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Literature summary for 3.4.21.7 extracted from

  • Al-Horani, R.; Karuturi, R.; White, D.; Desai, U.
    Plasmin regulation through allosteric, sulfated, small molecules (2015), Molecules, 20, 608-624 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.7

Inhibitors

Inhibitors Comment Organism Structure
(E)-5,5'-(but-2-ene-1,4-diylbis(oxy))bis(2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4Hchromen-4-one about 43% residual activity at 0.4 mM Homo sapiens
3-(8-(4-((2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4-oxo-4H-chromen-5-yloxy)methyl)-1H-1,2,3-triazol-1-yl)heptyl)-2-(4-O-sulfonato-phenyl)quinazolin-4(3H)-one about 1% residual activity at 0.4 mM Homo sapiens
3-(8-(4-((2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4-oxo-4H-chromen-5-yloxy)methyl)-1H-1,2,3-triazol-1-yl)octyl)-2-(4-O-sulfonato-phenyl)quinazolin-4(3H)-one about 2% residual activity at 0.4 mM Homo sapiens
5,5'-(butane-1,4-diylbis(oxy))bis(2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4H-chromen-4-one about 42% residual activity at 0.4 mM Homo sapiens
Aprotinin
-
 Homo sapiens
disodium 2-methoxy-4-[(1E)-3-[4-methyl-2-(sulfonatooxy)phenyl]-3-oxoprop-1-en-1-yl]phenyl sulfate about 73% residual activity at 0.4 mM Homo sapiens
disodium 2-methoxy-6-[(1E)-3-oxo-3-[2-(sulfonatooxy)phenyl]prop-1-en-1-yl]phenyl sulfate about 40% residual activity at 0.4 mM Homo sapiens
disodium 3,5-dimethoxy-2-[(2E)-3-[3-methoxy-4-(sulfonatooxy)phenyl]prop-2-enoyl]phenyl sulfate about 40% residual activity at 0.4 mM Homo sapiens
disodium 3,5-dimethoxy-2-[(2E)-3-[4-methoxy-3-(sulfonatooxy)phenyl]prop-2-enoyl]phenyl sulfate about 75% residual activity at 0.4 mM Homo sapiens
disodium 3-(4-oxo-3-[[1-(4-[4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate about 40% residual activity at 0.4 mM Homo sapiens
disodium 3-(acetyloxy)-5-(4-oxo-3-[4-[4-([4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]butyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate about 84% residual activity at 0.4 mM Homo sapiens
disodium 3-[4-oxo-3-[3-[4-([4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]propyl]quinazolin-2(4H)-yl]phenyl sulfate about 35% residual activity at 0.4 mM Homo sapiens
disodium 4-(4-oxo-3,4-dihydroquinazolin-2-yl)benzene-1,3-diyl disulfate about 77% residual activity at 0.4 mM Homo sapiens
disodium 4-(4-oxo-3-[5-[5-([4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]pentyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate about 25% residual activity at 0.4 mM; about 35% residual activity at 0.4 mM Homo sapiens
disodium 4-(4-oxo-3-[[1-(10-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]decyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate about 5% residual activity at 0.4 mM Homo sapiens
disodium 4-(4-oxo-3-[[1-(12-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]dodecyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate about 2% residual activity at 0.4 mM; about 30% residual activity at 0.4 mM; about 40% residual activity at 0.4 mM Homo sapiens
disodium 4-(4-oxo-3-[[1-(7-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]heptyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate about 30% residual activity at 0.4 mM Homo sapiens
disodium 4-[(2E)-3-(2-methoxyphenyl)prop-2-enoyl]benzene-1,3-diyl disulfate about 39% residual activity at 0.4 mM Homo sapiens
disodium 4-[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]benzene-1,3-diyl disulfate about 31% residual activity at 0.4 mM Homo sapiens
disodium 4-[4-oxo-3-[11-[4-([4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]undecyl]quinazolin-2(4H)-yl]phenyl sulfate about 3% residual activity at 0.4 mM Homo sapiens
disodium 4-[4-oxo-3-[8-[4-([4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]octyl]quinazolin-2(4H)-yl]phenyl sulfate about 7% residual activity at 0.4 mM Homo sapiens
disodium 4-[4-oxo-3-[9-[4-([4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]nonyl]quinazolin-2(4H)-yl]phenyl sulfate about 7% residual activity at 0.4 mM Homo sapiens
disodium 4-[4-oxo-6-(sulfonatooxy)-4H-chromen-2-yl]phenyl sulfate about 85% residual activity at 0.4 mM Homo sapiens
N-oleoyl heparin noncompetitive inhibition Homo sapiens
octasodium [(ethane-1,2-diyl)bis(oxy)[4-oxo-3,7-bis(sulfonatooxy)-4H-1-benzopyran-5,2-diyl]benzene-4,1,2-triyl] tetrasulfate about 16% residual activity at 0.4 mM; about 18% residual activity at 0.4 mM; about 65% residual activity at 0.4 mM Homo sapiens
octasodium [(propane-1,3-diyl)bis(oxy)[4-oxo-3,7-bis(sulfonatooxy)-4H-1-benzopyran-5,2-diyl]benzene-1,2,4-triyl] tetrasulfate about 30% residual activity at 0.4 mM Homo sapiens
pentasodium (2R)-2-[3,4-bis(sulfonatooxy)phenyl]-3,4-dihydro-2H-1-benzopyran-3,6,7-triyl trisulfate about 32% residual activity at 0.4 mM Homo sapiens
pentasodium 2-[3,4-bis(sulfonatooxy)phenyl]-4-oxo-5-[[1-(10-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]decyl)-1H-1,2,3-triazol-4-yl]methoxy]-4H-1-benzopyran-3,7-diyl disulfate about 5% residual activity at 0.4 mM Homo sapiens
pentasodium 2-[3-[2,5-bis(sulfonatooxy)phenyl]propanoyl]-5,8-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate about 73% residual activity at 0.4 mM Homo sapiens
pentasodium 2-[3-[2,5-bis(sulfonatooxy)phenyl]propanoyl]-6,7-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate about 60% residual activity at 0.4 mM Homo sapiens
pentasodium 2-[4-[2,5-bis(sulfonatooxy)phenyl]butanoyl]-5,8-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate about 78% residual activity at 0.4 mM Homo sapiens
pentasodium 2-[4-[2,5-bis(sulfonatooxy)phenyl]butanoyl]-6,7-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate about 80% residual activity at 0.4 mM Homo sapiens
pentasodium 2-[[2,5-bis(sulfonatooxy)phenyl]acetyl]-6,7-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate about 75% residual activity at 0.4 mM Homo sapiens
pentasopentasodium 2-[[2,5-bis(sulfonatooxy)phenyl]acetyl]-6,7-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylatedium 2-[[2,5-bis(sulfonatooxy)phenyl]acetyl]-6,7-bis(sulfonatooxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate about 70% residual activity at 0.4 mM Homo sapiens
sodium 2,6-diformyl-4-(4-oxo-3,4-dihydroquinazolin-2-yl)phenyl sulfate about 93% residual activity at 0.4 mM Homo sapiens
sodium 3-(3-[[1-(4-[2-[3-(acetyloxy)phenyl]-4-oxoquinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methyl]-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl sulfate about 55% residual activity at 0.4 mM Homo sapiens
sucrose octasulfate about 99% residual activity at 0.4 mM Homo sapiens
tetrasodium 2-[2,4-bis(sulfonatooxy)phenyl]-5-hydroxy-4-oxo-4H-chromene-3,7-diyl disulfate about 45% residual activity at 0.4 mM Homo sapiens
tetrasodium 2-[2-[6,7-bis(sulfonatooxy)-3,4-dihydroisoquinolin-2(1H)-yl]-2-oxoethyl]-1,4-phenylene disulfate about 60% residual activity at 0.4 mM Homo sapiens
tetrasodium 2-[3,4-bis(sulfonatooxy)phenyl]-4-oxo-4H-chromene-3,7-diyl disulfate about 99% residual activity at 0.4 mM Homo sapiens
tetrasodium 2-[4-[5,6-bis(sulfonatooxy)-3,4-dihydroisoquinolin-2(1H)-yl]-4-oxobutyl]-1,4-phenylene disulfate about 48% residual activity at 0.4 mM Homo sapiens
tetrasodium 4-[5-hydroxy-4-oxo-3,7-bis(sulfonatooxy)-4H-chromen-2-yl]benzene-1,2-diyl disulfate about 93% residual activity at 0.4 mM Homo sapiens
tetrasodium 5-methoxy-2-[3-[[1-(4-[2-[3-methoxy-4-(sulfonatooxy)phenyl]-4-oxoquinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methoxy]-4-(sulfonatooxy)phenyl]-4-oxo-4H-1-benzopyran-3,7-diyl disulfate about 3% residual activity at 0.4 mM; about 7% residual activity at 0.4 mM; about 8% residual activity at 0.4 mM Homo sapiens
tetrasodium 5-methoxy-4-oxo-2-[3-[[1-(4-[4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methoxy]-4-(sulfonatooxy)phenyl]-4H-1-benzopyran-3,7-diyl disulfate about 20% residual activity at 0.4 mM Homo sapiens
trisodium 2-[(1E)-3-[2,4-bis(sulfonatooxy)phenyl]-3-oxoprop-1-en-1-yl]phenyl sulfate about 42% residual activity at 0.4 mM Homo sapiens
trisodium 4-oxo-2-[3-(sulfonatooxy)phenyl]-4H-chromene-3,7-diyl disulfate about 82% residual activity at 0.4 mM Homo sapiens
trisodium 4-[(1E)-3-[2,4-bis(sulfonatooxy)phenyl]-3-oxoprop-1-en-1-yl]phenyl sulfate about 58% residual activity at 0.4 mM Homo sapiens
trisodium 4-[(1E)-3-[2,5-bis(sulfonatooxy)phenyl]-3-oxoprop-1-en-1-yl]-2-methoxyphenyl sulfate about 90% residual activity at 0.4 mM Homo sapiens
trisodium 4-[(1E)-3-[2,5-bis(sulfonatooxy)phenyl]-3-oxoprop-1-en-1-yl]phenyl sulfate about 51% residual activity at 0.4 mM Homo sapiens
trisodium 5-(4-oxo-3-[4-[4-([4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]butyl]-3,4-dihydroquinazolin-2-yl)-1,3-phenylene disulfate about 45% residual activity at 0.4 mM Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.04 0.07 Spectrozyme PL at pH 7.4 and 37°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Spectrozyme PL + H2O i.e. L-norleucyl-L-hexahydrotyrosyl-L-lysine-4-nitroanilide Homo sapiens L-norleucyl-L-hexahydrotyrosyl-L-lysine + 4-nitroaniline
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000016
-
 at pH 7.4 and 37°C Homo sapiens N-oleoyl heparin
0.045
-
 at pH 7.4 and 37°C Homo sapiens 3-(8-(4-((2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4-oxo-4H-chromen-5-yloxy)methyl)-1H-1,2,3-triazol-1-yl)octyl)-2-(4-O-sulfonato-phenyl)quinazolin-4(3H)-one
0.056
-
 at pH 7.4 and 37°C Homo sapiens 3-(8-(4-((2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4-oxo-4H-chromen-5-yloxy)methyl)-1H-1,2,3-triazol-1-yl)heptyl)-2-(4-O-sulfonato-phenyl)quinazolin-4(3H)-one
0.075
-
 at pH 7.4 and 37°C Homo sapiens (E)-5,5'-(but-2-ene-1,4-diylbis(oxy))bis(2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4Hchromen-4-one
0.076
-
 at pH 7.4 and 37°C Homo sapiens 5,5'-(butane-1,4-diylbis(oxy))bis(2-(3,4-O,O-disulfonato-phenyl)-3,7-O,O-disulfonato-4H-chromen-4-one
0.084
-
 at pH 7.4 and 37°C Homo sapiens trisodium 5-(4-oxo-3-[4-[4-([4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]butyl]-3,4-dihydroquinazolin-2-yl)-1,3-phenylene disulfate
0.089
-
 at pH 7.4 and 37°C Homo sapiens disodium 4-(4-oxo-3-[[1-(12-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]dodecyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
0.098
-
 at pH 7.4 and 37°C Homo sapiens disodium 4-(4-oxo-3-[[1-(10-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]decyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
0.111
-
 at pH 7.4 and 37°C Homo sapiens disodium 4-[4-oxo-3-[11-[4-([4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]undecyl]quinazolin-2(4H)-yl]phenyl sulfate
0.125
-
 at pH 7.4 and 37°C Homo sapiens disodium 4-(4-oxo-3-[5-[5-([4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]pentyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
0.128
-
 at pH 7.4 and 37°C Homo sapiens tetrasodium 5-methoxy-2-[3-[[1-(4-[2-[3-methoxy-4-(sulfonatooxy)phenyl]-4-oxoquinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methoxy]-4-(sulfonatooxy)phenyl]-4-oxo-4H-1-benzopyran-3,7-diyl disulfate
0.13
-
 at pH 7.4 and 37°C Homo sapiens pentasodium 2-[3,4-bis(sulfonatooxy)phenyl]-4-oxo-5-[[1-(10-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]decyl)-1H-1,2,3-triazol-4-yl]methoxy]-4H-1-benzopyran-3,7-diyl disulfate
0.137
-
 at pH 7.4 and 37°C Homo sapiens disodium 4-[4-oxo-3-[9-[4-([4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]nonyl]quinazolin-2(4H)-yl]phenyl sulfate
0.149
-
 at pH 7.4 and 37°C Homo sapiens tetrasodium 5-methoxy-4-oxo-2-[3-[[1-(4-[4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methoxy]-4-(sulfonatooxy)phenyl]-4H-1-benzopyran-3,7-diyl disulfate
0.157
-
 at pH 7.4 and 37°C Homo sapiens tetrasodium 5-methoxy-2-[3-[[1-(4-[2-[3-methoxy-4-(sulfonatooxy)phenyl]-4-oxoquinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methoxy]-4-(sulfonatooxy)phenyl]-4-oxo-4H-1-benzopyran-3,7-diyl disulfate
0.161
-
 at pH 7.4 and 37°C Homo sapiens disodium 4-(4-oxo-3-[[1-(7-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]heptyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
0.183
-
 at pH 7.4 and 37°C Homo sapiens disodium 4-[4-oxo-3-[8-[4-([4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]octyl]quinazolin-2(4H)-yl]phenyl sulfate
0.185
-
 at pH 7.4 and 37°C Homo sapiens octasodium [(ethane-1,2-diyl)bis(oxy)[4-oxo-3,7-bis(sulfonatooxy)-4H-1-benzopyran-5,2-diyl]benzene-4,1,2-triyl] tetrasulfate
0.209
-
 at pH 7.4 and 37°C Homo sapiens octasodium [(ethane-1,2-diyl)bis(oxy)[4-oxo-3,7-bis(sulfonatooxy)-4H-1-benzopyran-5,2-diyl]benzene-4,1,2-triyl] tetrasulfate
0.22
-
 at pH 7.4 and 37°C Homo sapiens tetrasodium 5-methoxy-2-[3-[[1-(4-[2-[3-methoxy-4-(sulfonatooxy)phenyl]-4-oxoquinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methoxy]-4-(sulfonatooxy)phenyl]-4-oxo-4H-1-benzopyran-3,7-diyl disulfate
0.239
-
 at pH 7.4 and 37°C Homo sapiens disodium 4-(4-oxo-3-[5-[5-([4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]pentyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
0.277
-
 at pH 7.4 and 37°C Homo sapiens disodium 4-(4-oxo-3-[[1-(12-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]dodecyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
0.4
-
 at pH 7.4 and 37°C Homo sapiens disodium 3-(4-oxo-3-[[1-(4-[4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
0.4
-
 at pH 7.4 and 37°C Homo sapiens disodium 3-[4-oxo-3-[3-[4-([4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]propyl]quinazolin-2(4H)-yl]phenyl sulfate
0.4
-
 at pH 7.4 and 37°C Homo sapiens octasodium [(propane-1,3-diyl)bis(oxy)[4-oxo-3,7-bis(sulfonatooxy)-4H-1-benzopyran-5,2-diyl]benzene-1,2,4-triyl] tetrasulfate
0.621
-
 at pH 7.4 and 37°C Homo sapiens disodium 4-(4-oxo-3-[[1-(12-[4-oxo-2-[4-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]dodecyl)-1H-1,2,3-triazol-4-yl]methyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
0.642
-
 at pH 7.4 and 37°C Homo sapiens sodium 3-(3-[[1-(4-[2-[3-(acetyloxy)phenyl]-4-oxoquinazolin-3(4H)-yl]butyl)-1H-1,2,3-triazol-4-yl]methyl]-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl sulfate
1
-
 at pH 7.4 and 37°C Homo sapiens disodium 3-(acetyloxy)-5-(4-oxo-3-[4-[4-([4-oxo-2-[3-(sulfonatooxy)phenyl]quinazolin-3(4H)-yl]methyl)-1H-1,2,3-triazol-1-yl]butyl]-3,4-dihydroquinazolin-2-yl)phenyl sulfate
2.83
-
 at pH 7.4 and 37°C Homo sapiens octasodium [(ethane-1,2-diyl)bis(oxy)[4-oxo-3,7-bis(sulfonatooxy)-4H-1-benzopyran-5,2-diyl]benzene-4,1,2-triyl] tetrasulfate