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0.0004
(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
-
pH and temperature not specified in the publication
0.0000052 - 0.00003
(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
0.00000043
(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
-
at pH 7.4 and 37°C
0.00000023
(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
-
at pH 7.4 and 37°C
0.000001
(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
-
at pH 7.4 and 37°C
0.00002
(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
-
at pH 7.4 and 37°C
0.000015
(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
-
at pH 7.4 and 37°C
0.0000055
(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
-
at pH 7.4 and 37°C
0.0000022
(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
-
at pH 7.4 and 37°C
0.00000016
(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
-
at pH 7.4 and 37°C
0.0000025
(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
-
at pH 7.4 and 37°C
0.00000057
(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
-
at pH 7.4 and 37°C
0.018 - 0.054
(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
0.0000016
(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
-
pH and temperature not specified in the publication
0.000008
(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
-
pH and temperature not specified in the publication
0.000021
([5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]methyl)propanedioic acid
-
-
0.0046
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
-
pH and temperature not specified in the publication
0.000004
2-([5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-5'-fluoro-2',6-dihydroxybiphenyl-3-yl]methyl)butanedioic acid
-
-
0.0046 - 0.01
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
0.00092
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
-
pH and temperature not specified in the publication
0.0061
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
-
pH and temperature not specified in the publication
0.000004
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-5'-fluoro-2',6-dihydroxybiphenyl-3-yl]butanedioic acid
-
-
0.000022
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]butanedioic acid
-
-
0.000017
2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]pentanedioic acid
-
-
0.000001
2-[5-(5-carbamimidoyl-1H-indol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]butanedioic acid
-
-
0.000036
3-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]pentanedioic acid
-
-
0.000013
3-[5-(5-carbamimidoyl-1H-indol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]pentanedioic acid
-
-
0.0000007
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
-
pH and temperature not specified in the publication
0.0493 - 3.2
4-aminobenzamidine
0.00000061
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
-
at pH 7.4 and 37°C
0.0000002
EEWEVLCWTWETCER
-
inhibition of amidolytic activity
0.0000087
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
-
at pH 7.4 and 37°C
0.038 - 1.41
p-aminobenzamidine
0.00000035
R-4-[2-(3-aminobenzenesulfonylamino)-1-(3,5-diethoxy-2-fluorophenyl)-2-oxoethylamino]-2-hydroxy-benzamidine
-
0.00000028
[(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
-
at pH 7.4 and 37°C
0.000002
[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-5'-fluoro-2',6-dihydroxybiphenyl-3-yl]acetic acid
-
-
0.000015
[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]acetic acid
-
-
0.000003
[5-(5-carbamimidoyl-1H-indol-2-yl)-6-hydroxy-3'-nitrobiphenyl-3-yl]acetic acid
-
-
additional information
additional information
-
0.0000052
(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
-
pH and temperature not specified in the publication
0.00003
(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
-
pH and temperature not specified in the publication
0.018
(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
-
Ki above 0.018 mM, pH and temperature not specified in the publication
0.054
(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
-
pH and temperature not specified in the publication
0.0046
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
-
pH and temperature not specified in the publication
0.01
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
-
pH and temperature not specified in the publication
0.0493
4-aminobenzamidine
wild type enzyme, in the presence of soluble tissue factor (1-219), at pH 7.4 and 25°C
0.1
4-aminobenzamidine
wild-type + soluble tissue factor for induced allosteric activation of factor VIIa
0.7
4-aminobenzamidine
mutant G372 + soluble tissue factor for induced allosteric activation of factor VIIa
1.485
4-aminobenzamidine
wild type enzyme, in the absence of soluble tissue factor (1-219), at pH 7.4 and 25°C
3.2
4-aminobenzamidine
-
in 50 mM HEPES, pH 7.4, with 0.1 M NaCl, 5 mM CaCl2, 0.1% (w/v) bovine serum albumin, and 0.01% Tween 80, at 25°C
0.038
p-aminobenzamidine
-
mutant FVIIaVEAY-sTF, 210 nM
0.05
p-aminobenzamidine
-
mutant FVIIaIIa-sTF, 210 nM
0.077
p-aminobenzamidine
-
wild type FVIIa-sTF, 210 nM
0.116
p-aminobenzamidine
-
pH 8.0, wild-type enzyme, chromozym tPA as substrate with addition of tissue factor
0.124
p-aminobenzamidine
-
pH 8.0, mutant enzyme V21N/E154I/M156Q, chromozym tPA as substrate with addition of tissue factor
0.177
p-aminobenzamidine
-
mutant FVIIaVEAY, 10 nM
0.226
p-aminobenzamidine
-
mutant FVIIaIIa, 25 nM
0.317
p-aminobenzamidine
-
pH 8.0, mutant enzyme V21N/E154I/M156Q, chromozym tPA as substrate without addition of tissue factor
1.41
p-aminobenzamidine
-
wild type FVIIa, 100 nM
additional information
additional information
-
because of competitive binding of p-aminobenzamidine and D-Ile-Pro-Arg-p-nitroanilide, the apparent Ki values were calculated from the p-aminobenzamidine IC50, taking into account the concentration of D-Ile-Pro-Arg-p-nitroanilide ([S]) and the Km for this substrate using Ki =IC50/(1 + [S]/Km)
-
additional information
additional information
-
inhibition kinetics of wild-type and mutant enzymes, overview
-