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Literature summary for 3.4.21.68 extracted from

  • Venkatraj, M.; Messagie, J.; Joossens, J.; Lambeir, A.M.; Haemers, A.; Van der Veken, P.; Augustyns, K.
    Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA) (2012), Bioorg. Med. Chem., 20, 1557-1568.
    View publication on PubMed
Search for more literature for 3.4.21.68

Inhibitors

Inhibitors Comment Organism Structure
2-([6-[(3'-carbamimidoylbiphenyl-3-yl)oxy]-3,5-difluoro-4-methylpyridin-2-yl]oxy)-4-(dimethylamino)benzoic acid
-
 Homo sapiens
2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
-
 Homo sapiens
2-[(6-[[5-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
-
 Homo sapiens
4-(2-aminoethoxy)-N-[3-chloro-2-ethoxy-5-(piperidin-1-yl)phenyl]-3,5-dimethylbenzamide
-
 Homo sapiens
4-[(E)-(5-oxo-2-phenyl-1,3-oxazol-4(5H)-ylidene)methyl]benzenecarboximidamide
-
 Homo sapiens
6-carbamimidoyl-N-(3,5-dimethoxyphenyl)-2-naphthamide
-
 Homo sapiens
6-carbamimidoyl-N-phenyl-2-naphthamide
-
 Homo sapiens
6-methoxy-N-(3'-(trifluoromethyl)biphenyl-4-yl)-2-naphthamide
-
 Homo sapiens
6-methoxy-N-(3'-(trifluoromethyl)biphenyl-4-yl)naphthalene-2-sulfonamide
-
 Homo sapiens
6-methoxy-N-(3'-methoxybiphenyl-4-yl)-2-naphthamide
-
 Homo sapiens
6-methoxy-N-(3'-nitrobiphenyl-4-yl)-2-naphthamide
-
 Homo sapiens
bis[(phenylamino)acetyl] [2-(4-carbamimidamidophenyl)-1-[(methoxycarbonyl)amino]ethyl]phosphonate
-
 Homo sapiens
diphenyl [2-(4-carbamimidamidophenyl)-1-[(methoxycarbonyl)amino]ethyl]phosphonate
-
 Homo sapiens
ethyl 4-(3-carbamimidoyl-N-[[2,4,6-tri(propan-2-yl)phenyl]sulfonyl]-L-phenylalanyl)piperazine-1-carboxylate
-
 Homo sapiens
methyl 4'-(6-carbamoyl-2-naphthamido)biphenyl-3-carboxylate
-
 Homo sapiens
methyl 4'-(6-methoxy-2-naphthamido)biphenyl-3-carboxylate
-
 Homo sapiens
methyl 4'-(6-methoxynaphthalene-2-sulfonamido)biphenyl-3-carboxylate
-
 Homo sapiens
additional information synthesis and evaluation of a series of naphthamide and naphthalene sulfonamides as enzyme inhibitors containing non-basic groups as substitute for amidine or guanidine groups, overview Homo sapiens
N-(4-(aminomethyl)phenyl)-6-carbamimidoyl-2-naphthamide trifluoro acetate
-
 Homo sapiens
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
 Homo sapiens
N2-(2,4'-dimethoxybiphenyl-4-yl)naphthalene-2,6-dicarboxamide
-
 Homo sapiens
N2-(3'-(trifluoromethyl)biphenyl-4-yl)naphthalene-2,6-dicarboxamide
-
 Homo sapiens
N2-(3'-methoxybiphenyl-4-yl)naphthalene-2,6-dicarboxamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P00750
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-Ile-Pro-Arg-4-nitroanilide + H2O
-
 Homo sapiens D-Ile-Pro-Arg + 4-nitroaniline
-
 ?
plasmin + H2O
-
 Homo sapiens ?
-
 ?
pyro-Glu-Pro-Arg-4-nitroanilide + H2O
-
 Homo sapiens pyro-Glu-Pro-Arg + 4-nitroaniline
-
 ?
thrombin + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
tPA
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4 8.3 assay at, dependent on the substrate Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0049
-
 ethyl 4-(3-carbamimidoyl-N-[[2,4,6-tri(propan-2-yl)phenyl]sulfonyl]-L-phenylalanyl)piperazine-1-carboxylate pH 7.4-8.3, 37°C Homo sapiens
0.0074
-
 N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide pH 7.4-8.3, 37°C Homo sapiens
0.0318
-
 6-carbamimidoyl-N-phenyl-2-naphthamide pH 7.4-8.3, 37°C Homo sapiens
0.0584
-
 N-(4-(aminomethyl)phenyl)-6-carbamimidoyl-2-naphthamide trifluoro acetate pH 7.4-8.3, 37°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0034
-
 pH 7.4-8.3, 37°C Homo sapiens N2-(3'-(trifluoromethyl)biphenyl-4-yl)naphthalene-2,6-dicarboxamide
0.0036
-
 pH 7.4-8.3, 37°C Homo sapiens 4-(2-aminoethoxy)-N-[3-chloro-2-ethoxy-5-(piperidin-1-yl)phenyl]-3,5-dimethylbenzamide
0.0039
-
 pH 7.4-8.3, 37°C Homo sapiens 2-([6-[(3'-carbamimidoylbiphenyl-3-yl)oxy]-3,5-difluoro-4-methylpyridin-2-yl]oxy)-4-(dimethylamino)benzoic acid
0.0053
-
 pH 7.4-8.3, 37°C Homo sapiens 6-methoxy-N-(3'-(trifluoromethyl)biphenyl-4-yl)-2-naphthamide
0.0057
-
 pH 7.4-8.3, 37°C Homo sapiens N2-(3'-methoxybiphenyl-4-yl)naphthalene-2,6-dicarboxamide
0.0061
-
 pH 7.4-8.3, 37°C Homo sapiens bis[(phenylamino)acetyl] [2-(4-carbamimidamidophenyl)-1-[(methoxycarbonyl)amino]ethyl]phosphonate
0.0084
-
 pH 7.4-8.3, 37°C Homo sapiens methyl 4'-(6-methoxy-2-naphthamido)biphenyl-3-carboxylate
0.0086
-
 pH 7.4-8.3, 37°C Homo sapiens 6-methoxy-N-(3'-nitrobiphenyl-4-yl)-2-naphthamide
0.0097
-
 pH 7.4-8.3, 37°C Homo sapiens N2-(2,4'-dimethoxybiphenyl-4-yl)naphthalene-2,6-dicarboxamide
0.011
-
 pH 7.4-8.3, 37°C Homo sapiens methyl 4'-(6-carbamoyl-2-naphthamido)biphenyl-3-carboxylate
0.013
-
 pH 7.4-8.3, 37°C Homo sapiens 6-methoxy-N-(3'-(trifluoromethyl)biphenyl-4-yl)naphthalene-2-sulfonamide
0.021
-
 pH 7.4-8.3, 37°C Homo sapiens 6-methoxy-N-(3'-methoxybiphenyl-4-yl)-2-naphthamide
0.022
-
 pH 7.4-8.3, 37°C Homo sapiens 2-[(6-[[3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
0.023
-
 pH 7.4-8.3, 37°C Homo sapiens diphenyl [2-(4-carbamimidamidophenyl)-1-[(methoxycarbonyl)amino]ethyl]phosphonate
0.026
-
 pH 7.4-8.3, 37°C Homo sapiens methyl 4'-(6-methoxynaphthalene-2-sulfonamido)biphenyl-3-carboxylate
0.03
-
 pH 7.4-8.3, 37°C Homo sapiens 2-[(6-[[5-amino-3'-(aminomethyl)biphenyl-3-yl]oxy]-3,5-difluoropyridin-2-yl)oxy]-4-methylbenzoic acid
0.062
-
 pH 7.4-8.3, 37°C Homo sapiens 6-carbamimidoyl-N-(3,5-dimethoxyphenyl)-2-naphthamide
0.062
-
 pH 7.4-8.3, 37°C Homo sapiens N-(4-(aminomethyl)phenyl)-6-carbamimidoyl-2-naphthamide trifluoro acetate
0.1
-
 pH 7.4-8.3, 37°C Homo sapiens 4-[(E)-(5-oxo-2-phenyl-1,3-oxazol-4(5H)-ylidene)methyl]benzenecarboximidamide
0.125
-
 pH 7.4-8.3, 37°C Homo sapiens 6-carbamimidoyl-N-phenyl-2-naphthamide