BRENDA - Enzyme Database show

Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target

Friesen, R.W.; Mancini, J.A.; J. Med. Chem. 51, 4059-4067 (2008)

Data extracted from this reference:

Activating Compound
EC Number
Activating Compound
Commentary
Organism
Structure
5.3.99.3
interleukin-1beta
-
Homo sapiens
5.3.99.3
LPS
-
Homo sapiens
Application
EC Number
Application
Commentary
Organism
5.3.99.3
medicine
mPGES-1 plays a role in atherosclerosis, stroke, inflammation, pain and fever
Homo sapiens
Inhibitors
EC Number
Inhibitors
Commentary
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
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
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
Primary Accession No. (UniProt)
Commentary
Textmining
5.3.99.3
Homo sapiens
-
-
-
Source Tissue
EC Number
Source Tissue
Commentary
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
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
5.3.99.3
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
693551
Homo sapiens
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
?
Cofactor
EC Number
Cofactor
Commentary
Organism
Structure
5.3.99.3
glutathione
-
Homo sapiens
IC50 Value
EC Number
IC50 Value
IC50 Value Maximum
Commentary
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
15-deoxy-DELTA12,14-prostaglandin J2
5.3.99.3
0.0003
-
-
Homo sapiens
arachidonic acid
5.3.99.3
0.0003
-
-
Homo sapiens
eicosapentaenoic acid
5.3.99.3
0.00039
-
-
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
Activating Compound (protein specific)
EC Number
Activating Compound
Commentary
Organism
Structure
5.3.99.3
interleukin-1beta
-
Homo sapiens
5.3.99.3
LPS
-
Homo sapiens
Application (protein specific)
EC Number
Application
Commentary
Organism
5.3.99.3
medicine
mPGES-1 plays a role in atherosclerosis, stroke, inflammation, pain and fever
Homo sapiens
Cofactor (protein specific)
EC Number
Cofactor
Commentary
Organism
Structure
5.3.99.3
glutathione
-
Homo sapiens
IC50 Value (protein specific)
EC Number
IC50 Value
IC50 Value Maximum
Commentary
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
15-deoxy-DELTA12,14-prostaglandin J2
5.3.99.3
0.0003
-
-
Homo sapiens
arachidonic acid
5.3.99.3
0.0003
-
-
Homo sapiens
eicosapentaenoic acid
5.3.99.3
0.00039
-
-
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
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
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) (protein specific)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
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
-
-
?
Source Tissue (protein specific)
EC Number
Source Tissue
Commentary
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) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
5.3.99.3
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
693551
Homo sapiens
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
?