Activating Compound | Comment | Organism | Structure |
---|---|---|---|
additional information | Ca2+-ionophore A23187 | Homo sapiens |
Application | Comment | Organism |
---|---|---|
drug development | pirinixic acid derivatives constitute a novel class of dual mPGES-1/5-lipoxygenase inhibitors with a promising pharmacologial profile and a potential for therapeutic use | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
Escherichia coli MV1190 transformed with pT3-5LO plasmid | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(E)-N-hydroxy-N-(3-(3-phenoxyphenyl)-allyl)acetamide | BWA4C | Homo sapiens | |
([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)(naphthalen-1-yl)acetic acid | - |
Homo sapiens | |
2-(4-(biphenyl-4-ylamino)-6-chloropyrimidine-2-ylthio)octanoic acid | - |
Homo sapiens | |
2-(4-(biphenyl-4-ylmethylamino)-6-chloropyrimidin-2-ylthio)octanoic acid | - |
Homo sapiens | |
2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)acetic acid | - |
Homo sapiens | |
2-(4-chloro-6-(4'-cyanobiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid | - |
Homo sapiens | |
2-(4-chloro-6-(5-methoxy-2-methylbiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid | - |
Homo sapiens | |
2-([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)octanoic acid | - |
Homo sapiens | |
2-[(4-[[3,5-bis(2,2,2-trifluoroethoxy)phenyl]amino]-6-chloropyrimidin-2-yl)sulfanyl]octanoic acid | - |
Homo sapiens | |
ethyl 2-[[4-chloro-6-(quinolin-6-ylamino)pyrimidin-2-yl]sulfanyl]octanoate | - |
Homo sapiens | |
additional information | class of dual microsomal PGE2 synthase-1/5-lipoxygenase inhibitors based on the structure of pirinixic acid. Target oriented structural modification of pirinixic acid, particularly R substitution with extended n-alkyl or bulky aryl substituents and concomitant replacement of the 2,3-dimethylaniline by a biphenyl-4-yl-methane-amino residue, results in potent suppression of mPGES-1 and 5-lipoxygenase activity. Is not inhibited by 3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl)-2,2-dimethylpropanoic acid | Homo sapiens | |
N-hydroxy-N-[(2E)-3-(3-phenoxyphenyl)prop-2-en-1-yl]acetamide | - |
Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
partially purified by sonication, centrifugation and gel filtration | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
polymorphonuclear leukocyte | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
arachidonate + O2 | - |
Homo sapiens | (6E,8Z,11Z,14Z)-(5S)-5-hydroperoxyicosa-6,8,11,14-tetraenoate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
5-lipoxygenase | - |
Homo sapiens |
5-LO | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00011 | - |
in intact polymorphonuclear leukocytes | Homo sapiens | N-hydroxy-N-[(2E)-3-(3-phenoxyphenyl)prop-2-en-1-yl]acetamide | |
0.00016 | - |
purified 5-lipoxygenase | Homo sapiens | N-hydroxy-N-[(2E)-3-(3-phenoxyphenyl)prop-2-en-1-yl]acetamide | |
0.0004 | - |
in intact polymorphonuclear leukocytes | Homo sapiens | 2-(4-chloro-6-(4'-cyanobiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid | |
0.0005 | - |
in intact polymorphonuclear leukocytes | Homo sapiens | 2-(4-chloro-6-(5-methoxy-2-methylbiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid | |
0.0006 | - |
in intact polymorphonuclear leukocytes | Homo sapiens | ethyl 2-[[4-chloro-6-(quinolin-6-ylamino)pyrimidin-2-yl]sulfanyl]octanoate | |
0.0007 | - |
in intact polymorphonuclear leukocytes | Homo sapiens | 2-(4-(biphenyl-4-ylamino)-6-chloropyrimidine-2-ylthio)octanoic acid | |
0.001 | - |
in intact polymorphonuclear leukocytes | Homo sapiens | 2-(4-(biphenyl-4-ylmethylamino)-6-chloropyrimidin-2-ylthio)octanoic acid | |
0.0015 | - |
in intact polymorphonuclear leukocytes | Homo sapiens | 2-[(4-[[3,5-bis(2,2,2-trifluoroethoxy)phenyl]amino]-6-chloropyrimidin-2-yl)sulfanyl]octanoic acid | |
0.0015 | - |
purified 5-lipoxygenase | Homo sapiens | 2-(4-(biphenyl-4-ylamino)-6-chloropyrimidine-2-ylthio)octanoic acid | |
0.0015 | - |
purified 5-lipoxygenase | Homo sapiens | 2-(4-chloro-6-(4'-cyanobiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid | |
0.002 | - |
purified 5-lipoxygenase | Homo sapiens | 2-(4-(biphenyl-4-ylmethylamino)-6-chloropyrimidin-2-ylthio)octanoic acid | |
0.002 | - |
purified 5-lipoxygenase | Homo sapiens | 2-(4-chloro-6-(5-methoxy-2-methylbiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid | |
0.003 | - |
purified 5-lipoxygenase | Homo sapiens | 2-[(4-[[3,5-bis(2,2,2-trifluoroethoxy)phenyl]amino]-6-chloropyrimidin-2-yl)sulfanyl]octanoic acid | |
0.0041 | - |
in intact polymorphonuclear leukocytes | Homo sapiens | 2-([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)octanoic acid | |
0.005 | - |
in intact polymorphonuclear leukocytes | Homo sapiens | ([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)(naphthalen-1-yl)acetic acid | |
0.0065 | - |
purified 5-lipoxygenase | Homo sapiens | 2-([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)octanoic acid | |
0.019 | - |
purified 5-lipoxygenase | Homo sapiens | ethyl 2-[[4-chloro-6-(quinolin-6-ylamino)pyrimidin-2-yl]sulfanyl]octanoate |