-carbamimidoyl-1H-indol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]pentanedioic acid
-
-
4,4-dimethyl-2-(3-phenyl-2-phenylmethanesulfonylamino-propionylamino)-pentanoic acid [4-guanidino-1-(thiazole-2-carbonyl)-butyl]-amide
-
IC50: 700 nM, reversible, covalent
4-((R)-7-ethanesulfonyl-3,12-dioxo-4,11-diaza-tricyclo-[14.2.2.16,10]henicosa-1(19),6,8,10(21),16(20),17-hexaen-2-ylamino)benzamidine trifluoroacetic acid
-
-
4-aminobenzamidine
4-[5-(4-fluorophenyl)-2-[4-(methylsulfonyl)phenyl]-1H-imidazol-4-yl]pyridine
-
-
5-(4-carboxybutoxy)-N-(ethylsulfonyl)-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
-
5-[(3-carboxybenzyl)oxy]-N-(ethylsulfonyl)-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
-
6-dimethylamino-2-(3-phenyl-2-phenylmethanesulfonylamino-propionylamino)-hexanoic acid [4-guanidino-1-(thiazole-2-carbonyl)-butyl]-amide
-
IC50: 0.00282 mM, reversible, covalent
acetyl-ALCDDPRVDRWYCQFVEG-NH2
i.e. E-76
active-site-inhibited factor Xa
-
80 nM: 60% inhibition
-
alpha1-proteinase inhibitor variant M358R
-
-
-
anti-gC antibody
-
20% inhibition
-
anti-TF antibody
-
40% inhibition
-
antithrombin
-
antithrombin III
-
benzamidine
-
benzamidine HCl
-
-
Bovine pancreatic trypsin inhibitor
-
mutant enzyme K192E is poorly inhibited, mutant enzyme K192Q is inhibited more than the wild-type enzyme
-
combination of the gC- and TF-specific antibodies
-
65% inhibition
-
D-Phe-Phe-Arg chloromethyl ketone
-
-
D-Phe-Phe-Arg chloromethylketone
-
D-Phe-Phe-Arg methyl ketone
-
D-Phe-Phe-Arg-chloromethyl ketone
-
-
D-prolyl-N-(4-carbamimidoylbenzyl)-L-prolinamide
-
diethyl [(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,17-trimethyl-3,12-dioxo-13-oxa-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaen-7-yl]phosphonate
-
-
diisopropylfluorophosphate
dimeric active site-inhibited blood clotting factor VIIa
-
dimeric fVIIai, 16000fold inhibitory effect
-
dimethyl (4-hydroxybenzyl)propanedioate
-
-
dimethyl 2-(4-hydroxybenzyl)butanedioate
-
-
dimethyl 2-(4-hydroxyphenyl)butanedioate
-
-
dimethyl 2-(4-hydroxyphenyl)pentanedioate
-
-
dimethyl 3-(4-hydroxyphenyl)pentanedioate
-
-
EEWEVLCWTWETCER
EEWEVLCWTWETCERGEG-(Z-domain of protein A)
-
IC50: 3.8 nM
-
EEWEVLCWTWETCERGEG-NH2
-
IC50: 1.5 nM
EEWEVLCWTWETCERGEGVEEELWEWR
-
maximal inhibition to 99%, IC50: 230 pM
EVLCWTWETCER-NH2
-
IC50: 470 nM
EWEVLCWTWETCERGE-(Z-domain of protein A)
-
IC50: 4.8 nM
-
FFR-FVIIa
-
derivate of FVIIa with a stably buried N-terminus representing the active conformation of FVIIa, IC50: 0.019 mM
-
H-D-Phe-Phe-Arg-chloromethylketone
-
hemextin A
-
0.05 mM, 70% inhibition
-
hemextin AB complex
-
IC50: 100 nM
-
MEEWEVLCWTWETCERGEGQ-(Z-domain of protein A)
-
IC50: 5.9 nM
-
methyl (2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,17-trimethyl-3,12-dioxo-13-oxa-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaene-7-carboxylate
-
-
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
-
pH 8.0, IC50: 450 nM
N-(4-(amino(imino)methyl)benzyl)-2-(2,6-difluoro-3-((2-phenylethyl)amino)phenyl)acetamide
-
IC50: 0.0164 mM
N-(4-(amino(imino)methyl)benzyl)-2-(3-fluoro-4-((2-phenylethyl)amino)-1,1'-biphenyl-2-yl)acetamide
-
IC50: 0.00398 mM
N-(4-(amino(imino)methyl)benzyl)-2-(3-hydroxy-4-((2-phenylethyl)amino)-1,1'-biphenyl-2-yl)acetamide
-
IC50: 0.0027 mM
N-(4-(amino(imino)methyl)benzyl)-2-(3-hydroxy-4-(isopropylamino)-1,1'-biphenyl-2-yl)acetamide
-
IC50: 0.0025 mM
N-(4-(amino(imino)methyl)benzyl)-2-(3-methoxy-4-((2-phenylethyl)amino)-1,1'-biphenyl-2-yl)acetamide
-
IC50: 0.025 mM
N-(4-(amino(imino)methyl)benzyl)-2-(4-(isopropylamino)-3-methoxy-1,1'-biphenyl-2-yl)acetamide
-
IC50: 0.0147 mM
N-(4-(amino(imino)methyl)benzyl)-2-(5-(isopropylamino)-3,6-dioxo-2-phenylcyclohexa-1,4-dien-1-yl)acetamide
-
IC50: 0.0028 mM
N-(4-(amino(imino)methyl)benzyl)-2-(6-(3,5-diaminophenyl)-3-(isopropylamino)-2-oxopyridin-1(2H)-yl)acetamide
-
IC50: 52 nM
N-(4-carbamimidoyl-benzyl)-2-(2-oxo-3-phenethylamino-6-phenyl-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 340 nM
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-3-phenethylamino-6-m-tolyl-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 0.001 mM
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-3-phenethylamino-6-o-tolyl-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 430 nM
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-3-phenethylamino-6-p-tolyl-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 0.00414 mM
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-3-phenethylamino-6-phenyl-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 630 nM
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-6-phenyl-3-phenylamino-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 0.0112 mM
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-6-phenyl-3-prop-2-ynylamino-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 720 nM
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-6-phenyl-3-propylamino-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 400 nM
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-6-phenyl-3-pyrrolidin-1-yl-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 0.0063 mM
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-cyclobutylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 400 nM
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-cyclohexylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 0.0014 mM
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-ethylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 400 nM
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-isopropylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 200 nM
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-methylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 700 nM
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-6-ethyl-2-oxo-3-phenethylamino-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 0.00345 mM
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-6-methyl-2-oxo-3-phenethylamino-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 0.00428 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-3-phenethylamino-6-(2-trifluoromethyl-phenyl)-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0027 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-3-phenethylamino-6-(3-trifluoromethyl-phenyl)-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0029 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-6-phenyl-3-(1-propyl-butylamino)-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0018 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-6-phenyl-3-(3-phenyl-propylamino)-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0126 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-6-phenyl-3-(3-trifluoromethyl-benzylamino)-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0063 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-6-phenyl-3-(4-phenyl-butylamino)-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0041 mM
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
-
pH 8.0, IC50: 0.001 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1-ethyl-hexylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0098 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1-ethyl-propylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 430 nM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1-methyl-butylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 840 nM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1-methyl-pentylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 900 nM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2,5-difluoro-benzylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0038 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2-dimethylamino-ethylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0209 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2-hydroxy-ethylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 500 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2-methoxy-ethylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 880 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2-morpholin-4-yl-ethylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.008 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(3,5-difluoro-benzylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.006 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(3-dimethylamino-propylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0176 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(3-hydroxy-propylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 500 nM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(4-chloro-benzylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0043 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(4-hydroxy-butylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 600 nM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(6-hydroxy-hexylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 470 nM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(isopropyl-methyl-amino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0091 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-cyclobutylamino-6-(2-hydroxy-phenyl)-2-oxo-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 340 nM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-cyclobutylamino-6-(3-hydroxy-phenyl)-2-oxo-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 200 nM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(2-chloro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.003 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(2-fluoro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0018 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(2-methoxy-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0016 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-chloro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.00198 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-dimethylamino-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0012 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-fluoro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0023 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-methanesulfonylamino-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 600 nM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-methoxy-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0052 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-methylamino-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 600 nM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-nitro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.00252 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(4-chloro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.00888 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(4-fluoro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.0081 mM
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(4-methoxy-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide
-
pH 8.0, IC50: 0.02345 mM
N-(4-carbamimidoyl-benzyl)-2-{5-chloro-2-oxo-6-phenyl-3-[2-(3-trifluoromethyl-phenyl)-ethylamino]-2H-pyrazin-1-yl}-acetamide
-
pH 8.0, IC50: 0.03 mM
N-(4-carbamimidoyl-benzyl)-2-{5-chloro-3-[2-(3-chloro-phenyl)-ethylamino]-2-oxo-6-phenyl-2H-pyrazin-1-yl}-acetamide
-
pH 8.0, IC50: 180 nM
N-(4-carbamimidoyl-benzyl)-2-{5-chloro-3-[2-(4-chloro-phenyl)-ethylamino]-2-oxo-6-phenyl-2H-pyrazin-1-yl}-acetamide
-
pH 8.0, IC50: 600 nM
N-(5-carbamimidoyl-pyridin-2-ylmethyl)-2-(2-oxo-3-phenethylamino-6-phenyl-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 0.0167 mM
N-(6-carbamimidoyl-pyridin-3-ylmethyl)-2-(2-oxo-3-phenethylamino-6-phenyl-2H-pyrazin-1-yl)-acetamide
-
pH 8.0, IC50: 0.0014 mM
N-(ethylsulfonyl)-1-methyl-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
-
N-(ethylsulfonyl)-5-hydroxy-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
-
N-(ethylsulfonyl)-5-methoxy-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
-
N-(ethylsulfonyl)-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-L-glutamamide
-
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-(3,4,5-trifluoro-phenyl)-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 200 nM, reversible, covalent
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-(3-trifluoromethyl-phenyl)-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 800 nM, reversible, covalent
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-(4-iodo-phenyl)-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 0.00156 mM, reversible, covalent
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-(4-nitro-phenyl)-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 0.00588 mM, reversible, covalent
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-hydroxy-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 110 nM, reversible, covalent
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-m-tolyl-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 170 nM, reversible, covalent
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-naphthalen-1-yl-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 0.0056 mM, reversible, covalent
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-naphthalen-2-yl-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 0.00195 mM, reversible, covalent
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-o-tolyl-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 240 nM, reversible, covalent
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-p-tolyl-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 0.00129 mM, reversible, covalent
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-phenyl-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 42 nM, reversible, covalent
N-[1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-2-pyridin-3-yl-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 200 nM, reversible, covalent
N-[2-(1-benzyl-1H-imidazol-4-yl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 0.00997 mM, reversible, covalent
N-[2-(2,6-dimethyl-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 700 nM, reversible, covalent
N-[2-(2-fluoro-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 90 nM, reversible, covalent
N-[2-(3,4-difluoro-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 160 nM, reversible, covalent
N-[2-(3,5-difluoro-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 190 nM, reversible, covalent
N-[2-(3-chloro-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 230 nM, reversible, covalent
N-[2-(3-fluoro-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 200 nM, reversible, covalent
N-[2-(4-acetylamino-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 570 nM, reversible, covalent
N-[2-(4-bromo-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 760 nM, reversible, covalent
N-[2-(4-chloro-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 680 mM, reversible, covalent
N-[2-(4-cyano-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 340 nM, reversible, covalent
N-[2-(4-fluoro-phenyl)-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 170 nM, reversible, covalent
N-[2-benzo[b]thiophen-3-yl-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 0.0005 mM, reversible, covalent
N-[2-benzyloxy-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 0.00153 mM, reversible, covalent
N-[2-biphenyl-3-yl-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 0.00183 mM, reversible, covalent
N-[2-biphenyl-4-yl-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 0.0178 mM, reversible, covalent
N-[2-cyclohexyl-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 0.0033 mM, reversible, covalent
N-[2-cyclopropyl-1-[4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl]-3-phenyl-2-phenylmethanesulfonylamino-propionamide
-
IC50: 820 nM, reversible, covalent
N-[3-[(2R)-1-[(2R)-2-[(1-aminoisoquinolin-6-yl)amino]-2-phenylacetyl]pyrrolidin-2-yl]-4-(propane-2-sulfonyl)phenyl]acetamide
-
-
N-[4-guanidino-1-(thiazole-2-carbonyl)-butyl]-3-(3-phenyl-2-phenylmethanesulfonylamino-propionylamino)-succinamic acid cyclohexyl ester
-
IC50: 0.00318 mM, reversible, covalent
N-[4-guanidino-1-(thiazole-2-carbonyl)-butyl]-4-methanesulfonyl-2-(3-phenyl-2-phenylmethanesulfonylamino-propionylamino)-butyramide
-
IC50: 0.0137 mM, reversible, covalent
N-[4-guanidino-1-(thiazole-2-carbonyl)-butyl]-4-phenyl-2-(3-phenyl-2-phenylmethanesulfonylamino-propionylamino)-butyramide
-
IC50: 900 nM, reversible, covalent
N1-[4-guanidino-1-(thiazole-2-carbonyl)-butyl]-2-(3-phenyl-2-phenylmethanesulfonylamino-propionylamino)-succinamide
-
IC50: 0.00103 mM, reversible, covalent
p-aminobenzamidine
-
-
R-4-[2-(3-aminobenzenesulfonylamino)-1-(3,5-diethoxy-2-fluorophenyl)-2-oxoethylamino]-2-hydroxy-benzamidine
incubation with enzyme in 100 mM Hepes, pH 7.8, 140 mM NaCl, 0.1% (v/v) polyethylene glycol 8000, 0.02% (v/v) Tween 80, 5 mM CaCl2 for 40 min at room temperature
SAEWEVLCWTWEGCGSVGL-(Z-domain of protein A)
-
IC50: 4400 nM
SEEWEVLCWTWEDCRLEGLE-(Z-domain of protein A)
-
IC50: 93 nM
-
tissue factor pathway inhibitor
-
Trp-Tyr-Thr-Arg-chloromethyl ketone
-
-
V154G-FVIIa
-
derivate of FVIIa with a fully exposed N-terminus representing the zymogen-like conformation of FVIIa, IC50: 0.014 mM
-
VLCWTWETCER-NH2
-
IC50: 0.022 nM
WEVLCWTWETC-NH2
-
IC50: 0.013 mM
WEVLCWTWETCE-NH2
-
IC50: 0.007 mM
WEVLCWTWETCER-NH2
-
IC50: 2.5 nM
Zn2+
-
two Zn2+ bind with high affinity to factor VIIa outside the N-terminal gamma-carboxyglutamic acid domain. Binding of Zn2+ is influenced by presence of Ca2+ and results in decreased amidolytic activity and slightly reduced affinity for tissue factor. After binding to tissue factor, factor VIIa is less susceptible to zinc inhibition
[(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,20-trimethyl-3,12-dioxo-13-oxa-4,11-diazatricyclo[14.2.2.16,10]henicosa-1-(18),6,8,10(21),16,19-hexaen-7-yl](ethoxy)phosphinic acid
-
-
[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-5'-fluoro-2',6-dihydroxybiphenyl-3-yl]acetic acid
-
-
[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]acetic acid
-
-
[5-(5-carbamimidoyl-1H-indol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]acetic acid
-
-