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5.3.99.3: prostaglandin-E synthase

This is an abbreviated version!
For detailed information about prostaglandin-E synthase, go to the full flat file.

Word Map on EC 5.3.99.3

Reaction

(13E)-(15S)-15-hydroxy-9-oxoprosta-10,13-dienoate
=
(13E)-(15S)-15-hydroxy-9-oxoprosta-11,13-dienoate

Synonyms

CPGES, cPGES/p23, cytosolic prostaglandin E synthase, cytosolic prostaglandin E(2) synthase, cytosolic prostaglandin E(2) synthase-2, endoperoxide isomerase, Isomerase, prostaglandin R2 E-, membrane-associated PGE2 synthase, membrane-associated prostaglandin E synthase-2, membrane-associated prostaglandin E(2) synthase-1, membrane-associated prostaglandin E(2) synthase-2, microsomal PG synthase-1, microsomal PGE synthase-1, microsomal PGE2 synthase, microsomal PGE2 synthase-1, microsomal prostaglandin E synthase, microsomal prostaglandin E synthase 1, microsomal prostaglandin E synthase type 1, microsomal prostaglandin E synthase type 2, microsomal prostaglandin E synthase type-2, microsomal prostaglandin E synthase-1, microsomal prostaglandin E synthase-2, microsomal prostaglandin E(2) synthase-1, microsomal prostaglandin E(2) synthase-2, microsomal prostaglandin E2 synthase 1, microsomal prostaglandin E2 synthase type 1, microsomal prostaglandin E2 synthase-1, microsomal prostaglandin synthase-1, microsomal prostaglandin-E synthase-1, mPGE synthase-2, mPGES, mPGES-1, mPGES-2, MPGES1, MPGES2, p23, PGE, PGE isomerase, PGE synthase, PGE synthase-1, PGE2, PGE2 isomerase, PGE2 synthase, PGE2-synthase, PGES, PGES-1, PGES-2, PGH-PGE isomerase, PGH2/PGE2 isomerase, prostagandin-E synthetase, Prostaglandin E synthase, prostaglandin E synthase 1, prostaglandin E synthase type 2, prostaglandin E synthase-1, prostaglandin E synthase-2, Prostaglandin E2 isomerase, prostaglandin E2 synthase, prostaglandin E2 synthase-1, prostaglandin E2 synthase-I, 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 synthase-1, prostaglandin-E synthase, Prostaglandin-H2 E-isomerase, PTGES

ECTree

     5 Isomerases
         5.3 Intramolecular oxidoreductases
             5.3.99 Other intramolecular oxidoreductases
                5.3.99.3 prostaglandin-E synthase

Inhibitors

Inhibitors on EC 5.3.99.3 - prostaglandin-E synthase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
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-[2,5-bis(2-cyclohexylethoxy)benzylidene]hexanoic acid
-
-
(2E)-2-[2,5-bis(2-phenylethoxy)benzylidene]hexanoic acid
-
-
(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
(2R)-2-([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
-
(2S)-2-([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
-
(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
-
-
11-oxo-beta-boswellic acid
-
-
15-deoxy-DELTA12,14-prostaglandin J2
-
-
2(4-(3-biphenyloxypropoxy)phenylthio)hexanoic acid
-
-
2-(2,3-diphenethoxybenzylidene)hexanoic acid
-
-
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)-4-(4-chlorophenyl)-1H-imidazole
-
-
2-(2-chloro-6-fluorophenyl)-4-(4-phenoxyphenyl)-1H-imidazole
-
-
2-(2-chloro-6-fluorophenyl)-4-[4-(2-phenylethyl)phenyl]-1H-imidazole
-
-
2-(2-chloro-6-fluorophenyl)-4-[4-(phenylethynyl)phenyl]-1H-imidazole
-
-
2-(2-chloro-6-fluorophenyl)-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
-
-
2-(2-chloro-6-fluorophenyl)-4-[4-(phenylsulfonyl)phenyl]-1H-imidazole
-
-
2-(2-chloro-6-fluorophenyl)-4-[4-[(E)-2-phenylethenyl]phenyl]-1H-imidazole
-
-
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-(3,5-diphenethoxybenzyl)hexanoic acid
-
-
2-(3,5-diphenethoxybenzylidene)hexanoic acid
-
-
2-(4-bromophenyl)-5-(2-chloro-6-fluorophenyl)-1H-imidazole
-
-
2-(4-dodecanoyl-3,5-dimethyl-1-phenylpyrrol-2-yl)acetic acid
-
23% inhibition at 0.001 mM
2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
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-cyanophenyl)ethoxy]pyrimidin-2-yl]sulfanyl)hexanoic acid
-
-
2-([4,6-bis[2-(4-methoxyphenyl)ethoxy]pyrimidin-2-yl]sulfanyl)hexanoic acid
-
63.7% residual activity at 0.01 mM
2-([4,6-bis[2-(4-methylphenyl)ethoxy]pyrimidin-2-yl]sulfanyl)hexanoic acid
-
-
2-([4,6-bis[2-(4-nitrophenyl)ethoxy]pyrimidin-2-yl]sulfanyl)hexanoic acid
-
-
2-([4,6-bis[2-(thiophen-3-yl)ethoxy]pyrimidin-2-yl]sulfanyl)hexanoic acid
-
-
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-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
-
2-([4-[3-(2-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
88.3% residual activity at 0.01 mM
2-([4-[3-(2-methylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
-
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-(4-chloro-2-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
-
2-([4-[3-(4-methylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
-
2-([4-[3-(5,6,7,8-tetrahydronaphthalen-1-yloxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
-
2-([4-[3-(quinolin-6-yloxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
-
2-bromo-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
-
-
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-(1H-imidazol-2-yl)benzamide
2-chloro-5-[(2,2-dimethylpropanamido)methyl]-N-[4-oxo-3-[4-(trifluoromethyl)phenyl]-3,4-dihydrophthalazin-6-yl]benzamide
-
2-chloro-5-[(3,3-dimethylbutanamido)methyl]-N-(1H-imidazol-2-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-(1H-imidazol-2-yl)-5-[(2-methylpropanamido)methyl]benzamide
-
-
2-chloro-N-[3-(naphthalen-1-ylcarbamoyl)phenyl]benzamide
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-[(3,5-diphenethoxyphenyl)thio]hexanoic acid
-
-
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-[(4,6-diphenethoxypyrimidin-2-yl)thio]hexanoic acid
-
-
2-[(4-[3-[2-(propan-2-yl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
-
-
2-[(4-[3-[3-(propan-2-yl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
-
-
2-[(4-[3-[3-(trifluoromethyl)phenoxy]propoxy]phenyl)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-[2,3-bis(2-phenylethoxy)benzyl]hexanoic acid
-
-
2-[2,4-bis(2-phenylethoxy)benzyl]hexanoic acid
-
90.1% residual activity at 0.01 mM
2-[2,5-bis(2-phenylethoxy)benzyl]hexanoic acid
-
-
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-[3,4-bis(2-phenylethoxy)benzyl]hexanoic acid
-
-
2-[3,5-bis(2-phenylethoxy)phenoxy]hexanoic 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-bromophenyl)-1H-imidazol-2-yl]benzonitrile
-
-
2-[4-(4-chlorophenyl)-1H-imidazol-2-yl]-3-fluorobenzonitrile
-
-
2-[4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)phenyl]propan-2-ol
-
-
2-[4-[3-(2,3-dimethylphenoxy)propoxy]benzyl]hexanoic acid
-
-
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-cyclohexylethoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
-
-
2-[[4,6-bis(2-cyclopentylethoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
-
90% residual activity at 0.01 mM
2-[[4,6-bis(2-cyclopropylethoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
-
-
2-[[4,6-bis(2-phenylethoxy)pyrimidin-2-yl]sulfanyl]butanoic acid
-
-
2-[[4,6-bis(2-phenylethoxy)pyrimidin-2-yl]sulfanyl]octanoic acid
-
-
2-[[4,6-bis(3-methylbutoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
-
54.5% residual activity at 0.01 mM
2-[[4,6-bis(3-phenylpropoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
-
-
2-[[4,6-bis(4-phenylbutoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
-
-
2-[[4,6-bis(benzyloxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
-
-
2-[[4-(3-phenoxypropoxy)phenyl]sulfanyl]hexanoic acid
-
81.9% residual activity at 0.01 mM
2-[[4-(biphenyl-4-ylamino)-6-chloropyrimidin-2-yl]sulfanyl]nonanoic acid
-
-
3,4-bis-(3-benzo[b]thiophen-3-yl-phenyl)-5-hydroxy-5H-furan-2-one
-
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-benzothiophen-2-yl)-2-bromo-5-hydroxycyclopent-2-en-1-one
-
-
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-bromophenyl)-5-(2-chloro-6-fluorophenyl)-1H-1,2,4-triazole
-
-
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-1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)propanoic acid
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-(naphthalen-1-ylamino)-6-nitrobenzo[d]isothiazole 1,1-dioxide
-
-
3-benzamidocarbazole
-
-
3-bromo-4-(4'-butyl-biphenyl-4-yl)-5-hydroxy-5H-furan-2-one
-
3-bromo-5-hydroxy-4-[1,1':4',1'']terphenyl-4-yl-5H-furan-2-one
-
3-O-acetyl-28-hydroxylupeolic acid
-
31.1% residual activity at 0.01 mM
3-O-acetyllupeolic acid
-
51.4% residual activity at 0.01 mM
3-O-acteyl-11-oxo-beta-boswellic acid
-
-
3-O-acteyl-beta-boswellic acid
-
-
3-oxo-8,24-dienetirucallic acid
-
16.7% residual activity at 0.01 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
-
3alpha-acetoxy-7,24-dienetirucallic acid
-
20.6% residual activity at 0.01 mM
3alpha-acetoxy-8,24-dienetirucallic acid
-
36.8% residual activity at 0.01 mM
3alpha-hydroxy-7,24-dienetirucallic acid
-
29.6% residual activity at 0.01 mM
3alpha-hydroxy-8,24-dienetirucallic acid
-
3.5% residual activity at 0.01 mM
3beta-hydroxy-8,24-dienetirucallic acid
-
29.2% residual activity at 0.01 mM
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,(23)-dihydro-11-oxo-roburic acid
-
21.6% residual activity at 0.01 mM
4,(23)-dihydronyctanthic acid
-
74.1% residual activity at 0.01 mM
4,(23)-dihydroroburic acid
-
92.4% residual activity at 0.01 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'-butyl-biphenyl-4-yl)-3-(4-butyl-phenyl)-5-hydroxy-5H-furan-2-one
-
4-(4'-phenoxybiphenyl-4-yl)-1-(3-phenylpropyl)-1H-1,2,3-triazole
-
88.7% residual activity at 0.03 mM
4-(4-benzylphenyl)-2-(2-chloro-6-fluorophenyl)-1H-imidazole
-
-
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-(biphenyl-4-yl)-2-(2-chloro-6-fluorophenyl)-1H-imidazole
-
-
4-(phenylethynyl)-N-(2-sulfamoylbenzene-1-sulfonyl)benzamide
AZ-7847
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-1,3,5-trimethyl-1H-pyrrole-2-carboxylic acid
-
37% inhibition at 0.001 mM; 59% inhibition at 0.001 mM
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-hydroxymercuribenzoate
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
5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole
-
-
5-(4-bromophenyl)-3-(2-chloro-6-fluorophenyl)-1,2,4-oxadiazole
-
-
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-hydroxy-3-naphthalen-2-yl-4-(3-naphthalen-2-yl-phenyl)-5H-furan-2-one
-
5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)-2-(trifluoromethyl)benzamide
-
-
5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)-2-methylbenzamide
-
-
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-(phenylethynyl)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-ethynylpyridine
-
-
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-bromo-2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
5-[5-chloro-2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
-
-
6-nitro-3-(m-tolylamino) benzo[d]isothiazole 1,1-dioxide
-
i.e. JMC-7
6-nitro-N-phenyl-1,2-benzothiazol-3-amine 1,1-dioxide
-
-
6-nitro-N-[3-(propan-2-yl)phenyl]-1,2-benzothiazol-3-amine 1,1-dioxide
-
-
7-hydroxy-N,N'-bis(2,4,6-trimethylphenyl)naphthalene-1,3-disulfonamide
-
-
acetaminophen
-
-
AF3442
aminomethyl 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzenesulfinate
-
-
arachidonic acid
-
-
benzothiophene gamma-hydroxybutenolide
-
beta-boswellic acid
-
-
biarylimidazole
-
-
Bis(3-carboxy-4-nitrophenyl)disulfide
-
-
cannflavin A
-
-
cannflavin B
-
-
Cay 10526
-
-
cysteinyl leukotriene LTC4
-
-
deoxy-prostaglandin J2
-
IC50: 0.0003 mM
dexamethasone
Diallyl disulfide-oxide
-
i.e. allicin
dyphylline
-
-
eicosapentaenoic acid
-
-
ethyl 2-([4-[3-(5,6,7,8-tetrahydronaphthalen-1-yloxy)propoxy]phenyl]sulfanyl)hexanoate
-
-
ethyl 2-([4-[3-(biphenyl-4-yloxy)propoxy]phenyl]sulfanyl)hexanoate
-
-
ethyl 2-([4-[3-(quinolin-6-yloxy)propoxy]phenyl]sulfanyl)hexanoate
-
83.9% residual activity at 0.01 mM
ethyl 2-[[4-chloro-6-(quinolin-6-ylamino)pyrimidin-2-yl]sulfanyl]nonanoate
-
-
geldanamycin
-
-
heme
heme is bound to the enzyme subunits and alters the enzyme catalytic specificity, overview. Heme is attached to the bound GSH by an iron-sulfur bond, but heme cannot bind to mPGES2 in the absence of GSH, other sulfhydryl compounds, such as DTT and 2-mercaptoethanol, are unable to promote heme binding to isozyme mPGES2. Bound heme is oxidized by H2O2, but it does not dissociate from mPGES2
HgCl2
-
-
imidazole
imidazole stacks on the bound heme and inhibits heme oxidation by H2O2, heme dissociation by DTT, and catalytic activity
Indocyanine green
indomethacin
iodoacetamide
-
-
iodoacetic acid
-
-
Iodosobenzoic acid
-
-
leukotriene C4
-
licofelone
-
-
lupeolic acid
-
43.1% 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
-
-
MK 886
MK-0886
0.002 mM, 50% inhibition
MK-886
MK886
-
-
N-(1,3-benzodioxol-4-yl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
-
-
N-(2-methylphenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
-
-
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-(3,4-dimethoxyphenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
-
-
N-(3-bromobenzyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
-
-
N-(3-bromophenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
-
-
N-(3-chloro-2-methylphenyl)-6-[2-chloro-6-(trifluoromethyl)benzamido]-2-(methoxymethyl)-1H-benzimidazole-4-carboxamide
-
N-(3-chlorophenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
-
-
N-(3-methoxyphenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
-
-
N-(3-tert-butylphenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
-
-
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-(4-methoxyphenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
-
-
N-(5-bromonaphthalen-1-yl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
-
-
N-(6-nitro-1,1-dioxido-1,2-benzothiazol-3-yl)quinolin-5-amine
-
-
N-(biphenyl-3-yl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
-
-
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
-
NS-398
Oxacillin
-
-
p-hydroxymercuribenzoate
-
-
PCMB
-
-
PF-4693627
-
PF-9184
resveratrol
-
-
roburic acid
-
83.9% residual activity at 0.01 mM
SB-203580
-
blocks the association of cPGES with casein kinase II and Hsp90, as well as cPGES phosphorylation
SC-236
sodium 3-[1-[(4-chlorophenyl)methyl]-5-(2-fluoro[1,1'-biphenyl]-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoate
-
-
sulindac sulfide
-
-
YS121
-
reversible and noncompetitive inhibition
[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](phenyl)acetic acid
-
-
[[4,6-bis(2-phenylethoxy)pyrimidin-2-yl]sulfanyl]acetic acid
-
66.4% residual activity at 0.01 mM
additional information
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