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Literature summary extracted from
- Urethanyl-3-amidinophenylalanine derivatives as inhibitors of factor Xa. X-ray crystal structure of a trypsin/inhibitor complex and modeling studies (2000), Biol. Chem., 381, 321-329.
Application
| EC Number | Application | Comment | Organism |
|---|---|---|---|
| 3.4.21.6 | pharmacology | enzyme is a target for inhibitor design as anti-thrombotic agents | Bos taurus |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.4.21.6 | methyl 3-[3-[amino(imino)methyl]phenyl]-5-[4-[amino(imino)methyl]phenyl]pentanoate | - |
Bos taurus |  |
| 3.4.21.6 | additional information | inhibition mechanism, inhibitor binding | Bos taurus | |
| 3.4.21.6 | N-1-adamantylaminocarbonyl-D,L-3-amidinophenylalanine methyl ester | - |
Bos taurus | |
| 3.4.21.6 | N-1-adamantyloxycarbonyl-(R)-3-amidinophenylalanine-(2-phenyl)-1-ethylamide | - |
Bos taurus | |
| 3.4.21.6 | N-1-adamantyloxycarbonyl-(R)-D-3-amidinophenylalanine benzylamide | - |
Bos taurus | |
| 3.4.21.6 | N-1-adamantyloxycarbonyl-(R)-D-3-amidinophenylalanine methyl ester | - |
Bos taurus | |
| 3.4.21.6 | N-1-adamantyloxycarbonyl-(R)-L-3-amidinophenylalanine methyl ester | - |
Bos taurus | |
| 3.4.21.6 | N-1-adamantyloxycarbonyl-D,L-3-amidinophenylalanine | - |
Bos taurus | |
| 3.4.21.6 | N-1-adamantyloxycarbonyl-D,L-3-amidinophenylalanine methyl ester | - |
Bos taurus | |
| 3.4.21.6 | N-1-adamantyloxycarbonyl-D,L-3-amidinophenylalanine piperidine | - |
Bos taurus | |
| 3.4.21.6 | N-1-adamantyloxycarbonyl-D,L-4-amidinophenylalanine methyl ester | - |
Bos taurus | |
| 3.4.21.6 | N-1-adamantyloxycarbonyl-D,L-4-guanidinophenylalanine methyl ester | - |
Bos taurus | |
| 3.4.21.6 | N-9-fluorenemethyloxycarbonyl-D,L-3-amidinophenylalanine methyl ester | - |
Bos taurus | |
| 3.4.21.6 | N-benzyloxycarbonyl-D,L-3-amidinophenylalanine piperidine | - |
Bos taurus | |
| 3.4.21.6 | N-tert-butyloxycarbonyl-D,L-3-amidinophenylalanine methyl ester | - |
Bos taurus | |
| 3.4.21.6 | Nalpha-4'-amidinobenzensulfonyl-glycyl-D,L-4-amimidinophenylalanine ethyl ester | - |
Bos taurus | |
| 3.4.21.6 | Nalpha-tosylglycyl-D,L-3-amidinophenylalanine alkyl ester | - |
Bos taurus | |
Natural Substrates/ Products (Substrates)
| EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.4.21.6 | prothrombin + H2O | Bos taurus | - |
thrombin + ? | - |
? | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 3.4.21.6 | Bos taurus | - |
- |
- |
Reaction
| EC Number | Reaction | Comment | Organism | Reaction ID |
|---|---|---|---|---|
| 3.4.21.6 | selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin | scutelarin has similar specificity | Bos taurus |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 3.4.21.6 | commercial preparation | - |
Bos taurus | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.4.21.6 | prothrombin + H2O | - |
Bos taurus | thrombin + ? | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 3.4.21.6 | More | the enzyme belongs to the peptidase family S1, i.e. trypsin family | Bos taurus |
Temperature Optimum [°C]
| EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|---|
| 3.4.21.6 | 25 | - |
assay at | Bos taurus |
pH Optimum
| EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|---|
| 3.4.21.6 | 8 | - |
assay at | Bos taurus |
Ki Value [mM]
| EC Number | Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 3.4.21.6 | 0.0000034 | - |
methyl 3-[3-[amino(imino)methyl]phenyl]-5-[4-[amino(imino)methyl]phenyl]pentanoate | pH 8.0, 25°C | Bos taurus | |
| 3.4.21.6 | 0.000074 | - |
N-1-adamantyloxycarbonyl-(R)-3-amidinophenylalanine-(2-phenyl)-1-ethylamide | pH 8.0, 25°C | Bos taurus | |
| 3.4.21.6 | 0.00022 | - |
N-1-adamantyloxycarbonyl-(R)-D-3-amidinophenylalanine benzylamide | pH 8.0, 25°C | Bos taurus | |
| 3.4.21.6 | 0.00039 | - |
N-1-adamantyloxycarbonyl-(R)-D-3-amidinophenylalanine methyl ester | pH 8.0, 25°C | Bos taurus | |
| 3.4.21.6 | 0.0005 | - |
Nalpha-4'-amidinobenzensulfonyl-glycyl-D,L-4-amimidinophenylalanine ethyl ester | pH 8.0, 25°C | Bos taurus | |
| 3.4.21.6 | 0.00062 | - |
N-1-adamantyloxycarbonyl-D,L-3-amidinophenylalanine methyl ester | pH 8.0, 25°C | Bos taurus | |
| 3.4.21.6 | 0.00084 | - |
Nalpha-tosylglycyl-D,L-3-amidinophenylalanine alkyl ester | pH 8.0, 25°C | Bos taurus | |
| 3.4.21.6 | 0.0009 | - |
N-1-adamantylaminocarbonyl-D,L-3-amidinophenylalanine methyl ester | pH 8.0, 25°C | Bos taurus | |
| 3.4.21.6 | 0.0014 | - |
N-1-adamantyloxycarbonyl-D,L-4-amidinophenylalanine methyl ester | pH 8.0, 25°C | Bos taurus | |
| 3.4.21.6 | 0.0017 | - |
N-1-adamantyloxycarbonyl-D,L-3-amidinophenylalanine piperidine | pH 8.0, 25°C | Bos taurus | |
| 3.4.21.6 | 0.0021 | - |
N-1-adamantyloxycarbonyl-D,L-3-amidinophenylalanine | pH 8.0, 25°C | Bos taurus | |
| 3.4.21.6 | 0.0034 | - |
N-9-fluorenemethyloxycarbonyl-D,L-3-amidinophenylalanine methyl ester | pH 8.0, 25°C | Bos taurus | |
| 3.4.21.6 | 0.0046 | - |
N-1-adamantyloxycarbonyl-(R)-L-3-amidinophenylalanine methyl ester | pH 8.0, 25°C | Bos taurus | |
| 3.4.21.6 | 0.016 | - |
N-tert-butyloxycarbonyl-D,L-3-amidinophenylalanine methyl ester | pH 8.0, 25°C | Bos taurus | |
| 3.4.21.6 | 0.033 | - |
N-benzyloxycarbonyl-D,L-3-amidinophenylalanine piperidine | pH 8.0, 25°C | Bos taurus | |
| 3.4.21.6 | 1 | - |
N-1-adamantyloxycarbonyl-D,L-4-guanidinophenylalanine methyl ester | pH 8.0, 25°C | Bos taurus | |
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