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Information on EC 5.3.99.3 - prostaglandin-E synthase and Organism(s) Homo sapiens and UniProt Accession Q9H7Z7
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5.3.99.3 prostaglandin-E synthaseIUBMB Comments
Brings about the opening of the epidioxy bridge. Requires glutathione.
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Word Map
- 5.3.99.3
- cox-2
-
cyclooxygenase
-
arachidonic
- synthases
-
prostanoids
- lipopolysaccharide
- tnf
- lps
- phospholipase
-
eicosanoids
-
lps-induced
- pain
- endometrium
-
leukotriene
- prostacyclin
-
thromboxane
-
nsaids
- indomethacin
-
pgf2alpha
-
5-lipoxygenase
- il-1beta
- celecoxib
-
nonsteroidal
- interleukin-1beta
-
luteolysis
- luteal
- platinum
- 15-pgdh
-
estrous
-
postictal
- medicine
-
rhodium
-
pencil
- palladium
- drug development
-
6-keto-pgf1alpha
-
automobile
- pghs-2
-
prostaglandin-endoperoxide
-
e-prostanoid
-
ictal
-
pge2-dependent
- l-pgds
- 15-hydroxyprostaglandin
-
lipocalin-type
- akr1b1
-
cox-2-dependent
-
6-keto
-
coxibs
-
6-keto-pgf1
- ptgds
-
cox-derived
The taxonomic range for the selected organisms is: Homo sapiens
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria, Archaea
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria, Archaea
Reaction Schemes
=
Synonyms
mpges-1, pges, microsomal prostaglandin e synthase-1, mpges, pge synthase, ptges, prostaglandin e synthase, mpges-2, cpges, mpges1, 
more
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
endoperoxide isomerase
-
-
-
-
Isomerase, prostaglandin R2 E-
-
-
-
-
microsomal prostaglandin E synthase 1
microsomal prostaglandin E synthase-1
microsomal prostaglandin E2 synthase-1
mPGES-1
MPGES1
PGE isomerase
-
-
-
-
PGE2 isomerase
-
-
-
-
PGH-PGE isomerase
-
-
-
-
PGH2/PGE2 isomerase
-
-
-
-
prostagandin-E synthetase
-
-
-
-
Prostaglandin E synthase
prostaglandin E synthase 1
Prostaglandin E2 isomerase
-
-
-
-
Prostaglandin endoperoxide E isomerase
-
-
-
-
Prostaglandin endoperoxide E2 isomerase
-
-
-
-
Prostaglandin endoperoxide-E isomerase
-
-
-
-
Prostaglandin H-E isomerase
-
-
-
-
Prostaglandin H-prostaglandin E isomerase
-
-
-
-
Prostaglandin R-prostaglandin E isomerase
-
-
-
-
Prostaglandin-H2 E-isomerase
-
-
-
-
microsomal prostaglandin E synthase-1
-
-
microsomal prostaglandin E synthase-1
-
microsomal prostaglandin E2 synthase-1
-
-
mPGES-1
-
-
mPGES-1
-
Prostaglandin E synthase
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
isomerization
intramolecular oxidation
-
-
-
-
isomerization
-
-
-
-
PATHWAY SOURCE
PATHWAYS
BRENDA
-
-, -, -, -
SYSTEMATIC NAME
IUBMB Comments
(5Z,13E)-(15S)-9alpha,11alpha-Epidioxy-15-hydroxyprosta-5,13-dienoate E-isomerase
Brings about the opening of the epidioxy bridge. Requires glutathione.
CAS REGISTRY NUMBER
COMMENTARY
52227-79-9
-
SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
(5Z,13E)-(15S)-9a,11a-epidioxy-15-hydroxyprosta-5,13-dienoate + GSH
(5Z,13E)-(15S)-11a,15-dihydroxyprosta-5,13-dienoate + GSSG
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate + GSH
(5Z,13E)-(15S)-11alpha,15-dihydroxyprosta-5,13-dienoate + GSSG
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate + reduced glutathione
(5Z,13E)-(15S)-11alpha,15-dihydroxyprosta-5,13-dienoate + oxidized glutathione
i.e. prostaglandin H2
i.e. prostaglandin E2
?
(5Z,13E,15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E,15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
1-chloro-2,4-dinitrobenzene + GSH
?
-
glutathione S-transferase activity
-
?
5-hydroperoxyeicosatetraenoic acid + 2 GSH
5-hydroxyeicosatetraenoic acid + GSSG + H2O
-
-
-
?
prostaglandin G2
15-hydroperoxy-prostaglandin E2
-
at pH 7.5, 2.5 mM glutathione and 10 microM substrate
-
-
?
(5Z,13E)-(15S)-9a,11a-epidioxy-15-hydroxyprosta-5,13-dienoate + GSH
(5Z,13E)-(15S)-11a,15-dihydroxyprosta-5,13-dienoate + GSSG
-
-
-
-
?
(5Z,13E)-(15S)-9a,11a-epidioxy-15-hydroxyprosta-5,13-dienoate + GSH
(5Z,13E)-(15S)-11a,15-dihydroxyprosta-5,13-dienoate + GSSG
-
i.e. prostaglandin H2
i.e. prostaglandin E2
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
PGH2
PGE2
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate + GSH
(5Z,13E)-(15S)-11alpha,15-dihydroxyprosta-5,13-dienoate + GSSG
-
i.e. prostaglandin H2
i.e. prostaglandin E2
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate + GSH
(5Z,13E)-(15S)-11alpha,15-dihydroxyprosta-5,13-dienoate + GSSG
i.e. prostaglandin H2
i.e. prostaglandin E2
?
Prostaglandin H2
Prostaglandin E2
-
-
660669, 662071, 667959, 668886, 670732, 702158, 702165, 702622, 703593, 706521, 714421, 714468, 715100, 715541, 715856, 715865, 747278, 748368, 748441, 748542, 748846
-
-
?
Prostaglandin H2
Prostaglandin E2
-
at pH 7.5, 2.5 mM glutathione and 10 microM substrate
-
-
?
Prostaglandin H2
Prostaglandin E2
-
mPGES-1 is a gonadotropin-regulated enzyme
-
-
?
additional information
?
-
-
platelet-derived growth factor-induced increase in enzyme activity occurs within min after exposure to the growth factor
-
-
?
additional information
?
-
-
glutathione-heme-complex bound enzyme catalyzes formation of 12(S)-hydroxy-5(Z),8(E),10(E)-heptadecatrienoic acid and malonaldehyde from prostaglandin H2, i.e. shows lyase activity
-
-
?
additional information
additional information
-
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate, PGH2, mutation R126A/Q creates a glutathione-dependent reductase which is able to convert prostaglandin H2 to prostaglandin F2alpha
(5Z,13E)-(15S)-9alpha,11alpha,15-trihydroxyprosta-5,13-dienoate, PGF2alpha
-
?
additional information
additional information
-
-
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate, PGH2, mutation R126A/Q creates a glutathione-dependent reductase which is able to convert prostaglandin H2 to prostaglandin F2alpha
(5Z,13E)-(15S)-9alpha,11alpha,15-trihydroxyprosta-5,13-dienoate, PGF2alpha
-
?
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
additional information
?
-
-
platelet-derived growth factor-induced increase in enzyme activity occurs within min after exposure to the growth factor
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
PGH2
PGE2
-
?
Prostaglandin H2
Prostaglandin E2
-
-
667959, 670732, 702158, 702622, 703593, 706521, 715541, 715856, 747278, 748368, 748441, 748542, 748846
-
-
?
Prostaglandin H2
Prostaglandin E2
-
mPGES-1 is a gonadotropin-regulated enzyme
-
-
?
COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
heme
-
crystallization data of red-coloured protein purified after growth of recombinant Escherichia coli in LB medium containing delta-aminolevulinate and Fe(NO3)3. Heme is complexed with bound glutathione forming a S-Fe coordination bond with no polar interaction with enzyme. Heme dissociation constant is 0.00053 mM
additional information
mutants R126A/Q possess glutathione-dependent reductase activity
-
additional information
-
mutants R126A/Q possess glutathione-dependent reductase activity
-
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(1-benzyl-4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl)acetic acid
-
35% inhibition at 0.001 mM
(2E)-2-(2,5-bis[2-[4-(trifluoromethyl)phenyl]ethoxy]benzylidene)hexanoic acid
-
-
(2E)-2-(2,5-bis[[4-(trifluoromethyl)benzyl]oxy]benzylidene)hexanoic acid
-
55.1% residual activity at 0.01 mM
(2E)-2-[4-[3-(2,3-dimethylphenoxy)propoxy]benzylidene]hexanoic acid
-
28.3% residual activity at 0.01 mM
(2E)-2-[5-(2-cyclohexylethoxy)-2-[[4-(trifluoromethyl)benzyl]oxy]benzylidene]hexanoic acid
-
74% residual activity at 0.01 mM
(3R)-1-(7-chloro-2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazolin-6-yl)pyrrolidin-3-yl acetate
-
(3S)-1-(7-chloro-2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazolin-6-yl)pyrrolidin-3-yl acetate
-
(4-dodecanoyl-1,3,5-trimethyl-1H-pyrrol-2-yl)acetic acid
-
22% inhibition at 0.001 mM
(4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl)acetic acid
-
17% inhibition at 0.001 mM
(4E)-4-[2-(3-bromophenyl)hydrazin-1-ylidene]-1-ethanethioyl-3-methyl-4,5-dihydro-1H-pyrazol-5-one
-
-
(4R)-1-(8-chloroquinolin-2-yl)-N-[cis-4-(hydroxymethyl)cyclohexyl]-3,3-dimethylpiperidine-4-carboxamide
-
-
(4R)-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-[4-(trifluoromethyl)phenyl]piperidine-4-carboxamide
-
-
(4S)-1-(8-chloroquinolin-2-yl)-N-[cis-4-(hydroxymethyl)cyclohexyl]-3,3-dimethylpiperidine-4-carboxamide
-
-
(4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)-N-[(3S)-oxan-3-yl]piperidine-4-carboxamide
-
-
(4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)-N-[(3S)-oxolan-3-yl]piperidine-4-carboxamide
-
-
(4S)-3,3-dimethyl-N-(3-methylbutan-2-yl)-1-(8-methylquinolin-2-yl)piperidine-4-carboxamide
-
-
(4S)-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-[4-(trifluoromethyl)phenyl]piperidine-4-carboxamide
-
-
(4S)-N-[(3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-(8-methylquinolin-2-yl)piperidine-4-carboxamide
-
-
([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)(5,8-dihydronaphthalen-1-yl)acetic acid
-
-
([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)acetic acid
-
75.4% residual activity at 0.01 mM
1,5-anhydro-2,3,4-trideoxy-3-[[(4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)piperidine-4-carbonyl]amino]-D-glycero-hexitol
-
-
1-(7-chloro-2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazolin-6-yl)-N-methylpiperidine-4-carboxamide
76% inhibition at 0.01 mM
1-benzyl-4-dodecanoyl-3,5-dimethyl-1H-pyrrole-2-carboxylic acid
-
65% inhibition at 0.001 mM
1-[2-(2-methylphenyl)ethyl]-4-[2'-[(naphthalen-1-yloxy)methyl]biphenyl-4-yl]-1H-1,2,3-triazole
-
90% residual activity at 0.03 mM
1-[4-[2-(2-carboxy-2-methylpropyl)-1-(4-chlorobenzyl)-3-methyl-1H-indol-4-yl]-2-fluorophenyl]pyridinium
-
-
1-[5-chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide
1-[6-(4-chlorophenyl)-5-methyl-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide
-
-
2-(2,6-dichloroanilino)-7,7-dimethyl-N-(2,2,2-trifluoroethyl)-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-7,7-dimethyl-N-(2,2,3,3,3-pentafluoropropyl)-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-7,7-dimethyl-N-phenyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-7,7-dimethyl-N-[6-(trifluoromethyl)pyridin-3-yl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-7-methyl-N-[3-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-7-methyl-N-[4-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-N-(2,6-dimethylpyridin-3-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-N-(2-fluorophenyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-N-(4,4-difluorocyclohexyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-N-(4-fluorophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-N-(6-methoxypyridin-3-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-N-[(4-fluorophenyl)methyl]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-N-(3-cyanophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-N-(4-cyanophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-N-(4-fluorophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-N-(4-fluorophenyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-N-(5-chloropyridin-2-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-N-(cyclohexylmethyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-N-[3-fluoro-5-(trifluoromethyl)phenyl]-1-methyl-7,8-dihydro-1H-[1,4]dioxino[2,3-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-N-[6-(difluoromethoxy)pyridin-3-yl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluorophenyl)-7-phenyl-1,5-dihydro-4H-naphtho[1,2-d]imidazol-4-one
-
2-(2-chloro-6-fluorophenyl)-9-fluoro-3,6-dihydro-7H-benzo[h]imidazo[4,5-f]isoquinolin-7-one
-
-
2-(4-dodecanoyl-3,5-dimethyl-1-phenylpyrrol-2-yl)acetic acid
-
23% inhibition at 0.001 mM
2-(difluoromethyl)-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
-
-
2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[5-methyl-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
2-(difluoromethyl)-N-(1H-imidazol-2-yl)-5-([[(2R)-2-methylbutanoyl]amino]methyl)benzamide
-
-
2-(difluoromethyl)-N-(1H-imidazol-2-yl)-5-[(2-methylpropanamido)methyl]benzamide
-
-
2-(difluoromethyl)-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]-5-(propanamidomethyl)pyridine-3-carboxamide
-
-
2-(trifluoromethyl)-N-(3-[[5-(trifluoromethyl)pyridin-2-yl]carbamoyl]phenyl)benzamide
-
2-([4,6-bis[2-(4-methoxyphenyl)ethoxy]pyrimidin-2-yl]sulfanyl)hexanoic acid
-
63.7% residual activity at 0.01 mM
2-([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid
-
-
2-([4-chloro-6-[(4'-cyanobiphenyl-4-yl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid
-
-
2-([4-chloro-6-[(5-methoxy-2-methylbiphenyl-4-yl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid
-
-
2-([4-[(biphenyl-4-ylmethyl)amino]-6-chloropyrimidin-2-yl]sulfanyl)nonanoic acid
-
-
2-([4-[3-(2-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
88.3% residual activity at 0.01 mM
2-([4-[3-(3-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
59.1% residual activity at 0.01 mM
2-([4-[3-(3-methylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
58% residual activity at 0.01 mM
2-([4-[3-(5,6,7,8-tetrahydronaphthalen-1-yloxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
-
2-chloro-4-fluoro-N-(1H-imidazol-2-yl)-5-[(2-methylpropanamido)methyl]benzamide
-
CEP-32496
2-chloro-4-[(2,2-dimethylpropanamido)methyl]-N-[3-[4-(trifluoromethyl)anilino][1,2]thiazolo[4,5-b]pyridin-7-yl]benzamide
-
2-chloro-5-[(2,2-dimethylpropanamido)methyl]-N-[4-oxo-3-[4-(trifluoromethyl)phenyl]-3,4-dihydrophthalazin-6-yl]benzamide
-
2-chloro-6-fluoro-N-[3-[4-(trifluoromethyl)anilino][1,2]thiazolo[4,5-b]pyridin-7-yl]benzamide
-
2-chloro-N-(1H-imidazol-2-yl)-4-methyl-5-[(2-methylpropanamido)methyl]benzamide
-
-
2-chloro-N-[3-(naphthalen-1-ylcarbamoyl)phenyl]benzamide
-
selective for human over rat MPGES1
2-methyl-2-(cis-4-[[1-(3-methyl-5-phenylfuro[2,3-b]pyridin-6-yl)piperidine-4-carbonyl]amino]cyclohexyl)propanoic acid
-
-
2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-N-(3-methylbutyl)-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-N-[4-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-[(3,5-dichloropyridin-4-yl)amino]-N-[(4-fluorophenyl)methyl]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-[(3,5-dichloropyridin-4-yl)amino]-N-[2-fluoro-4-(trifluoromethyl)phenyl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-[(3,5-dichloropyridin-4-yl)amino]-N-[4-fluoro-3-(trifluoromethyl)phenyl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-[(4,6-bis[2-[4-(trifluoromethoxy)phenyl]ethoxy]pyrimidin-2-yl)sulfanyl]hexanoic acid
-
88.3% residual activity at 0.01 mM
2-[(4,6-bis[2-[4-(trifluoromethyl)phenyl]ethoxy]pyrimidin-2-yl)sulfanyl]hexanoic acid
-
-
2-[(4-[3-[4-chloro-3-(trifluoromethyl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
-
-
2-[(4-[[3,5-bis(2,2,2-trifluoroethoxy)phenyl]amino]-6-chloropyrimidin-2-yl)sulfanyl]nonanoic acid
-
-
2-[2,4-bis(2-phenylethoxy)benzyl]hexanoic acid
-
90.1% residual activity at 0.01 mM
2-[2-(2-chloro-6-fluorophenyl)-4-[6-(phenylethynyl)pyridin-3-yl]-1H-imidazol-5-yl]ethanol
-
-
2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazoline-7-carboxamide
16% inhibition at 0.01 mM
2-[2-[(1S,2S)-2-([1-[4-(trifluoromethoxy)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]pyridine-3-carboxylic acid
-
2-[2-[(1S,2S)-2-([1-[5-(trifluoromethyl)pyridin-2-yl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
2-[2-[(1S,2S)-2-[[1-(8-methylquinolin-2-yl)piperidine-4-carbonyl]amino]cyclopentyl]ethyl]benzoic acid
-
2-[3-(aminooxy)-2,2-dimethyl-3-oxopropyl]-3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indole
-
IC50: 0.01 mM
2-[4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)phenyl]propan-2-ol
-
-
2-[6-(2-cyclopropylethoxy)-9-(3-hydroxy-3-methylbutyl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
-
-
2-[6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl] acetic acid
-
licofelone, ML3000
2-[6-bromo-9-(3-hydroxy-3-methylbut-1-yn-1-yl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
-
-
2-[6-chloro-9-(3-hydroxy-3-methylbut-1-yn-1-yl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
-
-
2-[6-chloro-9-(3-hydroxy-3-methylbutyl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
-
-
2-[[4,6-bis(2-cycloheptylethoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
-
62.4% residual activity at 0.01 mM
2-[[4,6-bis(2-cyclopentylethoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
-
90% residual activity at 0.01 mM
2-[[4,6-bis(3-methylbutoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
-
54.5% residual activity at 0.01 mM
2-[[4-(3-phenoxypropoxy)phenyl]sulfanyl]hexanoic acid
-
81.9% residual activity at 0.01 mM
3-(1,3,5-trimethyl-4-octadecanoyl-1H-pyrrol-2-yl)propanoic acid
-
97% inhibition at 0.001 mM
3-(1,3,5-trimethyl-4-tetradecanoyl-1H-pyrrol-2-yl)propanoic acid
-
91% inhibition at 0.001 mM
3-(1-benzyl-4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl)propanoic acid
-
62% inhibition at 0.001 mM
3-(1-benzyl-4-dodecanoyl-5-methyl-3-phenylpyrrol-2-yl)propionic acid
-
64% inhibition at 0.001 mM
3-(4-dodecanoyl-1,3,5-trimethyl-1H-pyrrol-2-yl)propanoic acid
-
54% inhibition at 0.001 mM
3-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)-N-(benzenesulfonyl)propanamide
-
77% inhibition at 0.001 mM
3-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)-N-(methanesulfonyl)propanamide
-
52% inhibition at 0.001 mM
3-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)propanamide
-
39% inhibition at 0.001 mM
3-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)propanehydrazide
-
35% inhibition at 0.001 mM
3-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)propanenitrile
-
22% inhibition at 0.001 mM
3-(4-dodecanoyl-3,5-dimethyl-1-phenylpyrrol-2-yl)propionic acid
-
65% inhibition at 0.001 mM
3-(4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl)propanoic acid
-
38% inhibition at 0.001 mM
3-(4-hexadecanoyl-1,3,5-trimethyl-1H-pyrrol-2-yl)propanoic acid
-
97% inhibition at 0.001 mM
3-[(5E)-3-(4-butylbenzyl)-1-(4-chlorobenzyl)-4-methylidene-5-[(2E)-4-methylpent-2-en-1-ylidene]-4,5-dihydro-1H-pyrrol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.00029 mM
3-[1-(4-carbamoylbenzyl)-4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl]propanoic acid
-
28% inhibition at 0.001 mM
3-[1-(4-chlorobenzyl)-3-(3,3-dimethylbutanoyl)-4-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzyl)-3-(3,3-dimethylbutanoyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.00025 mM
3-[1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.0032 mM
3-[1-(4-chlorobenzyl)-3-methyl-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.0011 mM
3-[1-(4-chlorobenzyl)-3-methyl-5-phenyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.00060 mM
3-[1-(4-chlorobenzyl)-3-methyl-7-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.0043 mM
3-[1-(4-chlorobenzyl)-3-t-butyl-thio-5-isopropylindol-2-yl]-2,2-dimethylpropanoic acid
-
MK-886
3-[1-(4-chlorobenzyl)-4-(2'-chloro-2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzyl)-4-(2,2'-difluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzyl)-4-(2-chlorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzyl)-4-(2-fluoro-2'-methoxybiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzyl)-4-(2-fluoro-2'-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzyl)-4-(2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzyl)-4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl]propanoic acid
-
78% inhibition at 0.001 mM
3-[1-(4-chlorobenzyl)-5-(1-methylethyl)-3-phenoxy-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.00065 mM
3-[1-(4-chlorobenzyl)-5-(1-methylethyl)-3-phenyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.0064 mM
3-[1-(4-chlorobenzyl)-5-(1-methylethyl)-3-[(2-methylphenyl)carbonyl]-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.00090 mM
3-[1-(4-chlorobenzyl)-5-(2'-chloro-2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000004 mM
3-[1-(4-chlorobenzyl)-5-(2,2'-difluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000008 mM
3-[1-(4-chlorobenzyl)-5-(2-chlorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000022 mM
3-[1-(4-chlorobenzyl)-5-(2-fluoro-2'-methoxybiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000005 mM
3-[1-(4-chlorobenzyl)-5-(2-fluoro-2'-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000003 mM
3-[1-(4-chlorobenzyl)-5-(2-fluoro-3'-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000033 mM
3-[1-(4-chlorobenzyl)-5-(2-fluoro-4'-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000031 mM
3-[1-(4-chlorobenzyl)-5-(2-fluoro-5-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzyl)-5-(2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
3-[1-(4-chlorobenzyl)-5-(3-fluoro-4-pyridin-3-ylphenyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000012 mM
3-[1-(4-chlorobenzyl)-5-fluoro-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.0026 mM
3-[1-(4-chlorobenzyl)-5-[2-fluoro-2'-(phenylcarbonyl)biphenyl-4-yl]-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000006 mM
3-[1-(4-chlorobenzyl)-5-[3-fluoro-4-(pyrimidin-5-ylmethyl)phenyl]-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000032 mM
3-[1-(p-chlorobenzvl)-5-isopropyl-3-tert-butylthioindol-2-yl]-2,2-dimethylpropanoic acid
-
i.e. 3-[1-(p-chlorobenzvl)-5-isopropyl-3-tert-butylthioindol-2-yl]-2,2-dimethylpropanoic acid or FLAP, formerly designated L-663,536, a lipoxygenase inhibitor, IC50: 0.0016 mM
3-[3-(benzylsulfanyl)-1-(4-chlorobenzyl)-5-[4-[(4-chloro-2-fluorophenyl)ethynyl]phenyl]-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(propan-2-yl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
3-[3-(tert-butylsulfanyl)-1-methyl-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.01 mM
3-[3-(tert-butylsulfanyl)-5-(1-methylethyl)-1-(3-phenylpropyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.0032 mM
3-[3-(tert-butylsulfanyl)-5-(1-methylethyl)-1-prop-2-en-1-yl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.0067 mM
3-[3-(tert-butylsulfanyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.01 mM
3-[3-[(tert-butylsulfanyl)acetyl]-1-(4-chlorobenzyl)-4-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[3-[(tert-butylsulfanyl)acetyl]-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.00026 mM
3-[4-(2'-acetyl-2-fluorobiphenyl-4-yl)-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[4-(4-butoxybenzoyl)-1,3,5-trimethyl-1H-pyrrol-2-yl]propanoic acid
-
32% inhibition at 0.001 mM
3-[4-biphenyl-4-yl-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[4-dodecanoyl-1-(4-hydroxybenzyl)-3,5-dimethyl-1H-pyrrol-2-yl]propanoic acid
-
53% inhibition at 0.001 mM
3-[4-dodecanoyl-1-(4-methoxybenzyl)-3,5-dimethyl-1H-pyrrol-2-yl]propanoic acid
-
72% inhibition at 0.001 mM
3-[4-dodecanoyl-3,5-dimethyl-1-(4-methylbenzyl)-1H-pyrrol-2-yl]propanoic acid
-
52% inhibition at 0.001 mM
3-[4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]propanoic acid
-
83.9% residual activity at 0.01 mM
3-[5-biphenyl-3-yl-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.00016 mM
3-[5-biphenyl-4-yl-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000016 mM
3-[5-tert-butyl-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.00033 mM
3-[6-([1,1'-biphenyl]-4-yl)-1-[(4-chlorophenyl)methyl]-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
4'-[1-(3-phenylpropyl)-1H-1,2,3-triazol-4-yl]biphenyl-4-ol
-
73.6% residual activity at 0.03 mM
4'-[1-[(phenylsulfanyl)methyl]-1H-1,2,3-triazol-4-yl]biphenyl-3-ol
-
60.1% residual activity at 0.03 mM
4'-[1-[(phenylsulfanyl)methyl]-1H-1,2,3-triazol-4-yl]biphenyl-4-ol
-
89% residual activity at 0.03 mM
4'-[1-[2-(2-methylphenyl)ethyl]-1H-1,2,3-triazol-4-yl]biphenyl-4-amine
-
98.2% residual activity at 0.03 mM
4-(2'-[[2-chloro-5-(trifluoromethyl)phenoxy]methyl]biphenyl-4-yl)-1-(3-phenylpropyl)-1H-1,2,3-triazole
-
91.9% residual activity at 0.03 mM
4-(2'-[[2-chloro-5-(trifluoromethyl)phenoxy]methyl]biphenyl-4-yl)-1-[2-(2-methylphenyl)ethyl]-1H-1,2,3-triazole
-
87.9% residual activity at 0.03 mM
4-(3-chlorobenzyl)-2,6-bis[4-(trifluoromethoxy)phenyl]-4H-thieno[3,2-b]pyrrole-5-carboxylic acid
-
-
4-(4'-phenoxybiphenyl-4-yl)-1-(3-phenylpropyl)-1H-1,2,3-triazole
-
88.7% residual activity at 0.03 mM
4-(4-chlorobenzyl)-2,6-bis[4-(trifluoromethoxy)phenyl]-4H-thieno[3,2-b]pyrrole
-
-
4-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)butanoic acid
-
70% inhibition at 0.001 mM
4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzamide
-
-
4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzoic acid
-
-
4-chloro-2-([[(1S,2S)-2-(2,2-dimethylpropanamido)cyclopentyl]methyl]amino)benzoic acid
-
4-chloro-2-([[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]methyl]amino)benzoic acid
-
4-chloro-2-[([(1S,2S)-2-[(1-phenylpiperidine-4-carbonyl)amino]cyclopentyl]methyl)amino]benzoic acid
-
4-chloro-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
4-chloro-2-[[(1R,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]methoxy]benzoic acid
-
4-dodecanoyl-3,5-dimethyl-1-phenylpyrrole-2-carboxylic acid
-
99% inhibition at 0.001 mM
4-dodecanoyl-3,5-dimethyl-1H-pyrrole-2-carboxylic acid
-
62% inhibition at 0.001 mM
4-fluoro-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
4-methyl-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
4-[(4-[2'-[(naphthalen-1-yloxy)methyl]biphenyl-4-yl]-1H-1,2,3-triazol-1-yl)sulfonyl]benzoic acid
-
59.8% residual activity at 0.03 mM
4-[2'-[(naphthalen-1-yloxy)methyl]biphenyl-4-yl]-1-(3-phenylpropyl)-1H-1,2,3-triazole
-
96.8% residual activity at 0.03 mM
4-[4-(phenanthren-9-yl)phenyl]-1-(3-phenylpropyl)-1H-1,2,3-triazole
-
78.2% residual activity at 0.03 mM
4-[4-benzyl-1-[(phenylsulfanyl)methyl]-1H-1,2,3-triazol-5-yl]benzaldehyde
-
72.1% residual activity at 0.03 mM
4-[[2-(2-carboxyethyl)-4-dodecanoyl-3,5-dimethyl-1H-pyrrol-1-yl]methyl]benzoic acid
-
27% inhibition at 0.001 mM
4-[[4-(biphenyl-4-yl)-1H-1,2,3-triazol-1-yl]methyl]-3-nitrobenzoic acid
-
most efficient inhibitor of mPGES-1, 12% residual activity at 0.03 mM
5-(4-cyclohexylphenyl)-1-[4-(1-methylethoxy)benzyl]-1H-indole-2-carboxylic acid
-
-
5-(4-tert-butylphenyl)-1-[4-(1-methylethoxy)benzyl]-1H-indole-2-carboxylic acid
-
-
5-(4-tert-butylphenyl)-3-[4-(1-methylethoxy)phenyl]-1-[4-[(1-methylethyl)amino]benzyl]-1H-indole-2-carboxylic acid
-
-
5-(acetamidomethyl)-2-(difluoromethyl)-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
-
-
5-(dimethylamino)-N-[4'-[1-(3-phenylpropyl)-1H-1,2,3-triazol-4-yl]biphenyl-4-yl]naphthalene-1-sulfonamide
-
85% residual activity at 0.03 mM
5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)-2-(trifluoromethyl)benzamide
-
-
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(1,3-thiazol-2-ylethynyl)pyridine
-
-
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclohex-1-en-1-ylethynyl)pyridine
-
-
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclohexylethynyl)pyridine
-
-
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclopropylethynyl)pyridine
-
-
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(pyridin-3-ylethynyl)pyridine
-
-
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(2-chlorophenyl)ethynyl]pyridine
-
-
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(3-chlorophenyl)ethynyl]pyridine
-
-
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(4-chlorophenyl)ethynyl]pyridine
-
-
5-[2-(2-chloro-6-fluorophenyl)-5-methyl-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
-
-
5-[5-(2-chloro-6-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-(phenylethynyl)pyridine
-
-
5-[5-chloro-2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
-
-
aminomethyl 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzenesulfinate
-
-
dexamethasone
-
inhibition of cytokine-induced expression of isoform mPGES-1, while isoforms mPGES-2 and cPGES remain unaffected
ethyl 2-([4-[3-(5,6,7,8-tetrahydronaphthalen-1-yloxy)propoxy]phenyl]sulfanyl)hexanoate
-
-
ethyl 2-([4-[3-(quinolin-6-yloxy)propoxy]phenyl]sulfanyl)hexanoate
-
83.9% residual activity at 0.01 mM
methyl 3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoate
-
IC50: 0.0072 mM
methyl 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzenesulfinate
-
-
methyl 4-[6-bromo-2-(2-chloro-6-fluorophenyl)-1H-phenanthro[9,10-d]imidazol-9-yl]but-3-ynoate
-
-
N-(2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazolin-7-yl)cyclopropanecarboxamide
74% inhibition at 0.01 mM
N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-1,1-dioxo-1,2-dihydro-1lambda~6~,2-benzothiazine-3-carboxamide
N-(3-chloro-2-methylphenyl)-6-[2-chloro-6-(trifluoromethyl)benzamido]-2-(methoxymethyl)-1H-benzimidazole-4-carboxamide
-
N-(4-bromophenyl)-2-[2-chloro-5-[(2,2-dimethylpropanamido)methyl]anilino]-6-(2,2-difluoroethoxy)-1-methyl-1H-benzimidazole-5-carboxamide
-
N-(4-chloro-2-fluorophenyl)-2-[2,6-dichloro-3-[(2,2-dimethylpropanamido)methyl]anilino]-6-(2,2-difluoroethoxy)-1-methyl-1H-benzimidazole-5-carboxamide
-
N-(cyclohexylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
N-(cyclohexylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
N-(cyclopentylmethyl)-2-(2,6-dichloroanilino)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
N-(cyclopropylmethyl)-2-(2,6-dichloroanilino)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
N-(cyclopropylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
N-([3-[(4-chlorophenyl)ethynyl]phenyl]methyl)-N'-propan-2-yl-N-([3-[(pyridin-4-yl)ethynyl]phenyl]methyl)urea
-
N-([4-chloro-3-[4-oxo-7-(trifluoromethyl)-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
-
N-([4-chloro-3-[7-chloro-4-oxo-6-(3-oxopiperazin-1-yl)-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
79% inhibition at 0.01 mM
N-([4-chloro-3-[7-chloro-4-oxo-6-(pyridin-4-yl)-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
-
N-([4-chloro-3-[7-chloro-6-(4-hydroxypiperidin-1-yl)-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
-
N-([4-chloro-3-[7-chloro-6-(4-methylpiperazin-1-yl)-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
75% inhibition at 0.01 mM
N-([4-chloro-3-[7-chloro-6-(morpholin-4-yl)-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
-
N-cyclohexyl-2-(2,6-dichloroanilino)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
N-cyclohexyl-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
N-cyclohexyl-2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
N-cyclopentyl-1-[5,6-diamino-1-(3-amino-4-fluorophenyl)-1H-benzimidazol-2-yl]piperidine-4-carboxamide
-
-
N-tert-butyl-1-(7-chloro-2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazolin-6-yl)azetidine-3-carboxamide
-
N-[(4-chloro-3-[4-oxo-6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
-
N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl]phenyl)methyl]-2-methylpropanamide
-
N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
-
N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)piperidin-1-yl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
-
N-[(4-chloro-3-[4-oxo-7-[6-(trifluoromethyl)pyridin-3-yl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
-
N-[(4-chloro-3-[7-chloro-4-oxo-6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
-
N-[(4-chloro-3-[7-chloro-6-[(3R)-3-hydroxypyrrolidin-1-yl]-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
95% inhibition at 0.01 mM
N-[(4-chloro-3-[7-chloro-6-[(3S)-3-hydroxypyrrolidin-1-yl]-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
91% inhibition at 0.01 mM
N-[(4-chloro-3-[7-chloro-6-[4-(difluoromethyl)piperidin-1-yl]-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
-
N-[(6-chloro-5-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydropyrido[4,3-d]pyrimidin-2-yl]pyridin-3-yl)methyl]-2-methylpropanamide
-
N-[3-(4-bromophenyl)-4-oxo-3,4-dihydrophthalazin-6-yl]-2-chloro-6-fluorobenzamide
-
N-[3-[(4-bromophenyl)carbamoyl]-4-(2,2-difluoroethoxy)phenyl]-2-chloro-5-[(2,2-dimethylpropanamido)methyl]benzamide
-
N-[4-chloro-3-(5-methyl-1,3-benzoxazol-2-yl)phenyl]-2-(trifluoromethyl)benzamide
-
-
N-[5-(4-chlorophenyl)-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]benzamide
-
-
N-[5-(4-chlorophenyl)-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]pyridine-3-carboxamide
-
-
N-[5-(4-chlorophenyl)-4-methyl-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]pyridine-3-carboxamide
-
-
N-[[3-(7-amino-4-oxo-3,4-dihydroquinazolin-2-yl)-4-chlorophenyl]methyl]-2-methylpropanamide
70% inhibition at 0.01 mM
N-[[3-(7-bromo-4-oxo-3,4-dihydroquinazolin-2-yl)-4-chlorophenyl]methyl]-2-methylpropanamide
-
N-[[4-chloro-3-(4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
67% inhibition at 0.01 mM
N-[[4-chloro-3-(7-chloro-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
-
N-[[4-chloro-3-(7-chloro-6-cyclopropyl-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
-
N-[[4-chloro-3-(7-chloro-6-methoxy-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
-
N-[[4-chloro-3-(7-fluoro-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
98% inhibition at 0.01 mM
N-[[4-chloro-3-(7-methoxy-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
-
N-[[4-chloro-3-(7-nitro-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
-
N-[[6-(difluoromethyl)-5-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydropyrido[4,3-d]pyrimidin-2-yl]pyridin-3-yl]methyl]-2-methylpropanamide
-
N-[[6-(difluoromethyl)-5-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]pyridin-3-yl]methyl]-2-methylpropanamide
-
sodium 3-[1-[(4-chlorophenyl)methyl]-5-(2-fluoro[1,1'-biphenyl]-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoate
-
-
[1-[(phenylsulfanyl)methyl]-1H-1,2,3-triazol-4-yl]methyl benzoate
-
76.1% residual activity at 0.03 mM
[[4,6-bis(2-phenylethoxy)pyrimidin-2-yl]sulfanyl]acetic acid
-
66.4% residual activity at 0.01 mM
1-[5-chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide
-
1-[5-chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide
PF-4693627
2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
-
fludrocortisone
2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
MF-63
2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
-
-
2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
-
2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[5-methyl-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
-
-
2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[5-methyl-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
-
2-chloro-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
-
3-(4-dodecanoyl-1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)propanoic acid
-
90% inhibition at 0.001 mM
3-[1-(4-chlorobenzyl)-5-(2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzyl)-5-(2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000007 mM
3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(propan-2-yl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
75% inhibition at 0.01 mM
3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(propan-2-yl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
12% residual activity at 0.03 mM
4-dodecanoyl-1,3,5-trimethyl-1H-pyrrole-2-carboxylic acid
-
37% inhibition at 0.001 mM
4-dodecanoyl-1,3,5-trimethyl-1H-pyrrole-2-carboxylic acid
-
59% inhibition at 0.001 mM
5-[5-bromo-2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
-
-
5-[5-bromo-2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
-
MF63
i.e. 2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-isophthalonitrile
MK-886
-
inhibition of cytokine-induced expression of isoform mPGES-1, while isoforms mPGES-2 and cPGES remain unaffected
MK-886
-
i.e. 3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl)-2,2-dimethylpropanoic acid
N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-1,1-dioxo-1,2-dihydro-1lambda~6~,2-benzothiazine-3-carboxamide
-
N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-1,1-dioxo-1,2-dihydro-1lambda~6~,2-benzothiazine-3-carboxamide
PF-1984
PF-9184
-
potent, competitive and reversible mPGES-1 inhibitor, i.e. N-(3',4'-dichlorobiphenyl-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide
additional information
-
structure-activity relationship analysis of inhibitors
-
additional information
-
not inhibited by BWA4C, i.e. (E)-N-hydroxy-N-(3-(3-phenoxyphenyl)-allyl)acetamide
-
additional information
-
pyrrole alkanoic acid derivatives as nuisance inhibitors of microsomal prostaglandin E2 synthase-1, overview. No inhibition at 0.001 mM by 3-(4-butanoyl-1,3,5-trimethyl-1H-pyrrol-2-yl)propanoic acid, 3-(4-heptanoyl-1,3,5-trimethyl-1H-pyrrol-2-yl)propanoic acid, 3-(1,3,5-trimethyl-4-octanoyl-1H-pyrrol-2-yl)propanoic acid, 3-(4-decanoyl-1,3,5-trimethyl-1H-pyrrol-2-yl)propanoic acid, 3-[1,3,5-trimethyl-4-[2-(octyloxy)benzoyl]-1H-pyrrol-2-yl]propanoic acid, 3-[4-(3-heptyloxybenzoyl)-1,3,5-trimethylpyrrol-2-yl]propionic acid, 3-(4-benzoyl-1,3,5-trimethyl-1H-pyrrol-2-yl)propanoic acid, 3-[1,3,5-trimethyl-4-(naphthalen-1-ylcarbonyl)-1H-pyrrol-2-yl]propanoic acid, 3-[1,3,5-trimethyl-4-(naphthalen-2-ylcarbonyl)-1H-pyrrol-2-yl]propanoic acid, 3-[4-(2-ethylbenzoyl)-1,3,5-trimethyl-1H-pyrrol-2-yl]propanoic acid, 3-[4-(4-ethylbenzoyl)-1,3,5-trimethyl-1H-pyrrol-2-yl]propanoic acid, 3-[4-(4-benzylbenzoyl)-1,3,5-trimethyl-1H-pyrrol-2-yl]propanoic acid, 4-dodecanoyl-1-methyl-1H-pyrrole-2-carboxylic acid, (4-dodecanoyl-1-methyl-1H-pyrrol-2-yl)acetic acid, and 3-(4-dodecanoyl-1-methyl-1H-pyrrol-2-yl)propanoic acid
-
additional information
-
synthesis and inhibitory potency of a series of 6-nitro-3-(m-tolylamino) benzo[d]isothiazole 1,1-dioxide analogues against microsomal prostaglandin E2 synthase. No inhibition by Zileuton
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
epigallocatechin gallate
-
enhances COX-2 and isoform mPGES-1 gene expression and production of prostaglandin E2. Induction of mPGES-1 is mediated by active ERK1/2MAP kinases and early growth response gene 1
Tumor necrosis factor alpha
-
increase in protein expression and activity of isoform mPGES-1, accompanied by increased COX-2 expression and production of prostaglandin E2
-
interleukin 1beta
-
increase in protein expression and activity of isoform mPGES-1, accompanied by increased COX-2 expression and production of prostaglandin E2
-
interleukin 1beta
induces isoform mPGES-1 and subsequent production of prostaglandin E2, while production of prostaglandin I2 is reduced by increased expression of mPGES-1
-
interleukin 1beta
stimulates release of prostaglandin E2 by myometrical smooth muscle cells and increases COX-2 and mPGES-1 mRNA and protein expression
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.13
(5Z,13E)-(15S)-9a,11a-epidioxy-15-hydroxyprosta-5,13-dienoate
-
wild-type, 0°C, pH 7.2
0.734
(5Z,13E)-(15S)-9a,11a-epidioxy-15-hydroxyprosta-5,13-dienoate
-
mutant Q134E, 0°C, pH 7.2
1.61
(5Z,13E)-(15S)-9a,11a-epidioxy-15-hydroxyprosta-5,13-dienoate
-
mutant Q36E, 0°C, pH 7.2
0.0024
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
-
0.014
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
0.1
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
in the presence of 0.3 mM dodecylmaltoside
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
7
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
dodecylmaltoside activated
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0035
(2E)-2-(2,5-bis[2-[4-(trifluoromethyl)phenyl]ethoxy]benzylidene)hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
(2E)-2-(2,5-bis[[4-(trifluoromethyl)benzyl]oxy]benzylidene)hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0034
(2E)-2-[2,5-bis(2-cyclohexylethoxy)benzylidene]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0015
(2E)-2-[2,5-bis(2-phenylethoxy)benzylidene]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
(2E)-2-[4-[3-(2,3-dimethylphenoxy)propoxy]benzylidene]hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.01
(2E)-2-[5-(2-cyclohexylethoxy)-2-[[4-(trifluoromethyl)benzyl]oxy]benzylidene]hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0042
(2R)-2-([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0046
(2S)-2-([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.000248
(3R)-1-(7-chloro-2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazolin-6-yl)pyrrolidin-3-yl acetate
Homo sapiens
pH and temperature not specified in the publication
0.000243
(3S)-1-(7-chloro-2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazolin-6-yl)pyrrolidin-3-yl acetate
Homo sapiens
pH and temperature not specified in the publication
0.00372
(4R)-1-(8-chloroquinolin-2-yl)-N-[cis-4-(hydroxymethyl)cyclohexyl]-3,3-dimethylpiperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000001 - 0.000504
(4R)-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-[4-(trifluoromethyl)phenyl]piperidine-4-carboxamide
0.000004
(4S)-1-(8-chloroquinolin-2-yl)-N-[cis-4-(hydroxymethyl)cyclohexyl]-3,3-dimethylpiperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000007
(4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)-N-[(3S)-oxan-3-yl]piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000006
(4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)-N-[(3S)-oxolan-3-yl]piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000012
(4S)-3,3-dimethyl-N-(3-methylbutan-2-yl)-1-(8-methylquinolin-2-yl)piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
(4S)-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-[4-(trifluoromethyl)phenyl]piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
(4S)-N-[(3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-(8-methylquinolin-2-yl)piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0051
([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)(5,8-dihydronaphthalen-1-yl)acetic acid
Homo sapiens
-
-
0.01
([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)acetic acid
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.000002
1,5-anhydro-2,3,4-trideoxy-3-[[(4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)piperidine-4-carbonyl]amino]-D-glycero-hexitol
Homo sapiens
-
pH and temperature not specified in the publication
0.03
1-[2-(2-methylphenyl)ethyl]-4-[2'-[(naphthalen-1-yloxy)methyl]biphenyl-4-yl]-1H-1,2,3-triazole
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.000012
1-[4-[2-(2-carboxy-2-methylpropyl)-1-(4-chlorobenzyl)-3-methyl-1H-indol-4-yl]-2-fluorophenyl]pyridinium
Homo sapiens
-
-
0.000003
1-[5-chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0022
2(4-(3-biphenyloxypropoxy)phenylthio)hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0011
2-(2,3-diphenethoxybenzylidene)hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.000023
2-(2,6-dichloroanilino)-7,7-dimethyl-N-(2,2,2-trifluoroethyl)-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000062
2-(2,6-dichloroanilino)-7,7-dimethyl-N-(2,2,3,3,3-pentafluoropropyl)-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000041
2-(2,6-dichloroanilino)-7,7-dimethyl-N-phenyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000037
2-(2,6-dichloroanilino)-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000017
2-(2,6-dichloroanilino)-7,7-dimethyl-N-[6-(trifluoromethyl)pyridin-3-yl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000046
2-(2,6-dichloroanilino)-7-methyl-N-[3-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000094
2-(2,6-dichloroanilino)-7-methyl-N-[4-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000013
2-(2,6-dichloroanilino)-N-(2,6-dimethylpyridin-3-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00001
2-(2,6-dichloroanilino)-N-(2-fluorophenyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000047
2-(2,6-dichloroanilino)-N-(4,4-difluorocyclohexyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000035
2-(2,6-dichloroanilino)-N-(4-fluorophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000067
2-(2,6-dichloroanilino)-N-(6-methoxypyridin-3-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000058
2-(2,6-dichloroanilino)-N-[(4-fluorophenyl)methyl]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000039
2-(2-chloro-6-fluoroanilino)-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000077
2-(2-chloro-6-fluoroanilino)-N-(3-cyanophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000042
2-(2-chloro-6-fluoroanilino)-N-(4-cyanophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000028
2-(2-chloro-6-fluoroanilino)-N-(4-fluorophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000022
2-(2-chloro-6-fluoroanilino)-N-(4-fluorophenyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000021
2-(2-chloro-6-fluoroanilino)-N-(5-chloropyridin-2-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000011
2-(2-chloro-6-fluoroanilino)-N-(cyclohexylmethyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000008
2-(2-chloro-6-fluoroanilino)-N-[3-fluoro-5-(trifluoromethyl)phenyl]-1-methyl-7,8-dihydro-1H-[1,4]dioxino[2,3-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00002
2-(2-chloro-6-fluoroanilino)-N-[6-(difluoromethoxy)pyridin-3-yl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00066
2-(2-chloro-6-fluorophenyl)-4-(4-chlorophenyl)-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.00032
2-(2-chloro-6-fluorophenyl)-4-(4-phenoxyphenyl)-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.00015
2-(2-chloro-6-fluorophenyl)-4-[4-(2-phenylethyl)phenyl]-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.000008
2-(2-chloro-6-fluorophenyl)-4-[4-(phenylethynyl)phenyl]-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.00018
2-(2-chloro-6-fluorophenyl)-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.0014
2-(2-chloro-6-fluorophenyl)-4-[4-(phenylsulfonyl)phenyl]-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.000035
2-(2-chloro-6-fluorophenyl)-4-[4-[(E)-2-phenylethenyl]phenyl]-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.0024
2-(3,5-diphenethoxybenzyl)hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0028
2-(3,5-diphenethoxybenzylidene)hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0037
2-(4-bromophenyl)-5-(2-chloro-6-fluorophenyl)-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.000001 - 0.0000053
2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
0.000676
2-(difluoromethyl)-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.0000009
2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
Homo sapiens
-
at pH 7.0 and 25°C
0.0000009
2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[5-methyl-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00112
2-(difluoromethyl)-N-(1H-imidazol-2-yl)-5-([[(2R)-2-methylbutanoyl]amino]methyl)benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.00246
2-(difluoromethyl)-N-(1H-imidazol-2-yl)-5-[(2-methylpropanamido)methyl]benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.0000103
2-(difluoromethyl)-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]-5-(propanamidomethyl)pyridine-3-carboxamide
Homo sapiens
-
at pH 7.0 and 25°C
0.0059
2-([4,6-bis[2-(4-cyanophenyl)ethoxy]pyrimidin-2-yl]sulfanyl)hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
2-([4,6-bis[2-(4-methoxyphenyl)ethoxy]pyrimidin-2-yl]sulfanyl)hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0009
2-([4,6-bis[2-(4-methylphenyl)ethoxy]pyrimidin-2-yl]sulfanyl)hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0037
2-([4,6-bis[2-(4-nitrophenyl)ethoxy]pyrimidin-2-yl]sulfanyl)hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0065
2-([4,6-bis[2-(thiophen-3-yl)ethoxy]pyrimidin-2-yl]sulfanyl)hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0039
2-([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid
Homo sapiens
-
-
0.0017
2-([4-chloro-6-[(4'-cyanobiphenyl-4-yl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid
Homo sapiens
-
-
0.0021
2-([4-chloro-6-[(5-methoxy-2-methylbiphenyl-4-yl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid
Homo sapiens
-
-
0.0013
2-([4-[(biphenyl-4-ylmethyl)amino]-6-chloropyrimidin-2-yl]sulfanyl)nonanoic acid
Homo sapiens
-
-
0.0029
2-([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.01
2-([4-[3-(2-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0088
2-([4-[3-(2-methylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.01
2-([4-[3-(3-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.01
2-([4-[3-(3-methylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0094
2-([4-[3-(4-chloro-2-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0093
2-([4-[3-(4-methylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0022
2-([4-[3-(5,6,7,8-tetrahydronaphthalen-1-yloxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.01
2-([4-[3-(quinolin-6-yloxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.000198
2-bromo-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.00367
2-chloro-4-fluoro-N-(1H-imidazol-2-yl)-5-[(2-methylpropanamido)methyl]benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.000003
2-chloro-4-[(2,2-dimethylpropanamido)methyl]-N-[3-[4-(trifluoromethyl)anilino][1,2]thiazolo[4,5-b]pyridin-7-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.000005
2-chloro-5-[(2,2-dimethylpropanamido)methyl]-N-[4-oxo-3-[4-(trifluoromethyl)phenyl]-3,4-dihydrophthalazin-6-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.000385
2-chloro-5-[(3,3-dimethylbutanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.000157
2-chloro-6-fluoro-N-[3-[4-(trifluoromethyl)anilino][1,2]thiazolo[4,5-b]pyridin-7-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.00232
2-chloro-N-(1H-imidazol-2-yl)-4-methyl-5-[(2-methylpropanamido)methyl]benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.000885
2-chloro-N-(1H-imidazol-2-yl)-5-[(2-methylpropanamido)methyl]benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.000058
2-chloro-N-[3-(naphthalen-1-ylcarbamoyl)phenyl]benzamide
Homo sapiens
-
wild type enzyme, in 0.1 M potassium phosphate buffer, pH 7.4, 2.5 mM glutathione, at 4°C
0.0000058
2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000082
2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-N-(3-methylbutyl)-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000065
2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-N-[4-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000157
2-[(3,5-dichloropyridin-4-yl)amino]-N-[(4-fluorophenyl)methyl]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000037
2-[(3,5-dichloropyridin-4-yl)amino]-N-[2-fluoro-4-(trifluoromethyl)phenyl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000047
2-[(3,5-dichloropyridin-4-yl)amino]-N-[4-fluoro-3-(trifluoromethyl)phenyl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0046
2-[(3,5-diphenethoxyphenyl)thio]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
2-[(4,6-bis[2-[4-(trifluoromethoxy)phenyl]ethoxy]pyrimidin-2-yl)sulfanyl]hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0019
2-[(4,6-bis[2-[4-(trifluoromethyl)phenyl]ethoxy]pyrimidin-2-yl)sulfanyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0012
2-[(4,6-diphenethoxypyrimidin-2-yl)thio]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0041
2-[(4-[3-[2-(propan-2-yl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0027
2-[(4-[3-[3-(propan-2-yl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.002
2-[(4-[3-[3-(trifluoromethyl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0017
2-[(4-[3-[4-chloro-3-(trifluoromethyl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0026
2-[(4-[[3,5-bis(2,2,2-trifluoroethoxy)phenyl]amino]-6-chloropyrimidin-2-yl)sulfanyl]nonanoic acid
Homo sapiens
-
-
0.0039
2-[2,3-bis(2-phenylethoxy)benzyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
2-[2,4-bis(2-phenylethoxy)benzyl]hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0024
2-[2,5-bis(2-phenylethoxy)benzyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.00018
2-[2-(2-chloro-6-fluorophenyl)-4-[6-(phenylethynyl)pyridin-3-yl]-1H-imidazol-5-yl]ethanol
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
2-[2-[(1S,2S)-2-([1-[4-(trifluoromethoxy)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000002
2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000006
2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]pyridine-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.000002
2-[2-[(1S,2S)-2-([1-[5-(trifluoromethyl)pyridin-2-yl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000001
2-[2-[(1S,2S)-2-[[1-(8-methylquinolin-2-yl)piperidine-4-carbonyl]amino]cyclopentyl]ethyl]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.0027
2-[3,4-bis(2-phenylethoxy)benzyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0006
2-[3,5-bis(2-phenylethoxy)phenoxy]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
2-[3-(aminooxy)-2,2-dimethyl-3-oxopropyl]-3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indole
Homo sapiens
-
IC50: 0.01 mM
0.0014
2-[4-(4-bromophenyl)-1H-imidazol-2-yl]benzonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.001
2-[4-(4-chlorophenyl)-1H-imidazol-2-yl]-3-fluorobenzonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.005
2-[4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)phenyl]propan-2-ol
Homo sapiens
-
IC50 above 0.005 mM, pH and temperature not specified in the publication
0.0071
2-[4-[3-(2,3-dimethylphenoxy)propoxy]benzyl]hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0000009
2-[6-(2-cyclopropylethoxy)-9-(3-hydroxy-3-methylbutyl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
Homo sapiens
-
-
0.006
2-[6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl] acetic acid
Homo sapiens
-
-
0.0000009
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
-
-
0.0000009
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
-
-
0.0000007
2-[6-chloro-9-(3-hydroxy-3-methylbutyl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
Homo sapiens
-
-
0.01
2-[[4,6-bis(2-cycloheptylethoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0024
2-[[4,6-bis(2-cyclohexylethoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
2-[[4,6-bis(2-cyclopentylethoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0096
2-[[4,6-bis(2-cyclopropylethoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0073
2-[[4,6-bis(2-phenylethoxy)pyrimidin-2-yl]sulfanyl]butanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.002
2-[[4,6-bis(2-phenylethoxy)pyrimidin-2-yl]sulfanyl]octanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
2-[[4,6-bis(3-methylbutoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0022
2-[[4,6-bis(3-phenylpropoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0009
2-[[4,6-bis(4-phenylbutoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0038
2-[[4,6-bis(benzyloxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
2-[[4-(3-phenoxypropoxy)phenyl]sulfanyl]hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0016
2-[[4-(biphenyl-4-ylamino)-6-chloropyrimidin-2-yl]sulfanyl]nonanoic acid
Homo sapiens
-
-
0.00011
3-(4-bromophenyl)-5-(2-chloro-6-fluorophenyl)-1H-1,2,4-triazole
Homo sapiens
-
pH and temperature not specified in the publication
0.0021
3-(naphthalen-1-ylamino)-6-nitrobenzo[d]isothiazole 1,1-dioxide
Homo sapiens
-
0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.00029
3-[(5E)-3-(4-butylbenzyl)-1-(4-chlorobenzyl)-4-methylidene-5-[(2E)-4-methylpent-2-en-1-ylidene]-4,5-dihydro-1H-pyrrol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.00029 mM
0.00025
3-[1-(4-chlorobenzyl)-3-(3,3-dimethylbutanoyl)-4-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.00025
3-[1-(4-chlorobenzyl)-3-(3,3-dimethylbutanoyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.00025 mM
0.0032
3-[1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.0032 mM
0.0011
3-[1-(4-chlorobenzyl)-3-methyl-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.0011 mM
0.0006
3-[1-(4-chlorobenzyl)-3-methyl-5-phenyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.00060 mM
0.0043
3-[1-(4-chlorobenzyl)-3-methyl-7-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.0043 mM
0.002
3-[1-(4-chlorobenzyl)-3-t-butyl-thio-5-isopropylindol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.000004
3-[1-(4-chlorobenzyl)-4-(2'-chloro-2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.000008
3-[1-(4-chlorobenzyl)-4-(2,2'-difluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.000022
3-[1-(4-chlorobenzyl)-4-(2-chlorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.000005
3-[1-(4-chlorobenzyl)-4-(2-fluoro-2'-methoxybiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.000003
3-[1-(4-chlorobenzyl)-4-(2-fluoro-2'-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.000007
3-[1-(4-chlorobenzyl)-4-(2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.00065
3-[1-(4-chlorobenzyl)-5-(1-methylethyl)-3-phenoxy-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.00065 mM
0.0064
3-[1-(4-chlorobenzyl)-5-(1-methylethyl)-3-phenyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.0064 mM
0.0009
3-[1-(4-chlorobenzyl)-5-(1-methylethyl)-3-[(2-methylphenyl)carbonyl]-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.00090 mM
0.000004
3-[1-(4-chlorobenzyl)-5-(2'-chloro-2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000004 mM
0.000008
3-[1-(4-chlorobenzyl)-5-(2,2'-difluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000008 mM
0.000022
3-[1-(4-chlorobenzyl)-5-(2-chlorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000022 mM
0.000005
3-[1-(4-chlorobenzyl)-5-(2-fluoro-2'-methoxybiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000005 mM
0.000003
3-[1-(4-chlorobenzyl)-5-(2-fluoro-2'-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000003 mM
0.000033
3-[1-(4-chlorobenzyl)-5-(2-fluoro-3'-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000033 mM
0.000031
3-[1-(4-chlorobenzyl)-5-(2-fluoro-4'-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000031 mM
0.000007
3-[1-(4-chlorobenzyl)-5-(2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000007 mM
0.000012
3-[1-(4-chlorobenzyl)-5-(3-fluoro-4-pyridin-3-ylphenyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000012 mM
0.0026
3-[1-(4-chlorobenzyl)-5-fluoro-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.0026 mM
0.000006
3-[1-(4-chlorobenzyl)-5-[2-fluoro-2'-(phenylcarbonyl)biphenyl-4-yl]-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000006 mM
0.000032
3-[1-(4-chlorobenzyl)-5-[3-fluoro-4-(pyrimidin-5-ylmethyl)phenyl]-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000032 mM
0.0016
3-[1-(p-chlorobenzvl)-5-isopropyl-3-tert-butylthioindol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
i.e. 3-[1-(p-chlorobenzvl)-5-isopropyl-3-tert-butylthioindol-2-yl]-2,2-dimethylpropanoic acid or FLAP, formerly designated L-663,536, a lipoxygenase inhibitor, IC50: 0.0016 mM
0.00006
3-[3-(benzylsulfanyl)-1-(4-chlorobenzyl)-5-[4-[(4-chloro-2-fluorophenyl)ethynyl]phenyl]-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.0021
3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.0024
3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(propan-2-yl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.01
3-[3-(tert-butylsulfanyl)-1-methyl-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.01 mM
0.0032
3-[3-(tert-butylsulfanyl)-5-(1-methylethyl)-1-(3-phenylpropyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.0032 mM
0.0067
3-[3-(tert-butylsulfanyl)-5-(1-methylethyl)-1-prop-2-en-1-yl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.0067 mM
0.01
3-[3-(tert-butylsulfanyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.01 mM
0.00026
3-[3-[(tert-butylsulfanyl)acetyl]-1-(4-chlorobenzyl)-4-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.00026
3-[3-[(tert-butylsulfanyl)acetyl]-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.00026 mM
0.000006
3-[4-(2'-acetyl-2-fluorobiphenyl-4-yl)-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.000016
3-[4-biphenyl-4-yl-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.01
3-[4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]propanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.00016
3-[5-biphenyl-3-yl-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.00016 mM
0.000016
3-[5-biphenyl-4-yl-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000016 mM
0.00033
3-[5-tert-butyl-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.00033 mM
0.000007
3-[6-([1,1'-biphenyl]-4-yl)-1-[(4-chlorophenyl)methyl]-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
pH and temperature not specified in the publication
0.03
4'-[1-(3-phenylpropyl)-1H-1,2,3-triazol-4-yl]biphenyl-4-ol
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.03
4'-[1-[(phenylsulfanyl)methyl]-1H-1,2,3-triazol-4-yl]biphenyl-3-ol
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.03
4'-[1-[(phenylsulfanyl)methyl]-1H-1,2,3-triazol-4-yl]biphenyl-4-ol
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.03
4'-[1-[2-(2-methylphenyl)ethyl]-1H-1,2,3-triazol-4-yl]biphenyl-4-amine
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.03
4-(2'-[[2-chloro-5-(trifluoromethyl)phenoxy]methyl]biphenyl-4-yl)-1-(3-phenylpropyl)-1H-1,2,3-triazole
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.03
4-(2'-[[2-chloro-5-(trifluoromethyl)phenoxy]methyl]biphenyl-4-yl)-1-[2-(2-methylphenyl)ethyl]-1H-1,2,3-triazole
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.03
4-(4'-phenoxybiphenyl-4-yl)-1-(3-phenylpropyl)-1H-1,2,3-triazole
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.00057
4-(4-benzylphenyl)-2-(2-chloro-6-fluorophenyl)-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.00039
4-(4-chlorobenzyl)-2,6-bis[4-(trifluoromethoxy)phenyl]-4H-thieno[3,2-b]pyrrole
Homo sapiens
-
-
0.00011
4-(biphenyl-4-yl)-2-(2-chloro-6-fluorophenyl)-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.005
4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzamide
Homo sapiens
-
IC50 above 0.005 mM, pH and temperature not specified in the publication
0.005
4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzoic acid
Homo sapiens
-
IC50 above 0.005 mM, pH and temperature not specified in the publication
0.000043
4-chloro-2-([[(1S,2S)-2-(2,2-dimethylpropanamido)cyclopentyl]methyl]amino)benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000004
4-chloro-2-([[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]methyl]amino)benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000002
4-chloro-2-[([(1S,2S)-2-[(1-phenylpiperidine-4-carbonyl)amino]cyclopentyl]methyl)amino]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000001
4-chloro-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000002
4-chloro-2-[[(1R,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]methoxy]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000001
4-fluoro-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000001
4-methyl-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.03
4-[(4-[2'-[(naphthalen-1-yloxy)methyl]biphenyl-4-yl]-1H-1,2,3-triazol-1-yl)sulfonyl]benzoic acid
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.03
4-[2'-[(naphthalen-1-yloxy)methyl]biphenyl-4-yl]-1-(3-phenylpropyl)-1H-1,2,3-triazole
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.03
4-[4-(phenanthren-9-yl)phenyl]-1-(3-phenylpropyl)-1H-1,2,3-triazole
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.03
4-[4-benzyl-1-[(phenylsulfanyl)methyl]-1H-1,2,3-triazol-5-yl]benzaldehyde
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.0032
4-[[4-(biphenyl-4-yl)-1H-1,2,3-triazol-1-yl]methyl]-3-nitrobenzoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.03
5-(4-bromophenyl)-3-(2-chloro-6-fluorophenyl)-1,2,4-oxadiazole
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.000074
5-(acetamidomethyl)-2-(difluoromethyl)-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
Homo sapiens
-
at pH 7.0 and 25°C
0.03
5-(dimethylamino)-N-[4'-[1-(3-phenylpropyl)-1H-1,2,3-triazol-4-yl]biphenyl-4-yl]naphthalene-1-sulfonamide
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.00108
5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)-2-(trifluoromethyl)benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.00311
5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)-2-methylbenzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.00094
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(1,3-thiazol-2-ylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000013
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclohex-1-en-1-ylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000033
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclohexylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.00017
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclopropylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000023
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.00048
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(pyridin-3-ylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.0025
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-ethynylpyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000009
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(2-chlorophenyl)ethynyl]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000004
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(3-chlorophenyl)ethynyl]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000031
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(4-chlorophenyl)ethynyl]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.00002
5-[2-(2-chloro-6-fluorophenyl)-5-methyl-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000016
5-[5-(2-chloro-6-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-(phenylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
5-[5-bromo-2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000005
5-[5-chloro-2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.0067
6-nitro-3-(m-tolylamino) benzo[d]isothiazole 1,1-dioxide
Homo sapiens
-
0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.0236
6-nitro-N-phenyl-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.05
6-nitro-N-[3-(propan-2-yl)phenyl]-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
above, 0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.0011
7-hydroxy-N,N'-bis(2,4,6-trimethylphenyl)naphthalene-1,3-disulfonamide
Homo sapiens
-
-
0.005
aminomethyl 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzenesulfinate
Homo sapiens
-
IC50 above 0.005 mM, pH and temperature not specified in the publication
0.01
ethyl 2-([4-[3-(quinolin-6-yloxy)propoxy]phenyl]sulfanyl)hexanoate
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0056
ethyl 2-[[4-chloro-6-(quinolin-6-ylamino)pyrimidin-2-yl]sulfanyl]nonanoate
Homo sapiens
-
-
0.0072
methyl 3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoate
Homo sapiens
-
IC50: 0.0072 mM
0.005
methyl 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzenesulfinate
Homo sapiens
-
IC50 above 0.005 mM, pH and temperature not specified in the publication
0.0000017
methyl 4-[6-bromo-2-(2-chloro-6-fluorophenyl)-1H-phenanthro[9,10-d]imidazol-9-yl]but-3-ynoate
Homo sapiens
-
-
0.05
N-(1,3-benzodioxol-4-yl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
above, 0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.05
N-(2-methylphenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
above, 0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.000016
N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-1,1-dioxo-1,2-dihydro-1lambda~6~,2-benzothiazine-3-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.05
N-(3,4-dimethoxyphenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
above, 0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.05
N-(3-bromobenzyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
above, 0.1 M potassium phosphate buffer, pH 7.4, 4°Cn
0.0073
N-(3-bromophenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.0057
N-(3-chlorophenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.0088
N-(3-methoxyphenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.05
N-(3-tert-butylphenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
above, 0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.000004
N-(4-chloro-2-fluorophenyl)-2-[2,6-dichloro-3-[(2,2-dimethylpropanamido)methyl]anilino]-6-(2,2-difluoroethoxy)-1-methyl-1H-benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0169
N-(4-methoxyphenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.05
N-(5-bromonaphthalen-1-yl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
above, 0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.00015
N-(6-nitro-1,1-dioxido-1,2-benzothiazol-3-yl)quinolin-5-amine
Homo sapiens
-
0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.05
N-(biphenyl-3-yl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
above, 0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.0000022
N-(cyclohexylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000013
N-(cyclohexylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000023
N-(cyclopentylmethyl)-2-(2,6-dichloroanilino)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000012
N-(cyclopropylmethyl)-2-(2,6-dichloroanilino)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000025
N-(cyclopropylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000026 - 0.000058
N-([4-chloro-3-[4-oxo-7-(trifluoromethyl)-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
0.000481
N-([4-chloro-3-[7-chloro-4-oxo-6-(pyridin-4-yl)-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000713
N-([4-chloro-3-[7-chloro-6-(4-hydroxypiperidin-1-yl)-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000261
N-([4-chloro-3-[7-chloro-6-(morpholin-4-yl)-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000026
N-cyclohexyl-2-(2,6-dichloroanilino)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000063
N-cyclohexyl-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000012
N-cyclohexyl-2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000007
N-tert-butyl-1-(7-chloro-2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazolin-6-yl)azetidine-3-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000055
N-[(4-chloro-3-[4-oxo-6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.00001
N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl]phenyl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000005 - 0.000007
N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
0.000074
N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)piperidin-1-yl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000016
N-[(4-chloro-3-[4-oxo-7-[6-(trifluoromethyl)pyridin-3-yl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000036
N-[(4-chloro-3-[7-chloro-4-oxo-6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000024
N-[(4-chloro-3-[7-chloro-6-[4-(difluoromethyl)piperidin-1-yl]-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000005
N-[(6-chloro-5-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydropyrido[4,3-d]pyrimidin-2-yl]pyridin-3-yl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000179
N-[3-(4-bromophenyl)-4-oxo-3,4-dihydrophthalazin-6-yl]-2-chloro-6-fluorobenzamide
Homo sapiens
pH and temperature not specified in the publication
0.0013
N-[4-chloro-3-(5-methyl-1,3-benzoxazol-2-yl)phenyl]-2-(trifluoromethyl)benzamide
Homo sapiens
-
-
0.000003
N-[5-(4-chlorophenyl)-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.000003
N-[5-(4-chlorophenyl)-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]pyridine-3-carboxamide
Homo sapiens
-
at pH 7.0 and 25°C
0.000003
N-[5-(4-chlorophenyl)-4-methyl-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]pyridine-3-carboxamide
Homo sapiens
-
at pH 7.0 and 25°C
0.000036
N-[[3-(7-bromo-4-oxo-3,4-dihydroquinazolin-2-yl)-4-chlorophenyl]methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000042
N-[[4-chloro-3-(7-chloro-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000032
N-[[4-chloro-3-(7-chloro-6-cyclopropyl-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000111
N-[[4-chloro-3-(7-chloro-6-methoxy-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000304
N-[[4-chloro-3-(7-methoxy-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000063
N-[[4-chloro-3-(7-nitro-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000004
N-[[6-(difluoromethyl)-5-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydropyrido[4,3-d]pyrimidin-2-yl]pyridin-3-yl]methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000006
N-[[6-(difluoromethyl)-5-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]pyridin-3-yl]methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.0000195
sodium 3-[1-[(4-chlorophenyl)methyl]-5-(2-fluoro[1,1'-biphenyl]-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoate
Homo sapiens
-
at pH 7.0 and 25°C
0.03
[1-[(phenylsulfanyl)methyl]-1H-1,2,3-triazol-4-yl]methyl benzoate
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.0012
[[4,6-bis(2-phenylethoxy)pyrimidin-2-yl]sulfanyl](phenyl)acetic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
[[4,6-bis(2-phenylethoxy)pyrimidin-2-yl]sulfanyl]acetic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.000001
(4R)-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-[4-(trifluoromethyl)phenyl]piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000504
(4R)-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-[4-(trifluoromethyl)phenyl]piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
Homo sapiens
-
-
0.000001
2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
Homo sapiens
pH and temperature not specified in the publication
0.0000053
2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
Homo sapiens
-
at pH 7.0 and 25°C
0.000241
2-chloro-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.000241
2-chloro-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0024
MK-886
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.000026
N-([4-chloro-3-[4-oxo-7-(trifluoromethyl)-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000058
N-([4-chloro-3-[4-oxo-7-(trifluoromethyl)-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000005
N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000007
N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
0.054
-
mutant enzyme T131V/L135F/A138F, in 0.1 M potassium phosphate buffer, pH 7.4, 2.5 mM glutathione, at 4°C
0.214
-
wild type enzyme, in 0.1 M potassium phosphate buffer, pH 7.4, 2.5 mM glutathione, at 4°C
100 - 200
-
in the presence of 0.4 mM prostaglandin H2 or prostaglandin G2 and 2.5 mM glutatione
510
-
in the presence of 10 microM prostaglandin H2 or prostaglandin G2 and 2.5 mM glutatione
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7.4
7.4
-
microsomal membranes are incubated with PGH2, enzyme activity assay
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
microsomal suspension is incubated on ice with PGH2, enzyme activity assay
additional information
-
microsomal suspension is incubated on ice with PGH2, enzyme activity assay
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
isoform mPGES-2 protein is largely in stromal cells surrounding smooth vascular muscle. Expression of mPGES-2 mRNA increases with term labour and preterm labour
cells express both microsomal isoforms mPGES-1 and mPGES-2 and cytosolic isoform cPGES
-
-
-
in normal breast the enzyme is seen in myoepithelial cells and in stromal fibroblasts and vascular smooth muscle, in breast disease, the enzyme is observed in epithelial cells adjacent to cancer, in scattered foci of fibrocystic disease, in ductal carcinoma in situ and in invasive cancers, in addition to myoepithelial cells
-
from women undergoing treatment for infertility, expression of mPGES-2, mPGES-1, and cPGES
-
extravillous cytotrophoblast is strongly posistive for enzyme protein in the basal plate
-
peripheral blood monocyte, no basal expression of enzyme, but strong induction of expression by proinflammatory stimulation via LPS. In alternatively activated M2 monocytes-macrophages, interleukins IL-4, IL-13, and to a lesser extent, IL-10 or interferon IFN-gamma inhibit LPS-induced expression of enzyme. Induction of enzyme expression correlates with changes at the protein level and production of prostaglandin E2
isoform mPGES-1 localizes mostly in myometrial and vascular smooth muscle cells of pregnant women. Isoform cPGES is diffusely located throughout the myometrium. Expression of COX-2 and isoform mPGES-1 mRNA with term labour, whereas cPGES expression does not change. Interleukin 1beta stimulates release of prostaglandin E2 by myometrical smooth muscle cells and increases COX-2 and mPGES-1 mRNA and protein expression
-
only isoform mPGES-1 can be found in neutrophils, it co-localizes with COX-2 and its expression is mainly constitutive
-
enzyme protein is prominent in vesicles separating from syncytiotrophoblast into the intervillous space
-
constitutive expression of enzyme is associated with increased prostaglandin E2 production and stimulation of growth. Inhibition of enzyme activity and expression block the release of prostaglandin E2 and decrease cellular proliferation. Antiproliferative effects may be overcome by exogenous prostaglandin E2
cells express both microsomal isoforms mPGES-1 and mPGES-2 and cytosolic isoform cPGES. Isoform mPGES-1 contributes most to total activity and is induced by interleukin IL-1beta, which in turn reduces the ability of cells to produce prostaglandin I2
additional information
-
in brain mPGES-2 is detected in neurons, activated microglia, and endothelium, but not in resting microglia, astrocytes, or smooth muscle cells
-
mPGES-2 colocalizedswith microglia in activated (amoeboid-shaped) cells
-
immunolocalized in extravillous trophoblasts and macrophages, in early gestation also in cytotrophoblasts and syncytiotrophoblasts
-
immunolocalized to the fibroblasts and macrophages in villous stroma, also in apoptotic early gestational syncytiotrophoblasts
additional information
-
in patients with rheumatoid arthritis, the protein is overexpressed in synovial tissue, particularly by macrophages and fibroblasts in the synovial lining layer
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
evolution
microsomal prostaglandin E2 synthase belongs to the MAPEG superfamily
malfunction
-
mPGES-1 knockdown delays tumor formation and reduced tumor weight in human cholangiocarcinoma tissue
metabolism
-
mPGES-1 is a rate-limiting enzyme that is coupled with cyclooxygenase-2 in the synthesis of prostaglandin E2
physiological function
additional information
physiological function
-
the enzyme is responsible for prostaglandin E2 synthesis in inflammation-associated pathologies
physiological function
-
overexpression of mPGES-1 in human cholangiocarcinoma cells increases tumor cell proliferation, migration, invasion, and colony formation. mPGES-1 inhibits the expression of phosphatase and tensin homologue deleted on chromosome 10 (PTEN), leading to activation of the epidermal growth factor/phosphoinositide 3-kinase/AKT/mammalian target of rapamycin signaling pathways in cholangiocarcinoma cells
additional information
the isozyme mPGES-1 structure reveals three well-defined active site cavities within the membrane-spanning region in each monomer interface of the trimeric structure. An important determinant of the active site cavity is a small cytosolic domain inserted between transmembrane helices I and II. A a 16-A-deep cone-shaped cavity extending from the cytosolic side into the membrane-spanning region might have a potential role in substrate access. Serine 127 plays a role in the catalytic mechanism, active site structure, overview
additional information
-
the isozyme mPGES-1 structure reveals three well-defined active site cavities within the membrane-spanning region in each monomer interface of the trimeric structure. An important determinant of the active site cavity is a small cytosolic domain inserted between transmembrane helices I and II. A a 16-A-deep cone-shaped cavity extending from the cytosolic side into the membrane-spanning region might have a potential role in substrate access. Serine 127 plays a role in the catalytic mechanism, active site structure, overview
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). PGES2_HUMAN
377
0
41943
Swiss-Prot
Mitochondrion (Reliability: 3)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
17000
18000
215000
-
gradient centrifugation, density equilibrium centrifugation, gel filtration
33000
-
dimer, determined by SDS-PAGE and Western blot analysis, crosslinked subunits
45000
-
trimer, determined by SDS-PAGE and Western blot analysis, crosslinked subunits
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
homotrimer
trimer
trimer
-
3 * ?, gradient centrifugation, density equilibrium centrifugation, gel filtration
trimer
-
trimeric state characterized by chemical cross-linking with glutaraldehyde
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
purified recombinant microsomal isozyme PGE2 synthase-1, in presence of beta-octyl-glycoside and GSH or 1-(4-phenylphenyl)-2-(S-glutathionyl)-ethanone (bis-phenyl-GSH), hanging drop vapor diffusion method, the reservoir solutions used contain 100 mM CAPSO, pH 9.5, 30% PEG 400, 100 mM NaCl, and 100 mM Li2SO4 (mersalyl acid soak and bis-phenyl-GSH complex) or 100 mM Tris, pH 8.0-8.5, 30% PEG400, 100 mM NaCl, and 1 mM TCEP (native GSH complex), 4°C, X-ray diffraction structure determination and analysis at 1.2 A resolution
red-coloured protein purified after growth of Escherichia coli in LB medium containing delta-aminolevulinate and Fe(NO3)3. Enzyme contains bound glutathione and heme
-
the structure of human MPGES1 is determined in complex with the tripeptide gamma-L-glutamyl-L-cysteinyl-glycine, glutathione, at 3.5 A in-plane resolution using electron crystallography
three-dimensional model of substrate-domain and its binding with subsrtates prostaglandin H2 and glutathione. Residue Y130 plays a key role in binding with prostaglandin H2 and in the catalytic process. R110 and T114 interact intensively with the carbonyl tail of prostaglandin H2, whereas Q36 and Q134 only enhance the prostaglandin H2 binding affinity. Prostaglandin H2 interacts with glutathione through hydrogen binding between the peroxy group of prostaglandin H2 and the -SH group of glutathione
-
threedimensional structural model of binding with inhibitors, quantitative structure-activity correlation
-
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
D49N
the mutant shows severely reduced activity compared to the wild type enzyme
H72A
R126A
R126K
the mutant shows severely reduced activity compared to the wild type enzyme
R126Q
R70A
R70A/R122A
the mutant shows increased Km compared to the wild type enzyme, the double mutant of the mPGES-1 significantly reduces the binding affinity of GSH
S127A
T131V/L135F/A138F
-
the mutant shows bout 4fold reduced specific activity towards prostaglandin H2 compared to the wild type enzyme and is not inhibited by 1-C-(2-chlorobenzene)-3-N-(naphthalen-1-yl)benzene-1,3-dicarboxamide
Y117A
Y117F
Y130I
additional information
-
knockdown of isoform mPGES-1 by siRNA results in downregulation of cytokine-induced mPGES-1 protein expression and activity. siRNA does not affect the cytokine-stimulated production of prostaglandin E2, whereas prostaglandin F2alpha levels are enhanced. Neither isoform mPGES-2 nor cPGES expression are affected by siRNA silencing of mPGES-1
R126A
mutant, exhibits a glutathione-dependent reductase activity, which allows conversion of prostaglandin H2 into prostaglandin F2alpha
R126A
-
the mutation of the enzyme abolishes its PGES activity to exhibit a novel glutathione-dependent reductase activity
R126Q
mutant, exhibits a glutathione-dependent reductase activity, which allows conversion of prostaglandin H2 into prostaglandin F2alpha
R126Q
-
the mutation of the enzyme abolishes its PGES activity to exhibit a novel glutathione-dependent reductase activity
R126Q
the mutant shows severely reduced activity compared to the wild type enzyme
Y117F
the mutant still maintains full catalytic activity relative to the wild type
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
activity in solubilized membranes remains stable for a prolonged time in the presence of reduced glutathione and glycerol
-
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
purification after expression of N-terminally truncated enzyme in recombinant Escherichia coli growing in LB medium containing delta-aminolevulinate and Fe(NO3)3 gives a protein of red colour. Purification after growth of Escherichia coli on minimal medium gives a colourless protein
-
recombinant active isozyme mPGES-1 from Spodoptera frugiperda Sf9 cell microsomes by hydroxylapatite chromatography
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expressed in A-549 cells, HeLa cells, HEK-293 cells, RAW 264.7 cells, Pichia pastoris strain KM71H, and Sf9 insect cells
-
expressed in Escherichia coli BL21Star (DE) pLysS cells and SF9 insect cells
expression in Escherichia coli
into the TA vector and subsequently into pET-28a for expression in various Escherichia coli strains, the expression rate is enhanced by modifying the utility of specific codons
-
into the vector pET30 for expression in Escherichia coli BL21Star DE3 cells
isozyme mPGES-1, recombinant functional expression in Spodoptera frugiperda Sf9 cells using the baculovirus transfection method
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
100 units/ml interleukin-1beta induces the expression of COX-2 and mPGES-1 in osteoarthritic chondrocytes
-
interleukin-1beta does not change expression of MPGES-1 in the prostate cancer cell lines
-
mPGES-2 immunoreactivity is particularly elevated in the pyramidal neurons of brains from three of five sporadic and four of five familial Alzheimer's disease patients compared with four of five age-matched control brains that showed minimal immunoreactivity
-
the enzyme shows elevated levels in the cartilages and chondrocytes of patients suffering from osteoarthritis. The enzyme is overexpressed in 80% of several cancer cells
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
drug development
medicine
drug development
-
the enzyme constitues an attractive drug target for treatment of inflammatory diseases
drug development
-
the enzyme is a potential target for therapy of breast cancer
medicine
-
a considerable increase of mPGES-2 expression is observed in human colorectal cancer
medicine
-
17beta-estradiol and proinflammatory cytokines can act together to up-regulate PTGES, the finding supports a model whereby estrogens and inflammatory factors orchestrate a complex network of cross talk and feedback mechanisms that can contribute to hormone-dependent breast tumor growth and progression
medicine
-
licofelone suppresses inflammatory PGE2 formation preferentially by inhibiting mPGES-1 at concentrations that do not affect COX-2
medicine
-
mPGES-1 expression is significantly elevated in Alzheimer's disease tissue
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
medicine
mPGES-1 is a promising target for the development of anti-inflammatory drugs
medicine
-
mPGES-1 plays a role in atherosclerosis, stroke, inflammation, pain and fever
medicine
MPGES1 has been implicated in a number of human diseases or pathological conditions, such as rheumatoid arthritis, fever, and pain, and is therefore regarded as a primary target for development of novel antiinflammatory drugs
medicine
-
the selective inhibition of mPGES-1 generates anti-inflammatory effects without unwanted side effects involving homeostasis
medicine
-
MPGES-1 is an alternative therapeutic target in cancer cells expressing this enzyme
medicine
-
enzyme inhibition can be useful for treating pain, fever, and anorexia
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
McNamara, D.B.; Hussey, J.L.; Kerstein, M.D.; Rosenson, R.S.; Hyman, A.L.; Kadowitz, P.J.
Modulation of prostacyclin synthetase and unmasking of PGE2 isomerase in bovine coronary arterial microsomes
Biochem. Biophys. Res. Commun.
118
33-39
1984
Bos taurus, Canis lupus familiaris, Ovis aries, Homo sapiens
Kelner, M.J.; Uglik, S.F.
Mechanism of prostaglandin E2 release and increase in PGH2/PGE2 isomerase activity by PDGF: involvement of nitric oxide
Arch. Biochem. Biophys.
321
240-243
1994
Homo sapiens
Kelner, M.J.; Uglik, S.F.
PDGF-induces the glutathione-dependent enzyme PGH2/PGE2 isomerase in NIH3T3 and pEJ transformed fibroblasts
Biochem. Biophys. Res. Commun.
198
298-303
1994
Homo sapiens
Han, R.; Tsui, S.; Smith, T.J.
Up-regulation of prostaglandin E2 synthesis by interleukin-1b in human orbital fibroblasts involves coordinate induction of prostaglandin-endoperoxide H synthase-2 and glutathione-dependent prostaglandin E2 synthase expression
J. Biol. Chem.
277
16355-16364
2002
Homo sapiens
Thoren, S.; Weinander, R.; Saha, S.; Jegerschoeld, C.; Pettersson, P.L.; Samuelsson, B.; Hebert, H.; Hamberg, M.; Morgenstern, R.; Jakobsson, P.J.
Human microsomal prostaglandin E synthase-1: purification, functional characterization, and projection structure determination
J. Biol. Chem.
278
22199-22209
2003
Homo sapiens
Jakobsson, P.J.; Thoren, S.; Morgenstern, R.; Samuelsson, B.
Identification of human prostaglandin E synthase: a microsomal, glutathione-dependent, inducible enzyme, constituting a potential novel drug target
Proc. Natl. Acad. Sci. USA
96
7220-7225
1999
Homo sapiens (O14684), Homo sapiens
Ouellet, M.; Falgueyret, J.P.; Ear, P.H.; Pen, A.; Mancini, J.A.; Riendeau, D.; David Percival, M.
Purification and characterization of recombinant microsomal prostaglandin E synthase-1
Protein Expr. Purif.
26
489-495
2002
Homo sapiens (O14684), Homo sapiens
Vazquez-Tello, A.; Fan, L.; Hou, X.; Joyal, J.S.; Mancini, J.A.; Quiniou, C.; Clyman, R.I.; Gobeil, F.Jr.; Varma, D.R.; Chemtob, S.
Intracellular-specific colocalization of prostaglandin E2 synthases and cyclooxygenases in the brain
Am. J. Physiol.
287
R1155-R1163
2004
Homo sapiens, Rattus norvegicus, Sus scrofa
Kudo, I.; Murakami, M.
Prostaglandin E synthase, a terminal enzyme for prostaglandin E2 biosynthesis
J. Biochem. Mol. Biol.
38
633-638
2005
Homo sapiens, Mus musculus, Rattus norvegicus
Mehrotra, S.; Morimiya, A.; Agarwal, B.; Konger, R.; Badve, S.
Microsomal prostaglandin E(2) synthase-1 in breast cancer: a potential target for therapy
J. Pathol.
208
356-363
2006
Homo sapiens
Pettersson, P.L.; Thoren, S.; Jakobsson, P.J.
Human microsomal prostaglandin E synthase 1: a member of the MAPEG protein superfamily
Methods Enzymol.
401
147-161
2005
Homo sapiens
Meadows, J.W.; Pitzer, B.; Brockman, D.E.; Myatt, L.
Differential localization of prostaglandin E synthase isoforms in human placental cell types
Placenta
25
259-265
2004
Homo sapiens
Riendeau, D.; Aspiotis, R.; Ethier, D.; Gareau, Y.; Grimm, E.L.; Guay, J.; Guiral, S.; Juteau, H.; Mancini, J.A.; Methot, N.; Rubin, J.; Friesen, R.W.
Inhibitors of the inducible microsomal prostaglandin E2 synthase (mPGES-1) derived from MK-886
Bioorg. Med. Chem. Lett.
15
3352-3355
2005
Homo sapiens
Duffy, D.M.; Seachord, C.L.; Dozier, B.L.
Microsomal prostaglandin E synthase-1 (mPGES-1) is the primary form of PGES expressed by the primate periovulatory follicle
Hum. Reprod.
20
1485-1492
2005
Homo sapiens, Macaca fascicularis (Q5DI74), Macaca fascicularis (Q6PWL5), Macaca fascicularis (Q9N0A4)
Stark, K.; Toermae, H.; Oliw, E.H.
Co-localization of COX-2, CYP4F8, and mPGES-1 in epidermis with prominent expression of CYP4F8 mRNA in psoriatic lesions
Prostaglandins Other Lipid Mediat.
79
114-125
2006
Homo sapiens
Fujikura, T.; Mukai, M.
Prostaglandin E2 synthase in syncytiotrophoblastic vesicles found in the placental intervillous space
Am. J. Obstet. Gynecol.
196
361-361
2007
Homo sapiens
-
Moon, Y.; Lee, M.; Yang, H.
Involvement of early growth response gene 1 in the modulation of microsomal prostaglandin E synthase 1 by epigallocatechin gallate in A549 human pulmonary epithelial cells
Biochem. Pharmacol.
73
125-135
2007
Homo sapiens
Yamada, T.; Takusagawa, F.
PGH2 degradation pathway catalyzed by GSH-heme complex bound microsomal prostaglandin E2 synthase type 2: the first example of a dual-function enzyme
Biochemistry
46
8414-8424
2007
Homo sapiens
St-Onge, M.; Flamand, N.; Biarc, J.; Picard, S.; Bouchard, L.; Dussault, A.; Laflamme, C.; James, M.J.; Caughey, G.E.; Cleland, L.G.; Borgeat, P.; Pouliot, M.
Characterization of prostaglandin E2 generation through the cyclooxygenase (COX)-2 pathway in human neutrophils
Biochim. Biophys. Acta
1771
1235-1245
2007
Homo sapiens
Bage, T.; Modeer, T.; Kawakami, T.; Quezada, H.C.; Yucel-Lindberg, T.
Regulation of prostaglandin E synthases: effects of siRNA-mediated inhibition of microsomal prostaglandin E synthase-1
Biochim. Biophys. Acta
1773
1589-1598
2007
Homo sapiens
Huang, X.; Yan, W.; Gao, D.; Tong, M.; Tai, H.H.; Zhan, C.G.
Structural and functional characterization of human microsomal prostaglandin E synthase-1 by computational modeling and site-directed mutagenesis
Bioorg. Med. Chem.
14
3553-3562
2006
Homo sapiens
Abdulhameed, M.D.; Hamza, A.; Liu, J.; Huang, X.; Zhan, C.G.
Human microsomal prostaglandin E synthase-1 (mPGES-1) Binding with inhibitors and the quantitative structure-activity Correlation
J. Chem. Inf. Model.
48
179-85
2008
Homo sapiens
Mosca, M.; Polentarutti, N.; Mangano, G.; Apicella, C.; Doni, A.; Mancini, F.; De Bortoli, M.; Coletta, I.; Polenzani, L.; Santoni, G.; Sironi, M.; Vecchi, A.; Mantovani, A.
Regulation of the microsomal prostaglandin E synthase-1 in polarized mononuclear phagocytes and its constitutive expression in neutrophils
J. Leukocyte Biol.
82
320-326
2007
Homo sapiens
Camacho, M.; Gerboles, E.; Escudero, J.R.; Anton, R.; Garcia-Moll, X.; Vila, L.
Microsomal prostaglandin E synthase-1, which is not coupled to a particular cyclooxygenase isoenzyme, is essential for prostaglandin E(2) biosynthesis in vascular smooth muscle cells
J. Thromb. Haemost.
5
1411-1419
2007
Homo sapiens, Homo sapiens (Q9H7Z7)
Payner, T.; Leaver, H.A.; Knapp, B.; Whittle, I.R.; Trifan, O.C.; Miller, S.; Rizzo, M.T.
Microsomal prostaglandin E synthase-1 regulates human glioma cell growth via prostaglandin E(2)-dependent activation of type II protein kinase A
Mol. Cancer Ther.
5
1817-1826
2006
Homo sapiens
Astle, S.; Newton, R.; Thornton, S.; Vatish, M.; Slater, D.M.
Expression and regulation of prostaglandin E synthase isoforms in human myometrium with labour
Mol. Hum. Reprod.
13
69-75
2007
Homo sapiens, Homo sapiens (Q9H7Z7)
Chaudhry, U.A.; Zhuang, H.; Crain, B.J.; Dore, S.
Elevated microsomal prostaglandin-E synthase-1 in Alzheimers disease
Alzheimers Dement. (N. Y.)
4
6-13
2008
Homo sapiens
Hetu, P.O.; Ouellet, M.; Falgueyret, J.P.; Ramachandran, C.; Robichaud, J.; Zamboni, R.; Riendeau, D.
Photo-crosslinking of proteins in intact cells reveals a dimeric structure of cyclooxygenase-2 and an inhibitor-sensitive oligomeric structure of microsomal prostaglandin E2 synthase-1
Arch. Biochem. Biophys.
477
155-162
2008
Homo sapiens
Kim, W.I.; Choi, K.A.; Do, H.S.; Yu, Y.G.
Expression and purification of human mPGES-1 in E. coli and identification of inhibitory compounds from a drug-library
BMB Rep.
41
808-813
2008
Homo sapiens
Frasor, J.; Weaver, A.E.; Pradhan, M.; Mehta, K.
Synergistic up-regulation of prostaglandin E synthase expression in breast cancer cells by 17beta-estradiol and proinflammatory cytokines
Endocrinology
149
6272-6279
2008
Homo sapiens
Hammarberg, T.; Hamberg, M.; Wetterholm, A.; Hansson, H.; Samuelsson, B.; Haeggstroem, J.Z.
Mutation of a critical arginine in microsomal prostaglandin E synthase-1 shifts the isomerase activity to a reductase activity that converts prostaglandin H2 into prostaglandin F2{alpha}
J. Biol. Chem.
284
301-305
2009
Homo sapiens (O14684), Homo sapiens
Xing, L.; Kurumbail, R.G.; Frazier, R.B.; Davies, M.S.; Fujiwara, H.; Weinberg, R.A.; Gierse, J.K.; Caspers, N.; Carter, J.S.; McDonald, J.J.; Moore, W.M.; Vazquez, M.L.
Homo-timeric structural model of human microsomal prostaglandin E synthase-1 and characterization of its substrate/inhibitor binding interactions
J. Comput. Aided Mol. Des.
23
13-24
2009
Homo sapiens (O14684), Homo sapiens
Lee, I.Y.; Cho, W.; Kim, J.; Park, C.S.; Choe, J.
Human follicular dendritic cells interact with T cells via expression and regulation of cyclooxygenases and prostaglandin E and I synthases
J. Immunol.
180
1390-1397
2008
Homo sapiens
Friesen, R.W.; Mancini, J.A.
Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target
J. Med. Chem.
51
4059-4067
2008
Homo sapiens
Koeberle, A.; Zettl, H.; Greiner, C.; Wurglics, M.; Schubert-Zsilavecz, M.; Werz, O.
Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase
J. Med. Chem.
51
8068-8076
2008
Homo sapiens
Koeberle, A.; Siemoneit, U.; Buehring, U.; Northoff, H.; Laufer, S.; Albrecht, W.; Werz, O.
Licofelone suppresses prostaglandin E2 formation by interference with the inducible microsomal prostaglandin E2 synthase-1
J. Pharmacol. Exp. Ther.
326
975-982
2008
Homo sapiens
Hamza, A.; Abdulhameed, M.D.; Zhan, C.G.
Understanding microscopic binding of human microsomal prostaglandin E synthase-1 with substrates and inhibitors by molecular modeling and dynamics simulation
J. Phys. Chem. B
112
7320-7329
2008
Homo sapiens (O14684), Homo sapiens
Jegerschoeld, C.; Pawelzik, S.C.; Purhonen, P.; Bhakat, P.; Gheorghe, K.R.; Gyobu, N.; Mitsuoka, K.; Morgenstern, R.; Jakobsson, P.J.; Hebert, H.
Structural basis for induced formation of the inflammatory mediator prostaglandin E2
Proc. Natl. Acad. Sci. USA
105
11110-11115
2008
Homo sapiens (O14684), Homo sapiens
Megias, J.; Guillen, M.I.; Clerigues, V.; Rojo, A.I.; Cuadrado, A.; Castejon, M.A.; Gomar, F.; Alcaraz, M.J.
Heme oxygenase-1 induction modulates microsomal prostaglandin E synthase-1 expression and prostaglandin E(2) production in osteoarthritic chondrocytes
Biochem. Pharmacol.
77
1806-1813
2009
Homo sapiens
Mbalaviele, G.; Pauley, A.M.; Shaffer, A.F.; Zweifel, B.S.; Mathialagan, S.; Mnich, S.J.; Nemirovskiy, O.V.; Carter, J.; Gierse, J.K.; Wang, J.L.; Vazquez, M.L.; Moore, W.M.; Masferrer, J.L.
Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor
Biochem. Pharmacol.
79
1445-1454
2010
Homo sapiens, Rattus norvegicus
Li, Y.; Angelastro, M.; Shimshock, S.; Reiling, S.; Vaz, R.J.
On the mechanism of microsomal prostaglandin E synthase type-2--a theoretical study of endoperoxide reaction with MeS-
Bioorg. Med. Chem. Lett.
20
338-340
2010
Homo sapiens
Chaudhry, U.; Zhuang, H.; Dore, S.
Microsomal prostaglandin E synthase-2: cellular distribution and expression in Alzheimers disease
Exp. Neurol.
223
359-365
2010
Homo sapiens
Hamza, A.; Tong, M.; AbdulHameed, M.D.; Liu, J.; Goren, A.C.; Tai, H.H.; Zhan, C.G.
Understanding microscopic binding of human microsomal prostaglandin E synthase-1 (mPGES-1) trimer with substrate PGH2 and cofactor GSH: insights from computational alanine scanning and site-directed mutagenesis
J. Phys. Chem. B
114
5605-5616
2010
Homo sapiens (O14684), Homo sapiens
Sveinbjoernsson, B.; Schumacher, M.C.; Hamberg, M.; Samuelsson, B.; Jakobsson, P.J.; Kogner, P.; Radmark, O.
Microsomal prostaglandin E synthase 1 determines tumor growth in vivo of prostate and lung cancer cells
Proc. Natl. Acad. Sci. USA
106
18757-18762
2009
Homo sapiens
Wu, T.Y.; Juteau, H.; Ducharme, Y.; Friesen, R.W.; Guiral, S.; Dufresne, L.; Poirier, H.; Salem, M.; Riendeau, D.; Mancini, J.; Brideau, C.
Biarylimidazoles as inhibitors of microsomal prostaglandin E2 synthase-1
Bioorg. Med. Chem. Lett.
20
6978-6982
2010
Homo sapiens
Greiner, C.; Zettl, H.; Koeberle, A.; Pergola, C.; Northoff, H.; Schubert-Zsilavecz, M.; Werz, O.
Identification of 2-mercaptohexanoic acids as dual inhibitors of 5-lipoxygenase and microsomal prostaglandin E2 synthase-1
Bioorg. Med. Chem.
19
3394-3401
2011
Homo sapiens
Lu, D.; Han, C.; Wu, T.
Microsomal prostaglandin E synthase-1 inhibits PTEN and promotes experimental cholangiocarcinogenesis and tumor progression
Gastroenterology
140
2084-2094
2011
Homo sapiens
Pawelzik, S.C.; Uda, N.R.; Spahiu, L.; Jegerschoeld, C.; Stenberg, P.; Hebert, H.; Morgenstern, R.; Jakobsson, P.J.
Identification of key residues determining species differences in inhibitor binding of microsomal prostaglandin E synthase-1
J. Biol. Chem.
285
29254-29261
2010
Homo sapiens, Rattus norvegicus
De Simone, R.; Chini, M.G.; Bruno, I.; Riccio, R.; Mueller, D.; Werz, O.; Bifulco, G.
Structure-based discovery of inhibitors of microsomal prostaglandin E2 synthase-1, 5-lipoxygenase and 5-lipoxygenase-activating protein: promising hits for the development of new anti-inflammatory agents
J. Med. Chem.
54
1565-1575
2011
Homo sapiens
Hieke, M.; Greiner, C.; Dittrich, M.; Reisen, F.; Schneider, G.; Schubert-Zsilavecz, M.; Werz, O.
Discovery and biological evaluation of a novel class of dual microsomal prostaglandin E2 synthase-1/5-lipoxygenase inhibitors based on 2-[(4,6-diphenethoxypyrimidin-2-yl)thio]hexanoic acid
J. Med. Chem.
54
4490-4507
2011
Homo sapiens
Shang, E.; Wu, Y.; Liu, P.; Liu, Y.; Zhu, W.; Deng, X.; He, C.; He, S.; Li, C.; Lai, L.
Benzo[d]isothiazole 1,1-dioxide derivatives as dual functional inhibitors of 5-lipoxygenase and microsomal prostaglandin E2 synthase-1
Bioorg. Med. Chem. Lett.
24
2764-2767
2014
Homo sapiens
Wiegard, A.; Hanekamp, W.; Griessbach, K.; Fabian, J.; Lehr, M.
Pyrrole alkanoic acid derivatives as nuisance inhibitors of microsomal prostaglandin E2 synthase-1
Eur. J. Med. Chem.
48
153-163
2012
Homo sapiens
Sjoegren, T.; Nord, J.; Ek, M.; Johansson, P.; Liu, G.; Geschwindner, S.
Crystal structure of microsomal prostaglandin E2 synthase provides insight into diversity in the MAPEG superfamily
Proc. Natl. Acad. Sci. USA
110
3806-3811
2013
Homo sapiens (O14684), Homo sapiens
Korotkova, M.; Jakobsson, P.
Characterization of microsomal prostaglandin E synthase 1 inhibitors
Basic Clin. Pharmacol. Toxicol.
114
64-69
2014
Homo sapiens (O14684)
Banerjee, A.; Pawar, M.Y.; Patil, S.; Yadav, P.S.; Kadam, P.A.; Kattige, V.G.; Deshpande, D.S.; Pednekar, P.V.; Pisat, M.K.; Gharat, L.A.
Development of 2-aryl substituted quinazolin-4(3H)-one, pyrido[4,3-d]pyrimidin-4(3H)-one and pyrido[2,3-d]pyrimidin-4(3H)-one derivatives as microsomal prostaglandin E2 synthase-1 inhibitors
Bioorg. Med. Chem. Lett.
24
4838-4844
2014
Homo sapiens (O14684), Homo sapiens
Kuklish, S.L.; Antonysamy, S.; Bhattachar, S.N.; Chandrasekhar, S.; Fisher, M.J.; Fretland, A.J.; Gooding, K.; Harvey, A.; Hughes, N.E.; Luz, J.G.; Manninen, P.R.; McGee, J.E.; Navarro, A.; Norman, B.H.; Partridge, K.M.; Quimby, S.J.; Schiffler, M.A.; Sloan, A.V.; Warshawsky, A.M.; York, J.S.; Yu, X.P.
Characterization of 3,3-dimethyl substituted N-aryl piperidines as potent microsomal prostaglandin E synthase-1 inhibitors
Bioorg. Med. Chem. Lett.
26
4824-4828
2016
Homo sapiens
Partridge, K.M.; Antonysamy, S.; Bhattachar, S.N.; Chandrasekhar, S.; Fisher, M.J.; Fretland, A.; Gooding, K.; Harvey, A.; Hughes, N.E.; Kuklish, S.L.; Luz, J.G.; Manninen, P.R.; McGee, J.E.; Mudra, D.R.; Navarro, A.; Norman, B.H.; Quimby, S.J.; Schiffler, M.A.; Sloan, A.V.; Warshawsky, A.M.; Weller, J.M.; Yor, Y.o.r.k.
Discovery and characterization of [(cyclopentyl)ethyl]benzoic acid inhibitors of microsomal prostaglandin E synthase-1
Bioorg. Med. Chem. Lett.
27
1478-1483
2017
Homo sapiens (O14684), Homo sapiens
Muthukaman, N.; Tambe, M.; Deshmukh, S.; Pisal, D.; Tondlekar, S.; Shaikh, M.; Sarode, N.; Kattige, V.G.; Pisat, M.; Sawant, P.; Honnegowda, S.; Karande, V.; Kulkarni, A.; Behera, D.; Jadhav, S.B.; Sangana, R.R.; Gudi, G.S.; Khairatkar-Joshi, N.; Gharat, L.A.
Discovery of furan and dihydrofuran-fused tricyclic benzo[d]imidazole derivatives as potent and orally efficacious microsomal prostaglandin E synthase-1 (mPGES-1) inhibitors Part-1
Bioorg. Med. Chem. Lett.
27
5131-5138
2017
Homo sapiens (O14684)
Li, D.; Howe, N.; Dukkipati, A.; Shah, S.T.; Bax, B.D.; Edge, C.; Bridges, A.; Hardwicke, P.; Singh, O.M.; Giblin, G.; Pautsch, A.; Pfau, R.; Schnapp, G.; Wang, M.; Olieric, V.; Caffrey, M.
Crystallizing membrane proteins in the lipidic mesophase. Experience with human prostaglandin E2 synthase 1 and an evolving strategy
Cryst. Growth Des.
14
2034-2047
2014
Homo sapiens (O14684), Homo sapiens
Schiffler, M.A.; Antonysamy, S.; Bhattachar, S.N.; Campanale, K.M.; Chandrasekhar, S.; Condon, B.; Desai, P.V.; Fisher, M.J.; Groshong, C.; Harvey, A.; Hickey, M.J.; Hughes, N.E.; Jones, S.A.; Kim, E.J.; Kuklish, S.L.; Luz, J.G.; Norman, B.H.; Rathmell, R.E.; Rizzo, J.R.; Seng, T.W.; Thibodeaux, S.J.; Woods, T.A.
Discovery and characterization of 2-acylaminoimidazole microsomal prostaglandin E synthase-1 inhibitors
J. Med. Chem.
59
194-205
2016
Homo sapiens
Verhoff, M.; Seitz, S.; Paul, M.; Noha, S.M.; Jauch, J.; Schuster, D.; Werz, O.
Tetra- and pentacyclic triterpene acids from the ancient anti-inflammatory remedy frankincense as inhibitors of microsomal prostaglandin E2 synthase-1
J. Nat. Prod.
77
1445-1451
2014
Homo sapiens
Bahia, M.S.; Katare, Y.K.; Silakari, O.; Vyas, B.; Silakari, P.
Inhibitors of microsomal prostaglandin E2 synthase-1 enzyme as emerging anti-inflammatory candidates
Med. Res. Rev.
34
825-855
2014
Homo sapiens
Werz, O.; Seegers, J.; Schaible, A.; Weinigel, C.; Barz, D.; Koeberle, A.; Allegrone, G.; Pollastro, F.; Zampieri, L.; Grassi, G.; Appendino, G.
Cannflavins from hemp sprouts, a novel cannabinoid-free hemp food product, target microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase
PharmaNutrition
2
53-60
2014
Homo sapiens
-
Raouf, J.; Rafique, N.; Goodman, M.; Idborg, H.; Bergqvist, F.; Armstrong, R.; Jakobsson, P.; Morgenstern, R.; Spahiu, L.
Arg126 and Asp49 are essential for the catalytic function of microsomal prostaglandin E2 synthase 1 and Ser127 is not
PLoS ONE
11
e163600
2016
Homo sapiens (O14684)
Brock, J.S.; Hamberg, M.; Balagunaseelan, N.; Goodman, M.; Morgenstern, R.; Strandback, E.; Samuelsson, B.; Rinaldo-Matthis, A.; Haeggstroem, J.Z.
A dynamic Asp-Arg interaction is essential for catalysis in microsomal prostaglandin E2 synthase
Proc. Natl. Acad. Sci. USA
113
972-977
2016
Homo sapiens (O14684), Homo sapiens
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