Cloned (Comment) | Organism |
---|---|
expression in Escherichia coli strain MV1190 | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-(2,4-difluorophenyl)-3-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)urea | - |
Homo sapiens | |
1-benzyl-3-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)urea | - |
Homo sapiens | |
1-[3-(methylsulfanyl)phenyl]-3-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)urea | - |
Homo sapiens | |
2-(2-methoxyphenyl)-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)acetamide | - |
Homo sapiens | |
2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-(5-methyl-1,3-thiazol-2-yl)propanamide | - |
Homo sapiens | |
2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-1,3-thiazol-2-ylpropanamide | - |
Homo sapiens | |
2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-pyridin-2-ylpropanamide | - |
Homo sapiens | |
2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-thiophen-3-ylpropanamide | - |
Homo sapiens | |
2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-(thiophen-2-ylmethyl)propanamide | - |
Homo sapiens | |
2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-1,3-thiazol-2-ylpropanamide | - |
Homo sapiens | |
2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-pyridin-2-ylpropanamide | - |
Homo sapiens | |
2-[5,8-dimethyl-7-(2-morpholin-4-ylethoxy)-1,2,3,4-tetrahydronaphthalen-2-yl]-N-1,3-thiazol-2-ylpropanamide | - |
Homo sapiens | |
2-[7-[2-(dimethylamino)ethoxy]-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl]-N-1,3-thiazol-2-ylpropanamide | - |
Homo sapiens | |
2-[7-[2-(dimethylamino)ethoxy]-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl]-N-pyridin-2-ylpropanamide | - |
Homo sapiens | |
3,4,5-trimethoxy-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)benzamide | - |
Homo sapiens | |
4-methoxy-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)benzamide | - |
Homo sapiens | |
4-methyl-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)-1,2,3-thiadiazole-5-carboxamide | - |
Homo sapiens | |
BWA4C | - |
Homo sapiens | |
additional information | virtual inhibitor screening, structure-function relationship analysis, overview | Homo sapiens | |
N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)-1,3-benzodioxole-5-carboxamide | - |
Homo sapiens | |
N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)cyclopentanecarboxamide | - |
Homo sapiens | |
N-(furan-2-ylmethyl)-2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)propanamide | - |
Homo sapiens | |
N-cyclopentyl-2-[7-(2-methoxyethoxy)-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl]propanamide | - |
Homo sapiens | |
N-tert-butyl-2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)propanamide | - |
Homo sapiens | |
ZM230487 | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
(6E,8Z,11Z,14Z)-(5S)-5-hydroperoxyeicosa-6,8,11,14-tetraenoate | Homo sapiens | - |
leukotriene A4 + H2O | is unstable and metabolized to leukotriene B4 | ? | |
arachidonic acid + O2 | Homo sapiens | - |
(6E,8Z,11Z,14Z)-(5S)-5-hydroperoxyeicosa-6,8,11,14-tetraenoate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
recombinant enzyme partially from Escherichia coli strain MV1190 by ammonium sulfate fractionation and ATP affinity chromatography | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
leukocyte | polymorphonuclear | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
(6E,8Z,11Z,14Z)-(5S)-5-hydroperoxyeicosa-6,8,11,14-tetraenoate | - |
Homo sapiens | leukotriene A4 + H2O | - |
? | |
(6E,8Z,11Z,14Z)-(5S)-5-hydroperoxyeicosa-6,8,11,14-tetraenoate | - |
Homo sapiens | leukotriene A4 + H2O | is unstable and metabolized to leukotriene B4 | ? | |
arachidonic acid + O2 | - |
Homo sapiens | (6E,8Z,11Z,14Z)-(5S)-5-hydroperoxyeicosa-6,8,11,14-tetraenoate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
5-lipoxygenase | - |
Homo sapiens |
5-LO | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0006 | - |
37°C, partially purified enzyme | Homo sapiens | 1-(2,4-difluorophenyl)-3-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)urea | |
0.0008 | - |
37°C, in intact polymorphonuclear leukocytes | Homo sapiens | 2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-1,3-thiazol-2-ylpropanamide | |
0.0008 | - |
37°C, partially purified enzyme | Homo sapiens | 2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-(5-methyl-1,3-thiazol-2-yl)propanamide | |
0.0008 | - |
37°C, partially purified enzyme | Homo sapiens | 2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-pyridin-2-ylpropanamide | |
0.0009 | - |
37°C, in intact polymorphonuclear leukocytes | Homo sapiens | 3,4,5-trimethoxy-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)benzamide | |
0.0009 | - |
37°C, intact polymorphonuclear leukocytes | Homo sapiens | 2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-pyridin-2-ylpropanamide | |
0.0009 | - |
37°C, partially purified enzyme | Homo sapiens | N-(furan-2-ylmethyl)-2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)propanamide | |
0.001 | - |
37°C, intact polymorphonuclear leukocytes | Homo sapiens | 2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-(5-methyl-1,3-thiazol-2-yl)propanamide | |
0.001 | - |
37°C, partially purified enzyme | Homo sapiens | 1-[3-(methylsulfanyl)phenyl]-3-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)urea | |
0.001 | - |
37°C, partially purified enzyme | Homo sapiens | 2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-1,3-thiazol-2-ylpropanamide | |
0.001 | - |
37°C, partially purified enzyme | Homo sapiens | 2-[7-[2-(dimethylamino)ethoxy]-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl]-N-1,3-thiazol-2-ylpropanamide | |
0.002 | - |
37°C, intact polymorphonuclear leukocytes | Homo sapiens | N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)-1,3-benzodioxole-5-carboxamide | |
0.003 | - |
37°C, intact polymorphonuclear leukocytes | Homo sapiens | 1-benzyl-3-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)urea | |
0.003 | - |
37°C, partially purified enzyme | Homo sapiens | 2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-thiophen-3-ylpropanamide | |
0.004 | - |
37°C, intact polymorphonuclear leukocytes | Homo sapiens | 1-[3-(methylsulfanyl)phenyl]-3-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)urea | |
0.004 | - |
37°C, intact polymorphonuclear leukocytes | Homo sapiens | 2-(2-methoxyphenyl)-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)acetamide | |
0.004 | - |
37°C, partially purified enzyme | Homo sapiens | N-tert-butyl-2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)propanamide | |
0.005 | - |
37°C, intact polymorphonuclear leukocytes | Homo sapiens | 2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-pyridin-2-ylpropanamide | |
0.006 | - |
37°C, intact polymorphonuclear leukocytes | Homo sapiens | 4-methoxy-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)benzamide | |
0.006 | - |
37°C, partially purified enzyme | Homo sapiens | 2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-pyridin-2-ylpropanamide | |
0.007 | - |
37°C, intact polymorphonuclear leukocytes | Homo sapiens | 1-(2,4-difluorophenyl)-3-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)urea | |
0.008 | - |
37°C, intact polymorphonuclear leukocytes | Homo sapiens | 2-(5,8-dimethyl-7-propoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-N-thiophen-3-ylpropanamide | |
0.008 | - |
37°C, intact polymorphonuclear leukocytes | Homo sapiens | 2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-(thiophen-2-ylmethyl)propanamide | |
0.008 | - |
37°C, intact polymorphonuclear leukocytes | Homo sapiens | N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)cyclopentanecarboxamide | |
0.01 | - |
37°C, intact polymorphonuclear leukocytes | Homo sapiens | 4-methyl-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)-1,2,3-thiadiazole-5-carboxamide | |
0.01 | - |
37°C, partially purified enzyme | Homo sapiens | 2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-(thiophen-2-ylmethyl)propanamide | |
0.01 | - |
37°C, partially purified enzyme | Homo sapiens | N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)cyclopentanecarboxamide | |
0.01 | - |
above, 37°C, intact polymorphonuclear leukocytes | Homo sapiens | 2-[7-[2-(dimethylamino)ethoxy]-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl]-N-1,3-thiazol-2-ylpropanamide | |
0.01 | - |
above, 37°C, intact polymorphonuclear leukocytes | Homo sapiens | N-(furan-2-ylmethyl)-2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)propanamide | |
0.01 | - |
above, 37°C, intact polymorphonuclear leukocytes | Homo sapiens | N-cyclopentyl-2-[7-(2-methoxyethoxy)-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl]propanamide | |
0.01 | - |
above, 37°C, intact polymorphonuclear leukocytes | Homo sapiens | N-tert-butyl-2-(7-methoxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl)propanamide | |
0.01 | - |
above, 37°C, partially purified enzyme | Homo sapiens | 1-benzyl-3-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)urea | |
0.01 | - |
above, 37°C, partially purified enzyme | Homo sapiens | 2-(2-methoxyphenyl)-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)acetamide | |
0.01 | - |
above, 37°C, partially purified enzyme | Homo sapiens | 3,4,5-trimethoxy-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)benzamide | |
0.01 | - |
above, 37°C, partially purified enzyme | Homo sapiens | 4-methoxy-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)benzamide | |
0.01 | - |
above, 37°C, partially purified enzyme | Homo sapiens | 4-methyl-N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)-1,2,3-thiadiazole-5-carboxamide | |
0.01 | - |
above, 37°C, partially purified enzyme | Homo sapiens | N-(3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d][1,3]thiazol-8-yl)-1,3-benzodioxole-5-carboxamide | |
0.01 | - |
above, 37°C, partially purified enzyme | Homo sapiens | N-cyclopentyl-2-[7-(2-methoxyethoxy)-5,8-dimethyl-1,2,3,4-tetrahydronaphthalen-2-yl]propanamide |