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amyloid beta-protein + H2O
?
-
cleaves cell adhesion RHDS sequence
-
?
benzyloxycarbonyl-Gly-Pro-4-nitroanilide + H2O
benzyloxycarbonyl-Gly-Pro + 4-nitroaniline
-
-
-
?
benzyloxycarbonyl-Gly-Pro-p-nitroanilide
benzyloxycarbonyl-Gly-Pro + p-nitroaniline
-
-
-
?
beta-2-glycoprotein I + H2O
clipped beta-2-glycoprotein I
-
cleavage at Lys317-Thr318
-
?
Boc-Glu(OBzl)-Ala-Arg-4-methylcoumaryl-7-amide + H2O
Boc-Glu(OBzl)-Ala-Arg + 7-amino-4-methylcoumarin
-
-
?
D-Ile-Pro-Arg-4-nitroanilide + H2O
D-Ile-Pro-Arg + 4-nitroaniline
substrate S-2288
-
?
D-LPRANSNH-C3H7 + H2O
D-LPR + ANSNH-C3H7
-
-
-
?
factor fIX + H2O
?
-
factor IX
-
?
factor IX + H2O
activated factor IX
factor IX + H2O
activated factor IX + ?
factor IX + H2O
factor IXa
factor IX + H2O
factor IXa + ?
factor IX + H2O
factor IXa + peptide
factor IX 10-mer + H2O
?
-
-
-
?
factor IX mutant G317E + H2O
?
-
-
-
?
factor IX mutant G317R + H2O
?
-
-
-
?
factor V + H2O
activated factor V + ?
-
fXIa cleaves COOH-terminal to R306, possibly at the fXa/plasmin cleavage site R348
-
?
factor VIII + H2O
activated factor VIII + ?
-
fXIa initially cleaves at R740 and R372 in the heavy chain and also makes several A3 cleavages most notably at R1652 and R1721
-
?
factor XI + H2O
activated factor XI + ?
-
-
-
?
Fibrinogen + H2O
?
-
Aalpha-chain and Bbeta-chain, gamma-chain after prolonged incubation
-
?
Gly-Gly-L-Arg-7-amido-4-methylcoumarin + H2O
Gly-Gly-L-Arg + 7-amino-4-methylcoumarin
-
-
-
?
L-Glu-L-Glu-L-Pro-L-Arg-4-nitroanilide + H2O
L-Glu-L-Glu-L-Pro-L-Arg + 4-nitroaniline
-
S-2366
-
?
L-pyro-Glu-Pro-Arg-4-nitroanilide + H2O
L-pyro-Glu-Pro-Arg + 4-nitroaniline
i.e. S-2366
-
?
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide + H2O
L-pyroGlu-L-Pro-L-Arg + 4-nitroaniline
-
-
-
?
L-pyroglutamyl-L-Pro-L-Arg-4-nitroanilide + H2O
L-pyroglutamyl-L-Pro-L-Arg + 4-nitroaniline
-
-
-
?
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide + H2O
L-pyroglutamyl-L-prolyl-L-arginine + p-nitroaniline
-
-
?
L-pyroglutamyl-L-prolyl-L-arginyl-7-amido-4-methylcoumarin + H2O
L-pyroglutamyl-L-prolyl-L-arginine + 7-amino-4-methylcoumarin
-
-
-
?
L-pyroglutamyl-L-prolyl-L-arginyl-p-nitroanilide + H2O
L-pyroglutamyl-L-prolyl-L-arginine + p-nitroaniline
methyl-sulfonyl-D-cyclo-hexyl-glycyl-glycyl-arginine-p-nitroanilide + H2O
?
-
substrate S-299
-
?
methyl-sulfonyl-D-cyclo-hexyl-glycyl-glycyl-arginine-p-nitroanilide + H2O
methyl-sulfonyl-D-cyclo-hexyl-glycyl-glycyl-arginine + p-nitroaniline
-
-
-
?
N-benzoyl-L-arginine-p-nitroanilide + H2O
N-benzoyl-L-arginine + p-nitroaniline
-
-
-
?
N-Cbz-D-arginylglycyl-L-arginyl-4-nitroanilide + H2O
N-Cbz-D-arginylglycyl-L-arginine + 4-nitroaniline
-
-
-
?
pefachrome Xa + H2O
?
-
-
?
platelet glycoprotein 1balpha + H2O
?
binding to the A3 domain of FXI
-
?
prochemerin + H2O
chemerin + ?
-
-
-
?
prochemerin chem163S + H2O
chemerin chem162R + chermerin chem158K
-
prochemerin is activated by a series of C-terminal proteolytic cleavages resulting in diverse chemerin forms with different levels of activity
-
?
proteinase-activated receptor 1E + H2O
?
-
-
-
?
pyroGlu-Pro-Arg-4-nitroanilide + H2O
?
pyroGlu-Pro-Arg-p-nitroanilide + H2O
?
-
-
-
?
pyroglutamoyl-prolyl-arginyl-4-methylcoumarin 7-amide + H2O
?
-
-
?
S2366 + H2O
L-pyroGlu-L-Pro-L-Arg + 4-nitroaniline
-
-
-
?
SN-13a + H2O
?
-
specific substrate for factor XIa
-
?
tert-butoxycarbonyl-Glu(O-benzyl)-Ala-Arg-7-amido-4-methylcoumarin + H2O
tert-butoxycarbonyl-Glu(O-benzyl)-Ala-Arg + 7-amino-4-methylcoumarin
-
-
-
?
tissue factor pathway inhibitor + H2O
?
-
the cleavage of the protein occurs between the Kunitz (K)1 and K2 domains (Lys86/Thr87) and at the active sites of the K2 (Arg107/Gly108) and K3 (Arg199/Ala200) domains
-
?
Z-Gly-Gly-Arg-7-amido-4-methylcoumarin + H2O
Z-Gly-Gly-Arg + 7-amino-4-methylcoumarin
-
-
?
additional information
?
-
factor IX + H2O

?
-
activation of Factor IX in the intrinsic coagulation cascade
-
?
factor IX + H2O
?
-
activation of Factor IX in the intrinsic coagulation cascade
-
?
factor IX + H2O

activated factor IX
-
-
-
?
factor IX + H2O
activated factor IX
-
-
-
?
factor IX + H2O

activated factor IX + ?
-
-
-
?
factor IX + H2O
activated factor IX + ?
-
-
?
factor IX + H2O
activated factor IX + ?
-
model for factor IX activation in which FXIa binds to activated platelets by one chain of the dimer, while binding to factor IX through the other
-
?
factor IX + H2O
activated factor IX + ?
factor XIa has a role in the intrinsic pathway of coagulation, and plays a significant role in venous thrombosis
-
?
factor IX + H2O
activated factor IX + ?
-
factor XIa is essential for the optimal activation of FIX
-
?
factor IX + H2O
activated factor IX + ?
-
two forms of activated factor XI are generated during coagulation, and each half of a factor XIa dimer behaves as an independent enzyme with respect to factor IX
-
?
factor IX + H2O
activated factor IX + ?
cleavage at Ala145 and Ala180
-
?
factor IX + H2O
activated factor IX + ?
-
cleavage at Ala145 and Ala180, activity of wild-type and mutant enzymes with wild-type and mutant substrate, overview
-
?
factor IX + H2O
activated factor IX + ?
-
cleavage of Arg145-Ala146, and Arg180-Val181, macromolecular substrate-binding exosites on both the heavy and light chains of factor XIa mediate the formation of the Michaelis complex required for factor IX-activation, mechanisms of activation, overview
-
?
factor IX + H2O
activated factor IX + ?
natural cleavage sites on FIX performed by FXIa, overview
-
?
factor IX + H2O
activated factor IX + ?
FXI is converted to the active protease by cleavage of the Arg369-Ile370 bond on each subunit. This converts the catalytic domains to the active forms, and unmasks exosites on the apple domains required for FIX binding
-
?
factor IX + H2O
activated factor IX + ?
-
-
-
?
factor IX + H2O

factor IXa
-
-
-
?
factor IX + H2O
factor IXa
-
FIX
-
?
factor IX + H2O

factor IXa + ?
-
-
-
?
factor IX + H2O
factor IXa + ?
-
-
?
factor IX + H2O
factor IXa + ?
-
after binding to factor XIa, factor IX undergoes a single cleavage to form the intermediate factor IXalpha. FIXalpha then rebinds to the A3 domain to undergo a second cleavage, generating factor IXalphabeta
-
?
factor IX + H2O

factor IXa + peptide
-
-
-
?
factor IX + H2O
factor IXa + peptide
-
-
containing 50% carbohydrate
?
factor IX + H2O
factor IXa + peptide
-
-
-
?
factor IX + H2O
factor IXa + peptide
-
-
-
?
kininogen + H2O

?
-
-
-
?
kininogen + H2O
?
binding to the A2 domain of FXI
-
?
L-pyroglutamyl-L-prolyl-L-arginyl-p-nitroanilide + H2O

L-pyroglutamyl-L-prolyl-L-arginine + p-nitroaniline
-
-
-
?
L-pyroglutamyl-L-prolyl-L-arginyl-p-nitroanilide + H2O
L-pyroglutamyl-L-prolyl-L-arginine + p-nitroaniline
-
-
?
pro-HGF + H2O

?
-
HGF i. e. hepatocyte growth factor, pro-HGF is processed by cleavage at two sites: Arg494-Val 495 and Arg424-His425. Cleavage at Arg424-His425 is independent of a prior cleavage at the primary kinetically preferred Arg 494-Val495 site. The mutant substrate pro-HGF(R424A/R494E) is completely resistant to cleavage
-
?
pro-HGF + H2O
?
-
the enzyme may regulate processes that involve the HGF/c-Met pathway, such as tissue repair and angiogenesis
-
?
pyroGlu-Pro-Arg-4-nitroanilide + H2O

?
-
substrate S-2366
-
?
pyroGlu-Pro-Arg-4-nitroanilide + H2O
?
substrate S-2366
-
?
S-2366 + H2O

?
-
commercial chromogenic substrate
-
?
S-2366 + H2O
?
commercial chromogenic substrate
-
?
S-2366 + H2O
?
-
i.e. L-pyroglutamyl-L-prolyl-L-arginine-4-nitroanilide
-
?
additional information

?
-
-
not: fibrin
-
?
additional information
?
-
-
specific and saturable zinc-dependent FXIa binding is demonstrated to 250 sites per activated platelet and 6.5 sites per umbilical vein endothelial cell. No binding to HEK293 cells is detected
-
?
additional information
?
-
a conformational transition accompanies conversion of factor XI to factor XIa that conceals the Apple 3 domain zymogen factor XI platelet binding site and exposes the factor XIa platelet binding site within the catalytic domain possibly comprising residues Cys527-Cys542
-
?
additional information
?
-
beta-branching of the side chain of residue 193 is deleterious for interactions with 4-aminobenzamidine, diisopropylfluorphosphate, and amidolytic substrates, situations where no S2'-P2' interactions are involved, overview
-
?
additional information
?
-
FXI contains 4 apple domains that form a disk structure with extensive interfaces at the base of the catalytic domain. Binding of FXI to platelets requires residues in the FXI A3 domain. Platelets bind and spread on glass coated with FXI
-
?
additional information
?
-
FXI is a homodimer, with each subunit containing four apple domains and a protease domain: the apple domains form a disk structure with binding sites for platelets
-
?
additional information
?
-
-
platelets bind and spread on glass coated with FXI. Platelets from ApoER2-deficient mice do not bind FXI
-
?
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(2,4-dibromo-3-[[(4-carbamimidamidobutyl)carbamoyl]oxy]-6-hydroxyphenyl)acetic acid
-
(2,4-dibromo-6-[[(4-carbamimidamidobutyl)carbamoyl]oxy]-3-hydroxyphenyl)acetic acid
-
(2E)-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-1H-imidazol-2-yl]-2-phenylethyl]-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enamide
-
-
(2E)-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enamide
-
-
(2S)-2-([[(1R)-1-(4-bromophenyl)ethyl]carbamoyl]amino)-N-[(2S)-1-[[(2S)-5-carbamimidamido-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-2-(4-hydroxyphenyl)ethanamide
-
(2S)-2-([[(1R)-1-(4-bromophenyl)ethyl]carbamoyl]amino)-N-[(2S)-1-[[(2S)-5-carbamimidamido-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-2-(pyridin-3-yl)ethanamide
-
(3R)-3-(4-bromophenyl)-N-[(1S)-2-[[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]amino]-1-cyclohexyl-2-oxoethyl]butanamide
-
(3R)-N-[(1S)-2-[[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]amino]-2-oxo-1-(pyridin-3-ylmethyl)ethyl]-3-(4-fluorophenyl)butanamide
-
(3S)-3-(4-bromophenyl)-N-[(1S)-2-[[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]amino]-1-cyclohexyl-2-oxoethyl]butanamide
-
(3S)-N-[(1S)-2-[[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]amino]-2-oxo-1-(pyridin-3-ylmethyl)ethyl]-3-(4-fluorophenyl)butanamide
-
(4S,7S)-18-chloro-7-cyclohexyl-4-(2-methylpropyl)-1,2,4,5,7,8,10,11,12,13,14,15-dodecahydro[1,2,5,8]thiatriazacyclohexadecino[11,10-b]indole-3,6-dione 9,9-dioxide
-
-
(4S,7S,10S,12Z)-18-chloro-7-cyclohexyl-4-(2-methylpropyl)-10-phenyl-4,5,7,8,10,11,14,15-octahydro-1H-[1,4,7]triazacyclohexadecino[10,9-b]indole-3,6,9(2H)-trione
-
-
(4S,7S,12Z)-18-chloro-7-cyclohexyl-4-(2-methylpropyl)-1,2,4,5,7,8,10,11,14,15-decahydro[1,2,5,8]thiatriazacyclohexadecino[11,10-b]indole-3,6-dione 9,9-dioxide
-
-
(S)-2-(3-(3,4-dichlorobenzyl)ureido)-N-((2S,3S)-1-((S)-5-guanidino-1-oxo-1-(thiazol-2-yl)pentan-2-ylamino)-3-methyl-1-oxopentan-2-yl)-4-methylpentanamide
-
1-amino-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-5,6,7,8-tetrahydroisoquinoline-6-carboxamide
-
-
1-amino-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]isoquinoline-6-carboxamide
-
-
1-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-(3-chloro-2,6-difluorobenzyl)urea
-
-
1-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-(3-chloro-2-fluorobenzyl)urea
-
-
1-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-(3-chlorobenzyl)urea
-
-
1-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-(5-chloro-2-fluorobenzyl)urea
-
-
1-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-(5-chloro-2-methoxybenzyl)urea
-
-
1-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-(5-chloro-2-methylbenzyl)urea
-
-
1-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-[2-(aminomethyl)-5-chlorobenzyl]urea
-
-
1-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-[5-chloro-2-(trifluoromethyl)benzyl]urea
-
-
1-[2-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]ethyl]guanidine
-
-
1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl]guanidine
-
-
1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]guanidine
-
-
2'-[(6-carbamimidoyl-1-ethyl-1H-indol-3-yl)methyl]-4-methyl-5'-[[(5-methylpyrazin-2-yl)methyl]carbamoyl]biphenyl-2-carboxylic acid
-
2,4-dibromo-3-([(4-carbamimidamidobutyl) carbamoyl]oxy)-6-hydroxyphenyl acetic acid
clavatadine A
2-(2-amino-2-oxoethyl)-3,5-dibromo-4-hydroxyphenyl (4-carbamimidamidobutyl)carbamate
clavatadine B
2-(3-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)phenyl)acetic acid
-
2-(4-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)phenyl)acetic acid
-
2-(N2-[[(1R)-1-(4-bromophenyl)ethyl]carbamoyl]-L-arginyl-L-valyl-L-arginyl)-1,3-thiazole
-
2-(N2-[[(1R)-1-(4-bromophenyl)ethyl]carbamoyl]-N5-carbamoyl-L-ornithyl-L-valyl-L-arginyl)-1,3-thiazole
-
2-carbamimidamido-1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]ethyl pyridine-3-carboxylate
3'-[(2S,4R)-6-carbamimidoyl-4-methyl-4-phenyl-1,2,3,4-tetrahydroquinolin-2-yl]-4-carbamoyl-5'-[(3-methylbutanoyl)amino]biphenyl-2-carboxylic acid
-
3-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)benzamide
-
3-(ethoxycarbonyl)-2-([[3-(ethoxycarbonyl)-2-([[3-(ethoxycarbonyl)-2-([[3-(ethoxycarbonyl)-6-methoxy-2-methyl-1-benzofuran-5-yl]oxy]methyl)-6-methoxy-1-benzofuran-5-yl]oxy]methyl)-6-methoxy-1-benzofuran-5-yl]oxy]methyl)-6-methoxy-1-benzofuran-5-yl sulfate
-
-
3-alkoxy-4-chloro-7-guanidinoisocoumarin
-
-
3-amino-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-1,2-benzoxazole-6-carboxamide
-
-
3-amino-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-1H-indazole-6-carboxamide
-
-
3-[(N-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-L-phenylalanyl)amino]benzoic acid
-
-
3-[[N-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-3-(pyridin-3-yl)-L-alanyl]amino]benzoic acid
-
-
3-[[N2-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-N-(pyrazin-2-ylmethyl)-L-asparaginyl]amino]benzoic acid
-
-
4-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)-N,N-dimethylbenzamide
-
4-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)-N-methylbenzamide
-
4-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)benzamide
-
4-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-5-bromo-1H-imidazol-4-yl)-benzamide
-
4-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-5-chloro-1H-imidazol-4-yl)-benzamide
-
4-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-5-fluoro-1H-imidazol-4-yl)-benzamide
-
4-(2-(S-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)benzoic acid
-
4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline
-
-
4-amidinophenylmethanesulfonyl fluoride
-
-
4-chloro-3-isothiureidoalkoxyisocoumarin
-
-
4-[(N-[(2E)-3-[2-(aminomethyl)-5-chlorophenyl]prop-2-enoyl]-L-phenylalanyl)amino]benzoic acid
-
-
4-[(N-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-L-phenylalanyl)amino]benzoic acid
-
-
4-[(N-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-L-tryptophyl)amino]benzoic acid
-
-
4-[(N2-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-N-[2-(morpholin-4-yl)ethyl]-L-asparaginyl)amino]benzoic acid
-
-
4-[[(2S)-2-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-4-(methylsulfonyl)butanoyl]amino]benzoic acid
-
-
4-[[N-[(2E)-3-[3-chloro-2-fluoro-6-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-3-(1-ethyl-5-methyl-1H-pyrazol-3-yl)-L-alanyl]amino]benzoic acid
-
-
4-[[N-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-3-(thiophen-2-yl)-L-alanyl]amino]benzoic acid
-
-
5-[(N-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-L-phenylalanyl)amino]thiophene-2-carboxylic acid
-
-
5-[[3-(ethoxycarbonyl)-5-hydroxy-6-methoxy-1-benzofuran-2-yl]methoxy]-6-methoxy-2-methyl-1-benzofuran-3-carboxylic acid
-
-
alpha1-protease inhibitor
-
-
amyloid beta-precursor protein Kunitz domain
beta-branching of the side chain of residue 193 is deleterious for interactions with 4-aminobenzamidine, diisopropylfluorphosphate, and amidolytic substrates, situations where no S2'-P2' interactions are involved, beta-branching causes steric conflicts with the FXIa 140-loop, overview
-
basic pancreatic trypsin inhibitor
competitive inhibition
-
basic pancreatic trypsin inhibitor mutant K15R
-
-
D-Phe-Pro-Arg-CH2Cl
-
irreversibly inhibits both active sites of the enzyme
decasodium 1,2,3,4,6-pentakis-O-[3,5-bis(sulfonatooxy)benzoyl]-beta-D-threo-hexopyranose
-
complete inhibition at 1 mg/ml
decasodium 1,2,3,4,6-pentakis-O-[4-hydroxy-3,5-bis(sulfonatooxy)benzoyl]-beta-D-threo-hexopyranose
-
complete inhibition at 0.2 mg/ml
dextran sulfate M 10000
-
51% saturable maximal inhibition at 37°C
-
dextran sulfate M 500000
-
86% saturable maximal inhibition at 37°
-
diisopropyl fluorophosphate
-
-
diisopropylfluorphosphate
beta-branching of the side chain of residue 193 is deleterious for interactions with 4-aminobenzamidine, diisopropylfluorphosphate, and amidolytic substrates, situations where no S2'-P2' interactions are involved, beta-branching causes steric conflicts with the FXIa 140-loop, overview
disodium 3-([[3,5-dicyano-6-nitro-4-(4-phenoxyphenyl)pyridin-2-yl]sulfanyl]acetyl)benzene-1,2-diyl disulfate
-
-
disodium 4-[[3-(1,3-dioxo-5-[[4-(sulfonatooxy)phenyl]carbamoyl]-1,3-dihydro-2H-isoindol-2-yl)benzoyl]amino]phenyl sulfate
-
-
ethyl 2-(3-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)phenyl)-acetate
-
ethyl 2-(4-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)phenyl)-acetate
-
ethyl 7-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-14-[(methoxycarbonyl)amino]-10-methyl-1,2,3,4,5,6,7,9-octahydro-11,8-(azeno)-1,9-benzodiazacyclotridecine-2-carboxylate
-
-
ethyl 7-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-15-[(methoxycarbonyl)amino]-2,3,4,5,6,7-hexahydro-1H-8,12-(metheno)-1,9-benzodiazacyclotetradecine-2-carboxylate
-
-
ethyl N-[[(3S,6S,9S)-14-amino-3-benzyl-14-imino-6-(1-methylethyl)-4,7-dioxo-9-(1,3-thiazol-2-ylcarbonyl)-2,5,8,13-tetraazatetradec-1-yl]carbamoyl]leucinate
-
ethyl N-[[(3S,6S,9S)-14-amino-3-benzyl-14-imino-6-(1-methylethyl)-4,7-dioxo-9-(1,3-thiazol-2-ylcarbonyl)-2,5,8,13-tetraazatetradec-1-yl]carbamoyl]phenylalaninate
-
ethyl [(4E)-7-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-14-[(methoxycarbonyl)amino]-1,6,7,9-tetrahydro-11,8-(azeno)-2,9-benzodiazacyclotridecin-2(3H)-yl]acetate
-
-
factor fIXai
-
factor IXai
-
fractionated heparin of 64 disaccharide units
-
70-80% saturable maximal inhibition at 37°C
-
hypersulfated heparin
-
54% saturable maximal inhibition at 37°C
-
methyl (4-[2-[(1S)-1-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-2-phenylethyl]-1H-imidazol-4-yl]phenyl)carbamate
-
-
methyl (4-[2-[(benzyl[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)methyl]-5-chloro-1H-imidazol-4-yl]phenyl)carbamate
-
-
methyl (4-[5-chloro-2-[(1S)-1-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-2-phenylethyl]-1H-imidazol-4-yl]phenyl)carbamate
-
-
methyl (4-[5-chloro-2-[(1S)-1-([3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]propanoyl]amino)-2-phenylethyl]-1H-imidazol-4-yl]phenyl)carbamate
-
-
methyl (4-[5-chloro-2-[(1S)-1-([N-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]glycyl]amino)-2-phenylethyl]-1H-imidazol-4-yl]phenyl)carbamate
-
-
methyl (4-[[N-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-3-(1-methyl-1H-pyrazol-3-yl)-L-alanyl]amino]phenyl)carbamate
-
-
methyl 2-[(N-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-L-phenylalanyl)amino][1,2,4]triazolo[1,5-a]pyridine-6-carboxylate
-
-
methyl 4-(2-((S)-1-(trans-4-(aminomethyl)-cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)-benzoate
-
methyl 7-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-14-[(methoxycarbonyl)amino]-1,2,3,4,5,6,7,9-octahydro-11,8-(azeno)-1,9-benzodiazacyclotridecine-2-carboxylate
-
-
methyl [(10S)-10-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-3-oxo-1,2,3,9,10,12-hexahydro-14,11-(azeno)-8,4-(metheno)-2,12-benzodiazacyclohexadecin-17-yl]carbamate
-
-
methyl [(10S)-13-chloro-10-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-3-oxo-1,2,3,9,10,12-hexahydro-14,11-(azeno)-8,4-(metheno)-2,12-benzodiazacyclohexadecin-17-yl]carbamate
-
-
methyl [(11S)-11-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-2-oxo-1,3,4,10,11,13-hexahydro-2H-15,12-(azeno)-5,9-(metheno)-1,13-benzodiazacycloheptadecin-18-yl]carbamate
-
-
methyl [(11S)-11-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-2-oxo-1,3,4,10,11,13-hexahydro-2H-5,9:15,12-di(azeno)-1,13-benzodiazacycloheptadecin-18-yl]carbamate
-
-
methyl [(11S)-11-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-6-fluoro-2-oxo-1,3,4,10,11,13-hexahydro-2H-15,12-(azeno)-5,9-(metheno)-1,13-benzodiazacycloheptadecin-18-yl]carbamate
-
-
methyl [(11S)-11-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-6-fluoro-2-oxo-1,3,4,10,11,13-hexahydro-2H-5,9:15,12-di(azeno)-1,13-benzodiazacycloheptadecin-18-yl]carbamate
-
-
methyl [(4E)-7-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-10-methyl-2,3,6,7-tetrahydro-9H-11,8-(azeno)-1,9-benzoxazacyclotridecin-14-yl]carbamate
-
-
methyl [(4E)-7-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-10-methyl-2-oxo-2,3,6,7-tetrahydro-1H-8,12-(metheno)-1,9,11-benzotriazacyclotetradecin-15-yl]carbamate
-
-
methyl [(4E)-7-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-2,2-dioxido-1,6,7,9-tetrahydro-3H-11,8-(azeno)-2,1,9-benzothiadiazacyclotridecin-14-yl]carbamate
-
-
methyl [(5S)-2-chloro-5-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-5,6,12,13,14,15-hexahydro-3H-1,4-(azeno)-7,11-(metheno)-3-benzazacycloheptadecin-17-yl]carbamate
-
-
methyl [(5S)-5-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-5,6,11,12,13,14-hexahydro-3H-1,4-(azeno)-7,10-etheno-3-benzazacyclohexadecin-16-yl]carbamate
-
-
methyl [(7E)-5-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-3,5,6,9,10,11-hexahydro-1,4-(azeno)-3-benzazacyclotridecin-13-yl]carbamate
-
-
methyl [(9S)-12-chloro-9-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-3-oxo-1,2,3,8,9,11-hexahydro-13,10-(azeno)-4,7-etheno-2,11-benzodiazacyclopentadecin-16-yl]carbamate
-
-
methyl [(9S)-9-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-3-oxo-1,2,3,8,9,11-hexahydro-13,10-(azeno)-4,7-etheno-2,11-benzodiazacyclopentadecin-16-yl]carbamate
-
-
methyl [1-(N-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-L-phenylalanyl)-1,2,3,4-tetrahydroquinolin-6-yl]carbamate
-
-
methyl [10-chloro-7-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-2-(trifluoromethyl)-1,2,3,4,5,6,7,9-octahydro-11,8-(azeno)-1,9-benzodiazacyclotridecin-14-yl]carbamate
-
-
methyl [2-(4-chloro-1-methyl-1H-pyrazol-3-yl)-7-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-10-methyl-1,2,3,4,5,6,7,9-octahydro-11,8-(azeno)-1,9-benzodiazacyclotridecin-14-yl]carbamate
-
-
methyl [7-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-2-(3-methyloxetan-3-yl)-1,2,3,4,5,6,7,9-octahydro-11,8-(azeno)-1,9-benzodiazacyclotridecin-14-yl]carbamate
-
-
methyl [7-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-2-oxo-1,2,3,4,5,6,7,9-octahydro-11,8-(azeno)-1,9-benzodiazacyclotridecin-14-yl]carbamate
-
-
methyl [7-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-3,3-difluoro-4-oxo-1,2,3,4,5,6,7,9-octahydro-11,8-(azeno)-1,5,9-benzotriazacyclotridecin-14-yl]carbamate
-
-
N-(3-amino-1H-indol-6-yl)-Nalpha-([[5-chloro-2-(1H-tetrazol-1-yl)phenyl]sulfinyl]acetyl)-L-phenylalaninamide
-
-
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-1-(3-aminopropyl)cyclohexanecarboxamide
-
-
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-2,6-difluoro-4-methoxybenzamide
-
-
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-2-fluoro-4-methoxybenzamide
-
-
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-2-fluoro-4-methylbenzamide
-
-
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-4-(aminomethyl)-2-fluorobenzamide
-
-
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-4-(aminomethyl)benzamide
-
-
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-4-methylbenzamide
-
-
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-5-chloro-2-fluorobenzamide
-
-
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-N2-[5-chloro-2-(1H-pyrazol-1-yl)phenyl]glycinamide
-
-
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-N2-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]glycinamide
-
-
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-N2-[5-chloro-2-(4H-1,2,4-triazol-4-yl)phenyl]glycinamide
-
-
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]benzene-1,4-dicarboxamide
-
-
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2,2-dimethylpropyl]-N2-[(3,4-dichlorobenzyl)carbamoyl]-L-leucinamide
-
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-N2-[(2,4-dichlorobenzyl)carbamoyl]-L-leucinamide
-
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-N2-[(3,4-dichlorobenzyl)carbamoyl]-L-leucinamide
-
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-N2-[(4-chlorobenzyl)carbamoyl]-L-leucinamide
-
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-Nalpha-([[(3,4-dichlorobenzyl)carbamoyl]amino]methyl)-L-phenylalaninamide
-
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-Nalpha-([[(3,4-dichlorophenyl)sulfonyl]amino]methyl)-L-phenylalaninamide
-
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-Nalpha-([[(4-fluorobenzyl)carbamoyl]amino]methyl)-L-phenylalaninamide
-
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-Nalpha-[[(furan-2-ylacetyl)amino]methyl]-L-phenylalaninamide
-
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-Nalpha-[[(furan-2-ylcarbonyl)amino]methyl]-L-phenylalaninamide
-
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-Nalpha-[[(phenylcarbamoyl)amino]methyl]-L-phenylalaninamide
-
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]propyl]-N2-[(3,4-dichlorobenzyl)carbamoyl]-L-leucinamide
-
N-[(1S)-2-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]amino]-1-cyclohexyl-2-oxoethyl]-N2-[(3,4-dichlorobenzyl)carbamoyl]-L-leucinamide
-
N-[(2S)-1-([2-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]ethyl]amino)-1-oxo-3-phenylpropan-2-yl]-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-carboxamide
-
-
N-[(2S)-1-([2-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]ethyl]amino)-1-oxo-3-phenylpropan-2-yl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazine-7-carboxamide
N-[(2S)-1-([2-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]ethyl]amino)-1-oxo-3-phenylpropan-2-yl]-4-hydroxy-2-oxo-1,2,3,4-tetrahydroquinoline-6-carboxamide
-
-
N-[(3,4-dichlorobenzyl)carbamoyl]-L-leucyl-N-[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]-L-phenylalaninamide
-
N-[2-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]ethyl]-Na-(imidazo[1,2-a]pyrimidin-2-ylcarbonyl)-L-phenylalaninamide
-
-
N-[2-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]ethyl]-Nalpha-(1H-indazol-3-ylcarbonyl)-L-phenylalaninamide
-
-
N-[[5-chloro-2-(prop-2-en-1-yl)-1H-indol-3-yl]methyl]-N2-[(2R)-2-cyclohexyl-2-(pent-4-enoylamino)acetyl]-L-leucinamide
-
-
N-[[5-chloro-2-(prop-2-en-1-yl)-1H-indol-3-yl]methyl]-N2-[(2R)-2-cyclohexyl-2-[[(2S)-2-phenylpent-4-enoyl]amino]acetyl]-L-leucinamide
-
-
N2-(benzylcarbamoyl)-N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-L-leucinamide
-
N2-acetyl-N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-L-leucinamide
-
N2-[(benzyloxy)carbonyl]-N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-L-leucinamide
-
N2-[[(1R)-1-(4-bromophenyl)ethyl]carbamoyl]-N1-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-L-aspartamide
-
N2-[[1-(4-bromophenyl)ethyl]carbamoyl]-N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-L-leucinamide
-
Na-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-3-fluoro-N-[4-(1H-tetrazol-5-yl)phenyl]-L-phenylalaninamide
-
-
Na-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-N-[4-(1H-tetrazol-5-yl)phenyl]-L-phenylalaninamide
-
-
Na-[[(1R)-1-(4-bromophenyl)ethyl]carbamoyl]-N2-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-L-tyrosinamide
-
Nalpha-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-N-(1,2,3,4-tetrahydroisoquinolin-6-yl)-L-phenylalaninamide
-
-
Nalpha-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-N-(1-oxo-2,3-dihydro-1H-isoindol-5-yl)-L-phenylalaninamide
-
-
Nalpha-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-N-(2-oxoazepan-3-yl)-L-phenylalaninamide
-
-
Nalpha-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-N-(6-fluoro-1,3-benzothiazol-2-yl)-L-phenylalaninamide
-
-
Nalpha-[(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]-N-[4-[(methoxycarbonyl)amino]cyclohexyl]-L-phenylalaninamide
-
-
Nalpha-[[(1R)-1-(4-bromophenyl)ethyl]carbamoyl]-N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-L-tryptophanamide
-
nexin-2
-
heparin potentiates the inhibition
-
protease nexin-2
highly specific and potent inhibitor of FXIa, is about 775fold more potent than basic pancreatic trypsin inhibitor in FXIa inhibition, provides single-step slow equilibration inhibition
-
protease nexin-2 mutant F34A
-
-
protease nexin-2 mutant M17A
-
-
protease nexin-2 mutant P13A
-
-
protease nexin-2 mutant R15K
-
-
protease nexin-2 mutant R20A
-
-
protease nexin-2 mutant S19A
-
-
protein Z dependent protease inhibitor
-
-
S-2366
-
noncompetitive inhibition versus factor IX
serpins
inhibition of autolysis of fXIa
-
sodium 2-([[3-(ethoxycarbonyl)-6-methoxy-2-methyl-1-benzofuran-5-yl]oxy]methyl)-6-methoxy-3-(methoxycarbonyl)-1-benzofuran-5-yl sulfate
-
-
sodium 2-[[(3-carboxy-6-methoxy-2-methyl-1-benzofuran-5-yl)oxy]methyl]-3-(ethoxycarbonyl)-6-methoxy-1-benzofuran-5-yl sulfate
-
-
sodium 3-(ethoxycarbonyl)-2-([[3-(ethoxycarbonyl)-6-methoxy-2-methyl-1-benzofuran-5-yl]oxy]methyl)-6-(propan-2-yloxy)-1-benzofuran-5-yl sulfate
-
-
sodium 3-(ethoxycarbonyl)-2-([[3-(ethoxycarbonyl)-6-methoxy-2-methyl-1-benzofuran-5-yl]oxy]methyl)-6-methoxy-1-benzofuran-5-yl sulfate
-
-
sodium 3-(ethoxycarbonyl)-6-methoxy-2-[([6-methoxy-2-methyl-3-[(prop-2-en-1-yloxy)carbonyl]-1-benzofuran-5-yl]oxy)methyl]-1-benzofuran-5-yl sulfate
-
-
sodium 6-ethoxy-3-(ethoxycarbonyl)-2-([[3-(ethoxycarbonyl)-6-methoxy-2-methyl-1-benzofuran-5-yl]oxy]methyl)-1-benzofuran-5-yl sulfate
-
most potent inhibitor
sodium 6-methoxy-3-(methoxycarbonyl)-2-([[6-methoxy-3-(methoxycarbonyl)-2-methyl-1-benzofuran-5-yl]oxy]methyl)-1-benzofuran-5-yl sulfate
-
-
sulfated pentagalloyl beta-D-glucopyranoside
-
-
trans-4-(aminomethyl)-N-((S)-1-(4-(3-cyanophenyl)-1H-imidazol-2-yl)-2-phenylethyl)cyclohexanecarboxamide
-
trans-4-(aminomethyl)-N-((S)-1-(4-(4-cyanophenyl)-1H-imidazol-2-yl)-2-phenylethyl)cyclohexanecarboxamide
-
trans-4-(aminomethyl)-N-((S)-1-(5-oxo-1-phenyl-4,5-dihydro-1H-1,2,4-triazol-3-yl)-2-phenylethyl)cyclohexanecarboxamide
-
trans-4-(aminomethyl)-N-((S)-2-phenyl-1-(2-phenyl-1H-imidazol-4-yl)ethyl)cyclohexanecarboxamide
-
trans-4-(aminomethyl)-N-((S)-2-phenyl-1-(3-phenyl-1H-1,2,4-triazol-5-yl)ethyl)cyclohexanecarboxamide
-
trans-4-(aminomethyl)-N-((S)-2-phenyl-1-(3-phenyl-1H-pyrazol-5-yl)ethyl)cyclohexanecarboxamide
-
trans-4-(aminomethyl)-N-((S)-2-phenyl-1-(4-(4-sulfamoylphenyl)-1H-imidazol-2-yl)ethyl)cyclohexanecarboxamide
-
trans-4-(aminomethyl)-N-((S)-2-phenyl-1-(4-phenyl-1H-imidazol-2-yl)ethyl)cyclohexanecarboxamide
-
trans-4-(aminomethyl)-N-((S)-2-phenyl-1-(5-phenyloxazol-2-yl)ethyl)cyclohexanecarboxamide
-
trans-4-(aminomethyl)-N-[1-(1-methyl-6-oxo-4-phenyl-1,6-dihydropyridin-2-yl)-2-phenylethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[1-(1-oxido-2-phenylpyridin-4-yl)-2-phenylethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[1-(1-oxido-4-phenylpyridin-2-yl)-2-phenylethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[1-(1-oxido-5-phenylpyridin-3-yl)-2-phenylethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[1-(5-chloro-4-phenyl-1H-imidazol-2-yl)-2-phenylethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[1-(5-fluoro-4-phenylpyridin-2-yl)-2-phenylethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[1-(6-amino-4-phenylpyridin-2-yl)-2-phenylethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[1-(6-chloro-4-phenylpyridin-2-yl)-2-phenylethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[1-(6-hydroxy-4-phenylpyridin-2-yl)-2-phenylethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[1-(6-methoxy-4-phenylpyridin-2-yl)-2-phenylethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[1-(biphenyl-3-yl)-2-phenylethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[1-[6-(methylamino)-4-phenylpyridin-2-yl]-2-phenylethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[2-phenyl-1-(2-phenylpyridin-4-yl)ethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[2-phenyl-1-(4-phenyl-1H-imidazol-2-yl)ethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[2-phenyl-1-(4-phenylpyridin-2-yl)ethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[2-phenyl-1-(4-phenylpyrimidin-2-yl)ethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[2-phenyl-1-(5-phenylpyridin-3-yl)ethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[2-phenyl-1-(6-phenylpyridin-2-yl)ethyl]cyclohexanecarboxamide
-
-
trans-4-(aminomethyl)-N-[2-phenyl-1-(6-phenylpyrimidin-4-yl)ethyl]cyclohexanecarboxamide
-
-
trans-N-((S)-1-(4-(3-(2-amino-2-oxoethyl)phenyl)-1H-imidazol-2-yl)-2-phenylethyl)-4-(aminomethyl)cyclohexanecarboxamide
-
trans-N-((S)-1-(4-(3-amino-1H-indazol-6-yl)-1H-imidazol-2-yl)-2-phenylethyl)-4-(aminomethyl)cyclohexanecarboxamide
-
trans-N-((S)-1-(4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl)-2-phenylethyl)-4-(aminomethyl)cyclohexanecarboxamide
reversible enzyme inhibition
trans-N-((S)-1-(4-(3-amino-1H-indazol-6-yl)-5-fluoro-1H-imidazol-2-yl)-2-phenylethyl)-4-(aminomethyl)cyclohexanecarboxamide
-
trans-N-((S)-1-(4-(4-(2-amino-2-oxoethyl)phenyl)-1H-imidazol-2-yl)-2-phenylethyl)-4-(aminomethyl)cyclohexanecarboxamide
-
trans-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-4-(aminomethyl)cyclohexanecarboxamide
-
-
trans-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-4-methylcyclohexanecarboxamide
-
-
trans-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]cyclohexane-1,4-dicarboxamide
-
-
trans-N-[1-[3-(3-amino-1H-indazol-6-yl)phenyl]-2-phenylethyl]-4-(aminomethyl)cyclohexanecarboxamide
-
-
trans-N-[1-[4-(3-amino-1H-indazol-6-yl)-6-oxo-1,6-dihydropyridin-2-yl]-2-phenylethyl]-4-(aminomethyl)cyclohexanecarboxamide
-
-
trans-N-[1-[4-(3-amino-1H-indazol-6-yl)pyridin-2-yl]-2-phenylethyl]-4-(aminomethyl)cyclohexanecarboxamide
-
-
trans-N-[1-[5-(3-amino-1H-indazol-6-yl)-1H-imidazol-2-yl]-2-phenylethyl]-4-(aminomethyl)cyclohexanecarboxamide
-
-
[4-(carbamimidamidomethyl)phenyl]boronic acid
-
-
[4-[(N-[3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]propanoyl]-L-phenylalanyl)amino]phenyl]acetic acid
2-carbamimidamido-1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]ethyl pyridine-3-carboxylate

-
-
2-carbamimidamido-1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]ethyl pyridine-3-carboxylate
-
4-aminobenzamidine

-
a reversible serine protease inhibitor, competitive versus substrate S-2366, noncompetitive versus substrate factor IX, inhibition of wild-type enzyme and recombinant peptide FXI/E361-V607
4-aminobenzamidine
beta-branching of the side chain of residue 193 is deleterious for interactions with 4-aminobenzamidine, diisopropylfluorphosphate, and amidolytic substrates, situations where no S2'-P2' interactions are involved, beta-branching causes steric conflicts with the FXIa 140-loop, overview
antithrombin

-
-
antithrombin
in presence of heaprin
-
benzamidine

-
weak inhibitor of FXIa
C1-inhibitor

-
-
ecotin

-
-
N-[(2S)-1-([2-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]ethyl]amino)-1-oxo-3-phenylpropan-2-yl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazine-7-carboxamide

-
N-[(2S)-1-([2-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]ethyl]amino)-1-oxo-3-phenylpropan-2-yl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazine-7-carboxamide
-
-
protease nexin 2

-
the major interactions required for factor XIa inhibition are localized to the catalytic domain of factor XIa and the Kunitz domain of protease nexin II
-
protease nexin 2
-
activated platelet surface has littlke or no direct effect on the rate of factor IX activation by factor Xia and the reaction proceeds at uninhibited rates when protease nexin 2 is present. Factor Xia-catalyzed FIX activation is completely inhibited by protease nexin 2 in solution or in the presence of umbilical vein endothelial cells
-
[4-[(N-[3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]propanoyl]-L-phenylalanyl)amino]phenyl]acetic acid

-
[4-[(N-[3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]propanoyl]-L-phenylalanyl)amino]phenyl]acetic acid
-
-
additional information

-
-
-
additional information
-
inhibition by recombinant Kunitz domain
-
additional information
the recombinant catalytic domain Ile370-Val607 of FXIa inhibits the binding of factor XIa to the platelets with a Ki of 3.5 nM, whereas the recombinant factor XI heavy chain does not
-
additional information
inhibitor design and synthesis, overview, inhibitor in vitro anticoagulant activity in human plasma
-
additional information
-
inhibitor design and synthesis, overview, inhibitor in vitro anticoagulant activity in human plasma
-
additional information
heparin accelerates inhibition of factor XIa. Heparin enhances antithrombin inhibition of catalytic domain-wild-type 212fold, but only 37-94fold for catalytic domain mutants
-
additional information
Arg184 may be part of a switch that holds FXI in an inactive conformation in the zymogen
-
additional information
not inhibited by protease nexin-2 mutant R15A
-
additional information
-
not inhibited by unfractionated heparin, enoxaparin, fondaparinux, sucrose octasulfate, chondroitin sulfate A, dermatan sulfate, and chondroitin sulfate C
-
additional information
-
potent activated factor VII inhibition with insect-derived serine protease inhibitor, but this protein is only 10fold selective over activated factor X. Inhibition by FXI neutralizing antibodies, which allow preexisting activated factor XI to remain active
-
additional information
-
a monoclonal antibody against FXI or activated factor XI reduces thrombus formation in balloon-injured iliac arteries
-
additional information
-
ketoarginine-based peptidomimetics are irreversible inhibitors of actived factor XI and form a covalent bond to the catalytic serine of the enzyme. Intravenous infusion is efficacious in a rat model of venous thrombosis. A pyridyl analog in a rat mesenteric bleeding model at a 4fold efficacious dose does not alter bleeding time
-
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0.09
benzyloxycarbonyl-Gly-Pro-4-nitroanilide
-
-
0.34
D-Ile-Pro-Arg-4-nitroanilide
recombinant wild-type enzyme, pH 7.5, 37°C
0.00012 - 0.151
factor IX
-
0.3
factor IX 10-mer
-
at pH 7.4 and 37°C
-
0.00038
factor IX mutant G317E
-
at 25°C, pH not specified in the publication
-
0.00035
factor IX mutant G317R
-
at 25°C, pH not specified in the publication
-
0.205 - 0.852
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
0.45 - 0.59
L-pyroglutamyl-L-Pro-L-Arg-4-nitroanilide
0.552 - 0.993
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
0.4 - 352
L-pyroglutamyl-L-prolyl-L-arginyl-p-nitroanilide
0.000103
prochemerin chem163S
-
at pH 7.4 and 37°C
-
0.26 - 0.4
pyroGlu-Pro-Arg-4-nitroanilide
0.56
pyroGlu-Pro-Arg-p-nitroanilide
-
-
additional information
additional information
-
0.00012
factor IX

-
FXIa/PKA4, 37°C
-
0.00016
factor IX
-
FXIa/PKA4-Gly326, 37°C
-
0.0002
factor IX
-
factor FXIa, 37°C
-
0.0002 - 0.00021
factor IX
-
37°C, recombinant wild-type enzyme
-
0.00025
factor IX
-
at 25°C, pH not specified in the publication
-
0.0003
factor IX
-
wild type enzyme, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
-
0.00039 - 0.00047
factor IX
-
37°C, recombinant peptide FXI/E361-V607
-
0.053
factor IX
-
pH 7.4, 37°C, recombinant wild-type enzyme
-
0.151
factor IX
-
at 22°C
-
0.205
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide

-
mutant enzyme K192R, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.268
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme R3704A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.292
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme Y5901A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.315
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme K192E, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.336
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme Y5901V, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.339
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
wild type enzyme, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.383
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme E98D, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.4
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme E98A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.525
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme E98V, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.538
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme Y143A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.603
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme K192Q, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.828
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme I151A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.852
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme K192A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.45
L-pyroglutamyl-L-Pro-L-Arg-4-nitroanilide

-
FXIa/PKA4
0.5
L-pyroglutamyl-L-Pro-L-Arg-4-nitroanilide
-
factor FXIa
0.59
L-pyroglutamyl-L-Pro-L-Arg-4-nitroanilide
-
FXIa/PKA4-Gly326
0.552
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide

fXIa-catalytic domain-K170A/R171A/R173A mutant
0.655
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
fXIa-catalytic domain-K170A mutant
0.757
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
fXIa-catalytic domain-wild type
0.764
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
fXIa-catalytic domain-K179A mutant
0.81
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
fXIa-catalytic domain-R173A mutant
0.812
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
fXIa-catalytic domain-R171A mutant
0.829
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
fXIa-catalytic domain-K175A mutant
0.943
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
fXIa-wild type
0.993
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
fXIa-R37Q mutant
0.4
L-pyroglutamyl-L-prolyl-L-arginyl-p-nitroanilide

-
-
233
L-pyroglutamyl-L-prolyl-L-arginyl-p-nitroanilide
-
FXIa
352
L-pyroglutamyl-L-prolyl-L-arginyl-p-nitroanilide
-
fXIaCD
0.26
pyroGlu-Pro-Arg-4-nitroanilide

recombinant wild-type enzyme, pH 7.5, 37°C
0.4
pyroGlu-Pro-Arg-4-nitroanilide
-
pH 7.4, 37°C, recombinant wild-type enzyme
0.225
S-2366

-
37°C, recombinant wild-type enzyme
0.357
S-2366
-
37°C, recombinant peptide FXI/E361-V607
0.384
S-2366
-
mutant FXIa/G326C
additional information
additional information

kinetics of recombinant wild-type and mutant enzymes, overview
-
additional information
additional information
-
kinetics of isolated subunits with each one active site, stoichiometry of FIX and FIXalphabeta binding to FXIa, overview
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
110.2
D-Ile-Pro-Arg-4-nitroanilide
recombinant wild-type enzyme, pH 7.5, 37°C
0.00065 - 5.8
factor IX
-
0.083
factor IX 10-mer
-
at pH 7.4 and 37°C
-
8
Factor XI
-
pH 7.3, 37°C
-
5.8 - 201
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
250 - 430
L-pyroglutamyl-L-Pro-L-Arg-4-nitroanilide
98 - 148
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
67 - 117
L-pyroglutamyl-L-prolyl-L-arginyl-p-nitroanilide
0.91
prochemerin chem163S
-
at pH 7.4 and 37°C
-
0.268 - 145
pyroGlu-Pro-Arg-4-nitroanilide
350
pyroGlu-Pro-Arg-p-nitroanilide
-
-
0.00065
factor IX

-
37°C, recombinant peptide FXI/E361-V607
-
0.2
factor IX
-
in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
-
0.2
factor IX
-
kcat less than 0.2 s-1, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
-
0.2
factor IX
-
kcat less than 0.2 s-1, mutant enzyme E98A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
-
0.2
factor IX
-
kcat less than 0.2 s-1, mutant enzyme E98D, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
-
0.2
factor IX
-
kcat less than 0.2 s-1, mutant enzyme E98V, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
-
0.2
factor IX
-
kcat less than 0.2 s-1, mutant enzyme Y143A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
-
0.2
factor IX
-
mutant enzyme I151A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
-
0.334
factor IX
-
37°C, recombinant wild-type enzyme
-
0.55
factor IX
-
pH 7.4, 37°C, recombinant wild-type enzyme
-
0.66
factor IX
-
at 22°C
-
0.73
factor IX
-
wild type enzyme, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
-
3.4
factor IX
-
FXIa/PKA4, 37°C
-
5.7
factor IX
-
FXIa/PKA4-Gly326, 37°C
-
5.8
factor IX
-
factor FXIa, 37°C
-
5.8
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide

-
mutant enzyme E98D, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
7
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme Y143A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
8
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme R3704A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
14
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme K192R, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
21
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme E98V, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
29
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme Y5901A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
30
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme K192Q, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
42
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme Y5901V, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
58
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme I151A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
86
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme K192E, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
95
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme E98A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
95
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
mutant enzyme K192A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
201
L-pyroGlu-L-Pro-L-Arg-4-nitroanilide
-
wild type enzyme, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
250
L-pyroglutamyl-L-Pro-L-Arg-4-nitroanilide

-
FXIa/PKA4
310
L-pyroglutamyl-L-Pro-L-Arg-4-nitroanilide
-
factor FXIa
430
L-pyroglutamyl-L-Pro-L-Arg-4-nitroanilide
-
FXIa/PKA4-Gly326
98
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide

fXIa-catalytic domain-K170A mutant
115
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
fXIa-catalytic domain-K170A/R171A/R173A mutant
115
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
fXIa-catalytic domain-R171A mutant
116
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
fXIa-catalytic domain-K179A mutant
117
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
fXIa-catalytic domain-K175A mutant
117
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
fXIa-catalytic domain-R173A mutant
119
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
fXIa-catalytic domain-wild type
148
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
fXIa-R37Q mutant
148
L-pyroglutamyl-L-prolyl-L-argininyl-p-nitroanilide
fXIa-wild type
67
L-pyroglutamyl-L-prolyl-L-arginyl-p-nitroanilide

-
fXIaCD
117
L-pyroglutamyl-L-prolyl-L-arginyl-p-nitroanilide
-
fXIa
0.268
pyroGlu-Pro-Arg-4-nitroanilide

-
pH 7.4, 37°C, recombinant wild-type enzyme
145
pyroGlu-Pro-Arg-4-nitroanilide
recombinant wild-type enzyme, pH 7.5, 37°C
113
S-2366

-
37°C, recombinant wild-type enzyme
121
S-2366
-
37°C, recombinant peptide FXI/E361-V607
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0.000005
(2E)-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-1H-imidazol-2-yl]-2-phenylethyl]-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enamide
-
at 25°C, pH not specified in the publication
0.0000012
(2E)-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enamide
-
at 25°C, pH not specified in the publication
0.00000215
1-amino-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-5,6,7,8-tetrahydroisoquinoline-6-carboxamide
-
at 25°C, pH not specified in the publication
0.000019
1-amino-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]isoquinoline-6-carboxamide
-
at 25°C, pH not specified in the publication
0.000023
1-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-(3-chloro-2,6-difluorobenzyl)urea
-
at 25°C, pH not specified in the publication
0.000057
1-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-(3-chloro-2-fluorobenzyl)urea
-
at 25°C, pH not specified in the publication
0.000054
1-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-(3-chlorobenzyl)urea
-
at 25°C, pH not specified in the publication
0.000031
1-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-(5-chloro-2-fluorobenzyl)urea
-
at 25°C, pH not specified in the publication
0.000075
1-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-(5-chloro-2-methoxybenzyl)urea
-
at 25°C, pH not specified in the publication
0.000053
1-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-(5-chloro-2-methylbenzyl)urea
-
at 25°C, pH not specified in the publication
0.0000058
1-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-[2-(aminomethyl)-5-chlorobenzyl]urea
-
at 25°C, pH not specified in the publication
0.00024
1-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-3-[5-chloro-2-(trifluoromethyl)benzyl]urea
-
at 25°C, pH not specified in the publication
0.000275
2-(3-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)phenyl)acetic acid
at pH 7.4 and 37°C
0.00015
2-(4-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)phenyl)acetic acid
at pH 7.4 and 37°C
0.0000002
3'-[(2S,4R)-6-carbamimidoyl-4-methyl-4-phenyl-1,2,3,4-tetrahydroquinolin-2-yl]-4-carbamoyl-5'-[(3-methylbutanoyl)amino]biphenyl-2-carboxylic acid
at pH 7.4 and 37°C
0.0011
3-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)benzamide
at pH 7.4 and 37°C
0.000125
3-amino-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-1,2-benzoxazole-6-carboxamide
-
at 25°C, pH not specified in the publication
0.000058
3-amino-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-1H-indazole-6-carboxamide
-
at 25°C, pH not specified in the publication
0.00286
4-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)-N,N-dimethylbenzamide
at pH 7.4 and 37°C
0.00035
4-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)-N-methylbenzamide
at pH 7.4 and 37°C
0.00003
4-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)benzamide
at pH 7.4 and 37°C
0.000009
4-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-5-bromo-1H-imidazol-4-yl)-benzamide
at pH 7.4 and 37°C
0.000004
4-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-5-chloro-1H-imidazol-4-yl)-benzamide
at pH 7.4 and 37°C
0.00003
4-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-5-fluoro-1H-imidazol-4-yl)-benzamide
at pH 7.4 and 37°C
0.00059
4-(2-(S-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)benzoic acid
at pH 7.4 and 37°C
0.0000211 - 0.095
4-aminobenzamidine
0.000627
basic pancreatic trypsin inhibitor
in 50 mM Tris, 150 mM NaCl, 5 mM CaCl2, 0.1% (w/v) bovine serum albumin, pH 7.5, at 37°C
-
0.0000041
basic pancreatic trypsin inhibitor mutant K15R
in 50 mM Tris, 150 mM NaCl, 5 mM CaCl2, 0.1% (w/v) bovine serum albumin, pH 7.5, at 37°C
-
0.00063
ethyl 2-(3-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)phenyl)-acetate
at pH 7.4 and 37°C
0.000495
ethyl 2-(4-(2-((S)-1-(trans-4-(aminomethyl)cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)phenyl)-acetate
at pH 7.4 and 37°C
0.0000067
methyl (4-[2-[(1S)-1-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-2-phenylethyl]-1H-imidazol-4-yl]phenyl)carbamate
-
at 25°C, pH not specified in the publication
0.0000027 - 0.0000058
methyl (4-[5-chloro-2-[(1S)-1-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-2-phenylethyl]-1H-imidazol-4-yl]phenyl)carbamate
0.0000019
methyl (4-[5-chloro-2-[(1S)-1-([3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]propanoyl]amino)-2-phenylethyl]-1H-imidazol-4-yl]phenyl)carbamate
-
at 25°C, pH not specified in the publication
0.0000034
methyl (4-[5-chloro-2-[(1S)-1-([N-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]glycyl]amino)-2-phenylethyl]-1H-imidazol-4-yl]phenyl)carbamate
-
at 25°C, pH not specified in the publication
0.0008
methyl 4-(2-((S)-1-(trans-4-(aminomethyl)-cyclohexanecarboxamido)-2-phenylethyl)-1H-imidazol-4-yl)-benzoate
at pH 7.4 and 37°C
0.0005
methyl [(10S)-10-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-3-oxo-1,2,3,9,10,12-hexahydro-14,11-(azeno)-8,4-(metheno)-2,12-benzodiazacyclohexadecin-17-yl]carbamate
-
at 25°C, pH not specified in the publication
0.000092
methyl [(10S)-13-chloro-10-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-3-oxo-1,2,3,9,10,12-hexahydro-14,11-(azeno)-8,4-(metheno)-2,12-benzodiazacyclohexadecin-17-yl]carbamate
-
at 25°C, pH not specified in the publication
0.0000015
methyl [(11S)-11-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-2-oxo-1,3,4,10,11,13-hexahydro-2H-15,12-(azeno)-5,9-(metheno)-1,13-benzodiazacycloheptadecin-18-yl]carbamate
-
at 37°C, pH not specified in the publication
0.00000032
methyl [(11S)-11-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-2-oxo-1,3,4,10,11,13-hexahydro-2H-5,9:15,12-di(azeno)-1,13-benzodiazacycloheptadecin-18-yl]carbamate
-
at 37°C, pH not specified in the publication
0.00000053
methyl [(11S)-11-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-6-fluoro-2-oxo-1,3,4,10,11,13-hexahydro-2H-15,12-(azeno)-5,9-(metheno)-1,13-benzodiazacycloheptadecin-18-yl]carbamate
-
at 37°C, pH not specified in the publication
0.00000002
methyl [(11S)-11-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-6-fluoro-2-oxo-1,3,4,10,11,13-hexahydro-2H-5,9:15,12-di(azeno)-1,13-benzodiazacycloheptadecin-18-yl]carbamate
-
at 37°C, pH not specified in the publication
0.0000082
methyl [(5S)-2-chloro-5-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-5,6,12,13,14,15-hexahydro-3H-1,4-(azeno)-7,11-(metheno)-3-benzazacycloheptadecin-17-yl]carbamate
-
at 25°C, pH not specified in the publication
0.000071
methyl [(5S)-5-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-5,6,11,12,13,14-hexahydro-3H-1,4-(azeno)-7,10-etheno-3-benzazacyclohexadecin-16-yl]carbamate
-
at 25°C, pH not specified in the publication
0.000017 - 0.0081
methyl [(9S)-12-chloro-9-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-3-oxo-1,2,3,8,9,11-hexahydro-13,10-(azeno)-4,7-etheno-2,11-benzodiazacyclopentadecin-16-yl]carbamate
0.0064
methyl [(9S)-9-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-3-oxo-1,2,3,8,9,11-hexahydro-13,10-(azeno)-4,7-etheno-2,11-benzodiazacyclopentadecin-16-yl]carbamate
-
at 25°C, pH not specified in the publication
0.00000149
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-1-(3-aminopropyl)cyclohexanecarboxamide
-
at 25°C, pH not specified in the publication
0.000065
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-2,6-difluoro-4-methoxybenzamide
-
at 25°C, pH not specified in the publication
0.00028
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-2-fluoro-4-methoxybenzamide
-
at 25°C, pH not specified in the publication
0.0002
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-2-fluoro-4-methylbenzamide
-
at 25°C, pH not specified in the publication
0.00000103
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-4-(aminomethyl)-2-fluorobenzamide
-
at 25°C, pH not specified in the publication
0.00000116
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-4-(aminomethyl)benzamide
-
at 25°C, pH not specified in the publication
0.00039
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-4-methylbenzamide
-
at 25°C, pH not specified in the publication
0.00053
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-5-chloro-2-fluorobenzamide
-
at 25°C, pH not specified in the publication
0.00045
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-N2-[5-chloro-2-(1H-pyrazol-1-yl)phenyl]glycinamide
-
at 25°C, pH not specified in the publication
0.0000015
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-N2-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]glycinamide
-
at 25°C, pH not specified in the publication
0.000046
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-N2-[5-chloro-2-(4H-1,2,4-triazol-4-yl)phenyl]glycinamide
-
at 25°C, pH not specified in the publication
0.00031
N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]benzene-1,4-dicarboxamide
-
at 25°C, pH not specified in the publication
0.000001 - 0.0000047
protease nexin 2
-
0.00000081
protease nexin-2
in 50 mM Tris, 150 mM NaCl, 5 mM CaCl2, 0.1% (w/v) bovine serum albumin, pH 7.5, at 37°C
-
0.00000492
protease nexin-2 mutant F34A
in 50 mM Tris, 150 mM NaCl, 5 mM CaCl2, 0.1% (w/v) bovine serum albumin, pH 7.5, at 37°C
-
0.00000081
protease nexin-2 mutant M17A
in 50 mM Tris, 150 mM NaCl, 5 mM CaCl2, 0.1% (w/v) bovine serum albumin, pH 7.5, at 37°C
-
0.00000296
protease nexin-2 mutant P13A
in 50 mM Tris, 150 mM NaCl, 5 mM CaCl2, 0.1% (w/v) bovine serum albumin, pH 7.5, at 37°C
-
0.0000113
protease nexin-2 mutant R15K
in 50 mM Tris, 150 mM NaCl, 5 mM CaCl2, 0.1% (w/v) bovine serum albumin, pH 7.5, at 37°C
-
0.00000283
protease nexin-2 mutant R20A
in 50 mM Tris, 150 mM NaCl, 5 mM CaCl2, 0.1% (w/v) bovine serum albumin, pH 7.5, at 37°C
-
0.00000093
protease nexin-2 mutant S19A
in 50 mM Tris, 150 mM NaCl, 5 mM CaCl2, 0.1% (w/v) bovine serum albumin, pH 7.5, at 37°C
-
0.00112
trans-4-(aminomethyl)-N-((S)-1-(4-(3-cyanophenyl)-1H-imidazol-2-yl)-2-phenylethyl)cyclohexanecarboxamide
at pH 7.4 and 37°C
0.00023
trans-4-(aminomethyl)-N-((S)-1-(4-(4-cyanophenyl)-1H-imidazol-2-yl)-2-phenylethyl)cyclohexanecarboxamide
at pH 7.4 and 37°C
0.003074
trans-4-(aminomethyl)-N-((S)-1-(5-oxo-1-phenyl-4,5-dihydro-1H-1,2,4-triazol-3-yl)-2-phenylethyl)cyclohexanecarboxamide
at pH 7.4 and 37°C
0.00164
trans-4-(aminomethyl)-N-((S)-2-phenyl-1-(2-phenyl-1H-imidazol-4-yl)ethyl)cyclohexanecarboxamide
at pH 7.4 and 37°C
0.00098
trans-4-(aminomethyl)-N-((S)-2-phenyl-1-(3-phenyl-1H-1,2,4-triazol-5-yl)ethyl)cyclohexanecarboxamide
at pH 7.4 and 37°C
0.00694
trans-4-(aminomethyl)-N-((S)-2-phenyl-1-(3-phenyl-1H-pyrazol-5-yl)ethyl)cyclohexanecarboxamide
at pH 7.4 and 37°C
0.00134
trans-4-(aminomethyl)-N-((S)-2-phenyl-1-(4-(4-sulfamoylphenyl)-1H-imidazol-2-yl)ethyl)cyclohexanecarboxamide
at pH 7.4 and 37°C
0.00012
trans-4-(aminomethyl)-N-((S)-2-phenyl-1-(4-phenyl-1H-imidazol-2-yl)ethyl)cyclohexanecarboxamide
at pH 7.4 and 37°C
0.00144
trans-4-(aminomethyl)-N-((S)-2-phenyl-1-(5-phenyloxazol-2-yl)ethyl)cyclohexanecarboxamide
at pH 7.4 and 37°C
0.000479
trans-4-(aminomethyl)-N-[1-(1-methyl-6-oxo-4-phenyl-1,6-dihydropyridin-2-yl)-2-phenylethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.00253
trans-4-(aminomethyl)-N-[1-(1-oxido-2-phenylpyridin-4-yl)-2-phenylethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.00169
trans-4-(aminomethyl)-N-[1-(1-oxido-4-phenylpyridin-2-yl)-2-phenylethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.001063
trans-4-(aminomethyl)-N-[1-(1-oxido-5-phenylpyridin-3-yl)-2-phenylethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.000012
trans-4-(aminomethyl)-N-[1-(5-chloro-4-phenyl-1H-imidazol-2-yl)-2-phenylethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.00032
trans-4-(aminomethyl)-N-[1-(5-fluoro-4-phenylpyridin-2-yl)-2-phenylethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.000227
trans-4-(aminomethyl)-N-[1-(6-amino-4-phenylpyridin-2-yl)-2-phenylethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.000206
trans-4-(aminomethyl)-N-[1-(6-chloro-4-phenylpyridin-2-yl)-2-phenylethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.000113
trans-4-(aminomethyl)-N-[1-(6-hydroxy-4-phenylpyridin-2-yl)-2-phenylethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.000949
trans-4-(aminomethyl)-N-[1-(6-methoxy-4-phenylpyridin-2-yl)-2-phenylethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.000936
trans-4-(aminomethyl)-N-[1-(biphenyl-3-yl)-2-phenylethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.00086
trans-4-(aminomethyl)-N-[1-[6-(methylamino)-4-phenylpyridin-2-yl]-2-phenylethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.000433
trans-4-(aminomethyl)-N-[2-phenyl-1-(2-phenylpyridin-4-yl)ethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.00012
trans-4-(aminomethyl)-N-[2-phenyl-1-(4-phenyl-1H-imidazol-2-yl)ethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.000377
trans-4-(aminomethyl)-N-[2-phenyl-1-(4-phenylpyridin-2-yl)ethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.01142
trans-4-(aminomethyl)-N-[2-phenyl-1-(4-phenylpyrimidin-2-yl)ethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.00033
trans-4-(aminomethyl)-N-[2-phenyl-1-(5-phenylpyridin-3-yl)ethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.03021
trans-4-(aminomethyl)-N-[2-phenyl-1-(6-phenylpyridin-2-yl)ethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.000331
trans-4-(aminomethyl)-N-[2-phenyl-1-(6-phenylpyrimidin-4-yl)ethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.000545
trans-N-((S)-1-(4-(3-(2-amino-2-oxoethyl)phenyl)-1H-imidazol-2-yl)-2-phenylethyl)-4-(aminomethyl)cyclohexanecarboxamide
at pH 7.4 and 37°C
0.000003
trans-N-((S)-1-(4-(3-amino-1H-indazol-6-yl)-1H-imidazol-2-yl)-2-phenylethyl)-4-(aminomethyl)cyclohexanecarboxamide
at pH 7.4 and 37°C
0.000003
trans-N-((S)-1-(4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl)-2-phenylethyl)-4-(aminomethyl)cyclohexanecarboxamide
at pH 7.4 and 37°C
0.0000003
trans-N-((S)-1-(4-(3-amino-1H-indazol-6-yl)-5-fluoro-1H-imidazol-2-yl)-2-phenylethyl)-4-(aminomethyl)cyclohexanecarboxamide
at pH 7.4 and 37°C
0.0004
trans-N-((S)-1-(4-(4-(2-amino-2-oxoethyl)phenyl)-1H-imidazol-2-yl)-2-phenylethyl)-4-(aminomethyl)cyclohexanecarboxamide
at pH 7.4 and 37°C
0.00000031
trans-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-4-(aminomethyl)cyclohexanecarboxamide
0.000068
trans-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-4-methylcyclohexanecarboxamide
-
at 25°C, pH not specified in the publication
0.0029
trans-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]cyclohexane-1,4-dicarboxamide
-
at 25°C, pH not specified in the publication
0.000021
trans-N-[1-[3-(3-amino-1H-indazol-6-yl)phenyl]-2-phenylethyl]-4-(aminomethyl)cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.0000037
trans-N-[1-[4-(3-amino-1H-indazol-6-yl)-6-oxo-1,6-dihydropyridin-2-yl]-2-phenylethyl]-4-(aminomethyl)cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.000013
trans-N-[1-[4-(3-amino-1H-indazol-6-yl)pyridin-2-yl]-2-phenylethyl]-4-(aminomethyl)cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.0000032
trans-N-[1-[5-(3-amino-1H-indazol-6-yl)-1H-imidazol-2-yl]-2-phenylethyl]-4-(aminomethyl)cyclohexanecarboxamide
-
pH and temperature not specified in the publication
additional information
additional information
-
0.0000211
4-aminobenzamidine

-
mutant enzyme Y143A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.0000245
4-aminobenzamidine
-
mutant enzyme K192E, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.0000362
4-aminobenzamidine
-
mutant enzyme R3704A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.0000396
4-aminobenzamidine
-
mutant enzyme E98V, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.0000416
4-aminobenzamidine
-
mutant enzyme E98A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.0000419
4-aminobenzamidine
-
mutant enzyme Y5901V, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.0000497
4-aminobenzamidine
-
mutant enzyme Y5901A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.0000513
4-aminobenzamidine
-
wild type enzyme, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.0000714
4-aminobenzamidine
-
mutant enzyme K192R, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.0000739
4-aminobenzamidine
-
mutant enzyme I151A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.000079
4-aminobenzamidine
-
mutant enzyme K192Q, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.0001529
4-aminobenzamidine
-
mutant enzyme K192A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
0.06
4-aminobenzamidine
-
37°C, recombinant wild-type enzyme, versus substrate S-2366
0.085
4-aminobenzamidine
-
37°C, recombinant peptide FXI/E361-V607, versus substrate S-2366
0.086
4-aminobenzamidine
-
37°C, recombinant peptide FXI/E361-V607, versus substrate factor IX
0.095
4-aminobenzamidine
-
37°C, recombinant wild-type enzyme, versus substrate factor IX
0.52
Aprotinin

-
L-pyroglutamyl-L-prolyl-L-arginyl-p-nitroanilide substrate, free FXIa
0.96
Aprotinin
-
FIX substrate, free FXIa
10.42
Aprotinin
-
FIX substrate, FXIa-FIX complex
1.43
leupeptin

-
L-pyroglutamyl-L-prolyl-L-arginyl-p-nitroanilide substrate, free FXIa
2.91
leupeptin
-
FIX substrate, free FXIa
19.12
leupeptin
-
FIX substrate, FXIa-FIX complex
209
leupeptin
-
L-pyroglutamyl-L-prolyl-L-arginyl-p-nitroanilide substrate, FXIa-FIX complex
0.0000027
methyl (4-[5-chloro-2-[(1S)-1-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-2-phenylethyl]-1H-imidazol-4-yl]phenyl)carbamate

-
at 25°C, pH not specified in the publication
0.0000058
methyl (4-[5-chloro-2-[(1S)-1-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-2-phenylethyl]-1H-imidazol-4-yl]phenyl)carbamate
-
at 37°C, pH not specified in the publication
0.000017
methyl [(9S)-12-chloro-9-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-3-oxo-1,2,3,8,9,11-hexahydro-13,10-(azeno)-4,7-etheno-2,11-benzodiazacyclopentadecin-16-yl]carbamate

-
at 25°C, pH not specified in the publication
0.0081
methyl [(9S)-12-chloro-9-([(2E)-3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]prop-2-enoyl]amino)-3-oxo-1,2,3,8,9,11-hexahydro-13,10-(azeno)-4,7-etheno-2,11-benzodiazacyclopentadecin-16-yl]carbamate
-
at 25°C, pH not specified in the publication
0.000001
protease nexin 2

-
mutant enzyme E98A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
-
0.0000011
protease nexin 2
-
mutant enzyme E98V, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
-
0.0000013
protease nexin 2
-
mutant enzyme R3704A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
-
0.0000013
protease nexin 2
-
mutant enzyme Y143A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
-
0.0000014
protease nexin 2
-
mutant enzyme I151A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
-
0.0000015
protease nexin 2
-
mutant enzyme K192Q, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
-
0.0000015
protease nexin 2
-
wild type enzyme, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
-
0.0000047
protease nexin 2
-
mutant enzyme K192A, in 50 mM Tris-HCl, 150 mM NaCl, 5 mM CaCl2, 0.5% (w/v) bovine serum albumin, pH 7.3, at 37°C
-
0.42
S-2366

-
37°C, recombinant peptide FXI/E361-V607, versus substrate factor IX
0.425
S-2366
-
37°C, recombinant wild-type enzyme, versus substrate factor IX
0.00000031
trans-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-4-(aminomethyl)cyclohexanecarboxamide

-
pH and temperature not specified in the publication
0.00000031
trans-N-[(1S)-1-[4-(3-amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-4-(aminomethyl)cyclohexanecarboxamide
-
at 25°C, pH not specified in the publication
additional information
additional information

-
-
-
additional information
additional information
competition for platelet binding by the wild-type enzyme and mutants, overview
-
additional information
additional information
second-order inhibition rate constants, wild-type and mutant enzymes with different inhibitors, overview
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.000132
(3R)-3-(4-bromophenyl)-N-[(1S)-2-[[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]amino]-1-cyclohexyl-2-oxoethyl]butanamide
Homo sapiens
pH 7.4, 37°C
0.000533
(3R)-N-[(1S)-2-[[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]amino]-2-oxo-1-(pyridin-3-ylmethyl)ethyl]-3-(4-fluorophenyl)butanamide
Homo sapiens
pH 7.4, 37°C
0.00001
(3S)-3-(4-bromophenyl)-N-[(1S)-2-[[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]amino]-1-cyclohexyl-2-oxoethyl]butanamide
Homo sapiens
pH 7.4, 37°C
0.000028
(3S)-N-[(1S)-2-[[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]amino]-2-oxo-1-(pyridin-3-ylmethyl)ethyl]-3-(4-fluorophenyl)butanamide
Homo sapiens
pH 7.4, 37°C
0.1759
(4S,7S)-18-chloro-7-cyclohexyl-4-(2-methylpropyl)-1,2,4,5,7,8,10,11,12,13,14,15-dodecahydro[1,2,5,8]thiatriazacyclohexadecino[11,10-b]indole-3,6-dione 9,9-dioxide
Homo sapiens
-
pH and temperature not specified in the publication
0.1358
(4S,7S,10S,12Z)-18-chloro-7-cyclohexyl-4-(2-methylpropyl)-10-phenyl-4,5,7,8,10,11,14,15-octahydro-1H-[1,4,7]triazacyclohexadecino[10,9-b]indole-3,6,9(2H)-trione
Homo sapiens
-
pH and temperature not specified in the publication
0.7678
(4S,7S,12Z)-18-chloro-7-cyclohexyl-4-(2-methylpropyl)-1,2,4,5,7,8,10,11,14,15-decahydro[1,2,5,8]thiatriazacyclohexadecino[11,10-b]indole-3,6-dione 9,9-dioxide
Homo sapiens
-
pH and temperature not specified in the publication
0.000076 - 0.0002
(S)-2-(3-(3,4-dichlorobenzyl)ureido)-N-((2S,3S)-1-((S)-5-guanidino-1-oxo-1-(thiazol-2-yl)pentan-2-ylamino)-3-methyl-1-oxopentan-2-yl)-4-methylpentanamide
0.0073
1-[2-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]ethyl]guanidine
Homo sapiens
-
-
0.0257
1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl]guanidine
Homo sapiens
-
-
0.0059
1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]guanidine
Homo sapiens
-
-
0.000007
2-(N2-[[(1R)-1-(4-bromophenyl)ethyl]carbamoyl]-L-arginyl-L-valyl-L-arginyl)-1,3-thiazole
Homo sapiens
pH 7.4, 37°C
0.00003
2-(N2-[[(1R)-1-(4-bromophenyl)ethyl]carbamoyl]-N5-carbamoyl-L-ornithyl-L-valyl-L-arginyl)-1,3-thiazole
Homo sapiens
pH 7.4, 37°C
0.0014
2-carbamimidamido-1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]ethyl pyridine-3-carboxylate
Homo sapiens
-
-
0.0773
benzamidine
Homo sapiens
-
-
0.0000028
BMS-262084
Homo sapiens
at pH 7.4 and 37°C
0.12
boronic acid
Homo sapiens
-
-
0.0013
clavatadine A
Homo sapiens
-
0.027
clavatadine B
Homo sapiens
-
0.0014
decasodium 1,2,3,4,6-pentakis-O-[3,5-bis(sulfonatooxy)benzoyl]-beta-D-threo-hexopyranose
Homo sapiens
-
at pH 7.4 and 37°C
0.0005
decasodium 1,2,3,4,6-pentakis-O-[4-hydroxy-3,5-bis(sulfonatooxy)benzoyl]-beta-D-threo-hexopyranose
Homo sapiens
-
at pH 7.4 and 37°C
0.000403
ethyl N-[[(3S,6S,9S)-14-amino-3-benzyl-14-imino-6-(1-methylethyl)-4,7-dioxo-9-(1,3-thiazol-2-ylcarbonyl)-2,5,8,13-tetraazatetradec-1-yl]carbamoyl]leucinate
Homo sapiens
pH 7.4, 37°C
0.000258
ethyl N-[[(3S,6S,9S)-14-amino-3-benzyl-14-imino-6-(1-methylethyl)-4,7-dioxo-9-(1,3-thiazol-2-ylcarbonyl)-2,5,8,13-tetraazatetradec-1-yl]carbamoyl]phenylalaninate
Homo sapiens
pH 7.4, 37°C
0.0092
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2,2-dimethylpropyl]-N2-[(3,4-dichlorobenzyl)carbamoyl]-L-leucinamide
Homo sapiens
pH 7.4, 37°C
0.000045
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-N2-[(2,4-dichlorobenzyl)carbamoyl]-L-leucinamide
Homo sapiens
pH 7.4, 37°C
0.000063
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-N2-[(3,4-dichlorobenzyl)carbamoyl]-L-leucinamide
Homo sapiens
pH 7.4, 37°C
0.000114
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-N2-[(4-chlorobenzyl)carbamoyl]-L-leucinamide
Homo sapiens
pH 7.4, 37°C
0.000093
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-Nalpha-([[(3,4-dichlorobenzyl)carbamoyl]amino]methyl)-L-phenylalaninamide
Homo sapiens
pH 7.4, 37°C
0.0026
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-Nalpha-([[(3,4-dichlorophenyl)sulfonyl]amino]methyl)-L-phenylalaninamide
Homo sapiens
pH 7.4, 37°C
0.00016
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-Nalpha-([[(4-fluorobenzyl)carbamoyl]amino]methyl)-L-phenylalaninamide
Homo sapiens
pH 7.4, 37°C
0.0023
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-Nalpha-[[(furan-2-ylacetyl)amino]methyl]-L-phenylalaninamide
Homo sapiens
pH 7.4, 37°C
0.0022
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-Nalpha-[[(furan-2-ylcarbonyl)amino]methyl]-L-phenylalaninamide
Homo sapiens
pH 7.4, 37°C
0.00192
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-Nalpha-[[(phenylcarbamoyl)amino]methyl]-L-phenylalaninamide
Homo sapiens
pH 7.4, 37°C
0.00092
N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]propyl]-N2-[(3,4-dichlorobenzyl)carbamoyl]-L-leucinamide
Homo sapiens
pH 7.4, 37°C
0.00034
N-[(1S)-2-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]amino]-1-cyclohexyl-2-oxoethyl]-N2-[(3,4-dichlorobenzyl)carbamoyl]-L-leucinamide
Homo sapiens
pH 7.4, 37°C
0.00071
N-[(3,4-dichlorobenzyl)carbamoyl]-L-leucyl-N-[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]-L-phenylalaninamide
Homo sapiens
pH 7.4, 37°C
0.1031
N-[[5-chloro-2-(prop-2-en-1-yl)-1H-indol-3-yl]methyl]-N2-[(2R)-2-cyclohexyl-2-(pent-4-enoylamino)acetyl]-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.1459
N-[[5-chloro-2-(prop-2-en-1-yl)-1H-indol-3-yl]methyl]-N2-[(2R)-2-cyclohexyl-2-[[(2S)-2-phenylpent-4-enoyl]amino]acetyl]-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000136
N2-(benzylcarbamoyl)-N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-L-leucinamide
Homo sapiens
pH 7.4, 37°C
0.027
N2-acetyl-N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-L-leucinamide
Homo sapiens
pH 7.4, 37°C
0.000356
N2-[(benzyloxy)carbonyl]-N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-L-leucinamide
Homo sapiens
pH 7.4, 37°C
0.000008
N2-[[(1R)-1-(4-bromophenyl)ethyl]carbamoyl]-N1-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-L-aspartamide
Homo sapiens
pH 7.4, 37°C
0.00001
N2-[[1-(4-bromophenyl)ethyl]carbamoyl]-N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-L-leucinamide
Homo sapiens
pH 7.4, 37°C
0.000006
Na-[[(1R)-1-(4-bromophenyl)ethyl]carbamoyl]-N2-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-L-tyrosinamide
Homo sapiens
pH 7.4, 37°C
0.000029
Nalpha-[[(1R)-1-(4-bromophenyl)ethyl]carbamoyl]-N-[(1S)-1-[[(1S)-4-carbamimidamido-1-(1,3-thiazol-2-ylcarbonyl)butyl]carbamoyl]-2-methylpropyl]-L-tryptophanamide
Homo sapiens
pH 7.4, 37°C
0.022
[4-(carbamimidamidomethyl)phenyl]boronic acid
Homo sapiens
-
-
0.000076
(S)-2-(3-(3,4-dichlorobenzyl)ureido)-N-((2S,3S)-1-((S)-5-guanidino-1-oxo-1-(thiazol-2-yl)pentan-2-ylamino)-3-methyl-1-oxopentan-2-yl)-4-methylpentanamide

Homo sapiens
pH 7.4, 37°C
0.0002
(S)-2-(3-(3,4-dichlorobenzyl)ureido)-N-((2S,3S)-1-((S)-5-guanidino-1-oxo-1-(thiazol-2-yl)pentan-2-ylamino)-3-methyl-1-oxopentan-2-yl)-4-methylpentanamide
Homo sapiens
pH 7.4, 37°C
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