Application | Comment | Organism |
---|---|---|
drug development | the enzyme is an attractive target for the development of small molecule active site inhibitors | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-[2-(7-amino-4-chloro-1-oxo-1H-isochromen-3-yloxy)ethyl]isothiourea hydrobromide | - |
Homo sapiens | |
2-[2-(7-benzamido-4-chloro-1-oxo-1H-isochromen-3-yloxy)ethyl]isothiourea hydrobromide | - |
Homo sapiens | |
2-[3-(7-amino-4-chloro-1-oxo-1H-isochromen-3-yloxy)propyl]isothiourea hydrobromide | - |
Homo sapiens | |
2-[3-(7-benzamido-4-chloro-1-oxo-1H-isochromen-3-yloxy]propyl)isothiourea hydrobromide | - |
Homo sapiens | |
3-(2-bromoethoxy)-7-nitro-1H-isochromen-1-one | - |
Homo sapiens | |
3-(3-bromopropoxy)-4-trifluoroacetyl-1H-isochromen-1-one | - |
Homo sapiens | |
3-(3-bromopropoxy)-7-nitro-1H-isochromen-1-one | - |
Homo sapiens | |
4-chloro-3-alkoxyisocoumarin | competitive reversible inhibition | Homo sapiens | |
7-amino-3-(2-bromoethoxy)-1H-isochromen-1-one | - |
Homo sapiens | |
additional information | development of potent uncharged inhibitors of uPA based upon the isocoumarin scaffold, bromine occupies the same position as positively charged arginino mimetic groups, structure activity relationships, inhibitor synthesis and molecular modeling, overview | Homo sapiens | |
N-[3-(2-bromoethoxy)-4-chloro-1-oxo-1H-isochromen-7-yl]benzamide | - |
Homo sapiens | |
N-[3-(3-bromopropoxy)-4-chloro-1-oxo-1H-isochromen-7-yl]benzamide | competitive reversible inhibition mechanism, the bromine occupies the same position as positively charged arginino mimetic groups, molecular modeling | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Homo sapiens | the enzyme plays a major role in extracellular proteolytic events associated with tumor cell growth, migration and angiogenesis | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | the enzyme plays a major role in extracellular proteolytic events associated with tumor cell growth, migration and angiogenesis | Homo sapiens | ? | - |
? | |
additional information | structure activity relationship | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
uPA | - |
Homo sapiens |
Urokinase-type plasminogen activator | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
8.8 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00001 | - |
2-[3-(7-benzamido-4-chloro-1-oxo-1H-isochromen-3-yloxy]propyl)isothiourea hydrobromide | pH 8.8, 25°C | Homo sapiens | |
0.00002 | - |
2-[2-(7-amino-4-chloro-1-oxo-1H-isochromen-3-yloxy)ethyl]isothiourea hydrobromide | pH 8.8, 25°C | Homo sapiens | |
0.000034 | - |
N-[3-(3-bromopropoxy)-4-chloro-1-oxo-1H-isochromen-7-yl]benzamide | pH 8.8, 25°C | Homo sapiens | |
0.000038 | - |
2-[3-(7-amino-4-chloro-1-oxo-1H-isochromen-3-yloxy)propyl]isothiourea hydrobromide | pH 8.8, 25°C | Homo sapiens | |
0.000084 | - |
2-[2-(7-benzamido-4-chloro-1-oxo-1H-isochromen-3-yloxy)ethyl]isothiourea hydrobromide | pH 8.8, 25°C | Homo sapiens | |
0.0014 | - |
N-[3-(2-bromoethoxy)-4-chloro-1-oxo-1H-isochromen-7-yl]benzamide | pH 8.8, 25°C | Homo sapiens | |
0.0042 | - |
3-(2-bromoethoxy)-7-nitro-1H-isochromen-1-one | pH 8.8, 25°C | Homo sapiens | |
0.0043 | - |
3-(3-bromopropoxy)-7-nitro-1H-isochromen-1-one | pH 8.8, 25°C | Homo sapiens | |
0.014 | - |
3-(3-bromopropoxy)-4-trifluoroacetyl-1H-isochromen-1-one | pH 8.8, 25°C | Homo sapiens | |
0.065 | - |
7-amino-3-(2-bromoethoxy)-1H-isochromen-1-one | pH 8.8, 25°C | Homo sapiens |