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Literature summary for 5.3.99.3 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
Search for more literature for 5.3.99.3

Activating Compound

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

Application

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

Inhibitors

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
(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

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(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

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

Cofactor

Cofactor Comment Organism Structure
glutathione
-
 Homo sapiens

IC50 Value

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