EC Number | Activating Compound | Comment | Organism | Structure |
---|---|---|---|---|
1.13.11.34 | additional information | Ca2+-ionophore A23187 | Homo sapiens |
EC Number | Application | Comment | Organism |
---|---|---|---|
1.13.11.34 | 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 |
5.3.99.3 | medicine | mPGES-1 is a potential target for inhibitors, pathological conditions, such as inflammation, pain, fever, anorexia, atherosclerosis, stroke, and tumorigenesis are related to elevated levels of PGE2 | Homo sapiens |
EC Number | Cloned (Comment) | Organism |
---|---|---|
1.13.11.34 | Escherichia coli MV1190 transformed with pT3-5LO plasmid | Homo sapiens |
EC Number | Inhibitors | Comment | Organism | Structure |
---|---|---|---|---|
1.13.11.34 | (E)-N-hydroxy-N-(3-(3-phenoxyphenyl)-allyl)acetamide | BWA4C | Homo sapiens | |
1.13.11.34 | ([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)(naphthalen-1-yl)acetic acid | - |
Homo sapiens | |
1.13.11.34 | 2-(4-(biphenyl-4-ylamino)-6-chloropyrimidine-2-ylthio)octanoic acid | - |
Homo sapiens | |
1.13.11.34 | 2-(4-(biphenyl-4-ylmethylamino)-6-chloropyrimidin-2-ylthio)octanoic acid | - |
Homo sapiens | |
1.13.11.34 | 2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)acetic acid | - |
Homo sapiens | |
1.13.11.34 | 2-(4-chloro-6-(4'-cyanobiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid | - |
Homo sapiens | |
1.13.11.34 | 2-(4-chloro-6-(5-methoxy-2-methylbiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid | - |
Homo sapiens | |
1.13.11.34 | 2-([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)octanoic acid | - |
Homo sapiens | |
1.13.11.34 | 2-[(4-[[3,5-bis(2,2,2-trifluoroethoxy)phenyl]amino]-6-chloropyrimidin-2-yl)sulfanyl]octanoic acid | - |
Homo sapiens | |
1.13.11.34 | ethyl 2-[[4-chloro-6-(quinolin-6-ylamino)pyrimidin-2-yl]sulfanyl]octanoate | - |
Homo sapiens | |
1.13.11.34 | 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 | |
1.13.11.34 | N-hydroxy-N-[(2E)-3-(3-phenoxyphenyl)prop-2-en-1-yl]acetamide | - |
Homo sapiens | |
5.3.99.3 | ([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)(5,8-dihydronaphthalen-1-yl)acetic acid | - |
Homo sapiens | |
5.3.99.3 | 2-([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid | - |
Homo sapiens | |
5.3.99.3 | 2-([4-chloro-6-[(4'-cyanobiphenyl-4-yl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid | - |
Homo sapiens | |
5.3.99.3 | 2-([4-chloro-6-[(5-methoxy-2-methylbiphenyl-4-yl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid | - |
Homo sapiens | |
5.3.99.3 | 2-([4-[(biphenyl-4-ylmethyl)amino]-6-chloropyrimidin-2-yl]sulfanyl)nonanoic acid | - |
Homo sapiens | |
5.3.99.3 | 2-[(4-[[3,5-bis(2,2,2-trifluoroethoxy)phenyl]amino]-6-chloropyrimidin-2-yl)sulfanyl]nonanoic acid | - |
Homo sapiens | |
5.3.99.3 | 2-[[4-(biphenyl-4-ylamino)-6-chloropyrimidin-2-yl]sulfanyl]nonanoic acid | - |
Homo sapiens | |
5.3.99.3 | 3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid | - |
Homo sapiens | |
5.3.99.3 | ethyl 2-[[4-chloro-6-(quinolin-6-ylamino)pyrimidin-2-yl]sulfanyl]nonanoate | - |
Homo sapiens |
EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
5.3.99.3 | (5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate | Homo sapiens | - |
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate | - |
? |
EC Number | Organism | UniProt | Comment | Textmining |
---|---|---|---|---|
1.13.11.34 | Homo sapiens | - |
- |
- |
5.3.99.3 | Homo sapiens | - |
- |
- |
EC Number | Purification (Comment) | Organism |
---|---|---|
1.13.11.34 | partially purified by sonication, centrifugation and gel filtration | Homo sapiens |
EC Number | Source Tissue | Comment | Organism | Textmining |
---|---|---|---|---|
1.13.11.34 | polymorphonuclear leukocyte | - |
Homo sapiens | - |
5.3.99.3 | A-549 cell | - |
Homo sapiens | - |
EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
1.13.11.34 | arachidonate + O2 | - |
Homo sapiens | (6E,8Z,11Z,14Z)-(5S)-5-hydroperoxyicosa-6,8,11,14-tetraenoate | - |
? | |
5.3.99.3 | (5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate | - |
Homo sapiens | (5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate | - |
? |
EC Number | Synonyms | Comment | Organism |
---|---|---|---|
1.13.11.34 | 5-lipoxygenase | - |
Homo sapiens |
1.13.11.34 | 5-LO | - |
Homo sapiens |
5.3.99.3 | microsomal prostaglandin E2 synthase-1 | - |
Homo sapiens |
5.3.99.3 | mPGES-1 | - |
Homo sapiens |
EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|---|
5.3.99.3 | 4 | - |
microsomal membranes are incubated with PGH2, enzyme activity assay | Homo sapiens |
EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|---|
5.3.99.3 | 7.4 | - |
microsomal membranes are incubated with PGH2, enzyme activity assay | Homo sapiens |
EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|---|
1.13.11.34 | 0.00011 | - |
in intact polymorphonuclear leukocytes | Homo sapiens | N-hydroxy-N-[(2E)-3-(3-phenoxyphenyl)prop-2-en-1-yl]acetamide | |
1.13.11.34 | 0.00016 | - |
purified 5-lipoxygenase | Homo sapiens | N-hydroxy-N-[(2E)-3-(3-phenoxyphenyl)prop-2-en-1-yl]acetamide | |
1.13.11.34 | 0.0004 | - |
in intact polymorphonuclear leukocytes | Homo sapiens | 2-(4-chloro-6-(4'-cyanobiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid | |
1.13.11.34 | 0.0005 | - |
in intact polymorphonuclear leukocytes | Homo sapiens | 2-(4-chloro-6-(5-methoxy-2-methylbiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid | |
1.13.11.34 | 0.0006 | - |
in intact polymorphonuclear leukocytes | Homo sapiens | ethyl 2-[[4-chloro-6-(quinolin-6-ylamino)pyrimidin-2-yl]sulfanyl]octanoate | |
1.13.11.34 | 0.0007 | - |
in intact polymorphonuclear leukocytes | Homo sapiens | 2-(4-(biphenyl-4-ylamino)-6-chloropyrimidine-2-ylthio)octanoic acid | |
1.13.11.34 | 0.001 | - |
in intact polymorphonuclear leukocytes | Homo sapiens | 2-(4-(biphenyl-4-ylmethylamino)-6-chloropyrimidin-2-ylthio)octanoic acid | |
1.13.11.34 | 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 | |
1.13.11.34 | 0.0015 | - |
purified 5-lipoxygenase | Homo sapiens | 2-(4-(biphenyl-4-ylamino)-6-chloropyrimidine-2-ylthio)octanoic acid | |
1.13.11.34 | 0.0015 | - |
purified 5-lipoxygenase | Homo sapiens | 2-(4-chloro-6-(4'-cyanobiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid | |
1.13.11.34 | 0.002 | - |
purified 5-lipoxygenase | Homo sapiens | 2-(4-(biphenyl-4-ylmethylamino)-6-chloropyrimidin-2-ylthio)octanoic acid | |
1.13.11.34 | 0.002 | - |
purified 5-lipoxygenase | Homo sapiens | 2-(4-chloro-6-(5-methoxy-2-methylbiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid | |
1.13.11.34 | 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 | |
1.13.11.34 | 0.0041 | - |
in intact polymorphonuclear leukocytes | Homo sapiens | 2-([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)octanoic acid | |
1.13.11.34 | 0.005 | - |
in intact polymorphonuclear leukocytes | Homo sapiens | ([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)(naphthalen-1-yl)acetic acid | |
1.13.11.34 | 0.0065 | - |
purified 5-lipoxygenase | Homo sapiens | 2-([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)octanoic acid | |
1.13.11.34 | 0.019 | - |
purified 5-lipoxygenase | Homo sapiens | ethyl 2-[[4-chloro-6-(quinolin-6-ylamino)pyrimidin-2-yl]sulfanyl]octanoate | |
5.3.99.3 | 0.0013 | - |
- |
Homo sapiens | 2-([4-[(biphenyl-4-ylmethyl)amino]-6-chloropyrimidin-2-yl]sulfanyl)nonanoic acid | |
5.3.99.3 | 0.0016 | - |
- |
Homo sapiens | 2-[[4-(biphenyl-4-ylamino)-6-chloropyrimidin-2-yl]sulfanyl]nonanoic acid | |
5.3.99.3 | 0.0017 | - |
- |
Homo sapiens | 2-([4-chloro-6-[(4'-cyanobiphenyl-4-yl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid | |
5.3.99.3 | 0.0021 | - |
- |
Homo sapiens | 2-([4-chloro-6-[(5-methoxy-2-methylbiphenyl-4-yl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid | |
5.3.99.3 | 0.0021 | - |
- |
Homo sapiens | 3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid | |
5.3.99.3 | 0.0026 | - |
- |
Homo sapiens | 2-[(4-[[3,5-bis(2,2,2-trifluoroethoxy)phenyl]amino]-6-chloropyrimidin-2-yl)sulfanyl]nonanoic acid | |
5.3.99.3 | 0.0039 | - |
- |
Homo sapiens | 2-([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid | |
5.3.99.3 | 0.0051 | - |
- |
Homo sapiens | ([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)(5,8-dihydronaphthalen-1-yl)acetic acid | |
5.3.99.3 | 0.0056 | - |
- |
Homo sapiens | ethyl 2-[[4-chloro-6-(quinolin-6-ylamino)pyrimidin-2-yl]sulfanyl]nonanoate |