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Literature summary extracted from

  • Friesen, R.W.; Mancini, J.A.
    Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target (2008), J. Med. Chem., 51, 4059-4067.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
5.3.99.3 interleukin-1beta
-
Homo sapiens
5.3.99.3 LPS
-
Homo sapiens

Application

EC Number Application Comment Organism
5.3.99.3 medicine mPGES-1 plays a role in atherosclerosis, stroke, inflammation, pain and fever Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.3 15-deoxy-DELTA12,14-prostaglandin J2
-
Homo sapiens
5.3.99.3 2-(2-chloro-6-fluorophenyl)-9-fluoro-3,6-dihydro-7H-benzo[h]imidazo[4,5-f]isoquinolin-7-one
-
Homo sapiens
5.3.99.3 2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
-
Homo sapiens
5.3.99.3 2-[6-(2-cyclopropylethoxy)-9-(3-hydroxy-3-methylbutyl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
-
Homo sapiens
5.3.99.3 2-[6-bromo-9-(3-hydroxy-3-methylbut-1-yn-1-yl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
-
Homo sapiens
5.3.99.3 2-[6-chloro-9-(3-hydroxy-3-methylbut-1-yn-1-yl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
-
Homo sapiens
5.3.99.3 2-[6-chloro-9-(3-hydroxy-3-methylbutyl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
-
Homo sapiens
5.3.99.3 3-(1-benzothiophen-2-yl)-2-bromo-5-hydroxycyclopent-2-en-1-one
-
Homo sapiens
5.3.99.3 3-benzamidocarbazole
-
Homo sapiens
5.3.99.3 3-[1-(4-chlorobenzyl)-5-(2-fluoro-5-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
Homo sapiens
5.3.99.3 3-[1-(4-chlorobenzyl)-5-(2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
Homo sapiens
5.3.99.3 3-[3-(benzylsulfanyl)-1-(4-chlorobenzyl)-5-[4-[(4-chloro-2-fluorophenyl)ethynyl]phenyl]-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
Homo sapiens
5.3.99.3 4-(4-chlorobenzyl)-2,6-bis[4-(trifluoromethoxy)phenyl]-4H-thieno[3,2-b]pyrrole
-
Homo sapiens
5.3.99.3 5-(4-cyclohexylphenyl)-1-[4-(1-methylethoxy)benzyl]-1H-indole-2-carboxylic acid
-
Homo sapiens
5.3.99.3 5-(4-tert-butylphenyl)-1-[4-(1-methylethoxy)benzyl]-1H-indole-2-carboxylic acid
-
Homo sapiens
5.3.99.3 5-(4-tert-butylphenyl)-3-[4-(1-methylethoxy)phenyl]-1-[4-[(1-methylethyl)amino]benzyl]-1H-indole-2-carboxylic acid
-
Homo sapiens
5.3.99.3 7-hydroxy-N,N'-bis(2,4,6-trimethylphenyl)naphthalene-1,3-disulfonamide
-
Homo sapiens
5.3.99.3 acetaminophen
-
Homo sapiens
5.3.99.3 arachidonic acid
-
Homo sapiens
5.3.99.3 biarylimidazole
-
Homo sapiens
5.3.99.3 cysteinyl leukotriene LTC4
-
Homo sapiens
5.3.99.3 eicosapentaenoic acid
-
Homo sapiens
5.3.99.3 methyl 4-[6-bromo-2-(2-chloro-6-fluorophenyl)-1H-phenanthro[9,10-d]imidazol-9-yl]but-3-ynoate
-
Homo sapiens
5.3.99.3 MK-886
-
Homo sapiens
5.3.99.3 N-[4-chloro-3-(5-methyl-1,3-benzoxazol-2-yl)phenyl]-2-(trifluoromethyl)benzamide
-
Homo sapiens
5.3.99.3 NS-398
-
Homo sapiens
5.3.99.3 resveratrol
-
Homo sapiens
5.3.99.3 sulindac sulfide
-
Homo sapiens

Natural Substrates/ Products (Substrates)

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
-
?

Organism

EC Number Organism UniProt Comment Textmining
5.3.99.3 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
5.3.99.3 brain
-
Homo sapiens
-
5.3.99.3 heart
-
Homo sapiens
-
5.3.99.3 kidney
-
Homo sapiens
-
5.3.99.3 lung
-
Homo sapiens
-
5.3.99.3 seminal vesicle
-
Homo sapiens
-
5.3.99.3 spleen
-
Homo sapiens
-
5.3.99.3 stomach
-
Homo sapiens
-
5.3.99.3 testis
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) 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
-
?

Synonyms

EC Number Synonyms Comment Organism
5.3.99.3 microsomal prostaglandin E2 synthase-1
-
Homo sapiens
5.3.99.3 mPGES-1
-
Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
5.3.99.3 glutathione
-
Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.3.99.3 0.0000007
-
-
Homo sapiens 2-[6-chloro-9-(3-hydroxy-3-methylbutyl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
5.3.99.3 0.0000008
-
-
Homo sapiens biarylimidazole
5.3.99.3 0.0000009
-
-
Homo sapiens 2-[6-(2-cyclopropylethoxy)-9-(3-hydroxy-3-methylbutyl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
5.3.99.3 0.0000009
-
-
Homo sapiens 2-[6-bromo-9-(3-hydroxy-3-methylbut-1-yn-1-yl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
5.3.99.3 0.0000009
-
-
Homo sapiens 2-[6-chloro-9-(3-hydroxy-3-methylbut-1-yn-1-yl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
5.3.99.3 0.000001
-
-
Homo sapiens 2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
5.3.99.3 0.0000017
-
-
Homo sapiens methyl 4-[6-bromo-2-(2-chloro-6-fluorophenyl)-1H-phenanthro[9,10-d]imidazol-9-yl]but-3-ynoate
5.3.99.3 0.00006
-
-
Homo sapiens 3-[3-(benzylsulfanyl)-1-(4-chlorobenzyl)-5-[4-[(4-chloro-2-fluorophenyl)ethynyl]phenyl]-1H-indol-2-yl]-2,2-dimethylpropanoic acid
5.3.99.3 0.0003
-
-
Homo sapiens arachidonic acid
5.3.99.3 0.0003
-
-
Homo sapiens eicosapentaenoic acid
5.3.99.3 0.0003
-
-
Homo sapiens 15-deoxy-DELTA12,14-prostaglandin J2
5.3.99.3 0.00039
-
-
Homo sapiens 4-(4-chlorobenzyl)-2,6-bis[4-(trifluoromethoxy)phenyl]-4H-thieno[3,2-b]pyrrole
5.3.99.3 0.0011
-
-
Homo sapiens 7-hydroxy-N,N'-bis(2,4,6-trimethylphenyl)naphthalene-1,3-disulfonamide
5.3.99.3 0.0012
-
-
Homo sapiens cysteinyl leukotriene LTC4
5.3.99.3 0.0013
-
-
Homo sapiens N-[4-chloro-3-(5-methyl-1,3-benzoxazol-2-yl)phenyl]-2-(trifluoromethyl)benzamide
5.3.99.3 0.0018
-
-
Homo sapiens 3-(1-benzothiophen-2-yl)-2-bromo-5-hydroxycyclopent-2-en-1-one
5.3.99.3 0.002
-
-
Homo sapiens 3-benzamidocarbazole
5.3.99.3 0.0032
-
-
Homo sapiens MK-886
5.3.99.3 0.02
-
-
Homo sapiens NS-398
5.3.99.3 0.044
-
-
Homo sapiens acetaminophen
5.3.99.3 0.08
-
-
Homo sapiens sulindac sulfide