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(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-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-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
-
-
aminomethyl 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzenesulfinate
-
-
benzothiophene gamma-hydroxybutenolide
-
Bis(3-carboxy-4-nitrophenyl)disulfide
-
-
cysteinyl leukotriene LTC4
-
-
deoxy-prostaglandin J2
-
IC50: 0.0003 mM
Diallyl disulfide-oxide
-
i.e. allicin
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
-
-
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
imidazole
imidazole stacks on the bound heme and inhibits heme oxidation by H2O2, heme dissociation by DTT, and catalytic activity
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-0886
0.002 mM, 50% inhibition
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
-
p-hydroxymercuribenzoate
-
-
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
sodium 3-[1-[(4-chlorophenyl)methyl]-5-(2-fluoro[1,1'-biphenyl]-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoate
-
-
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
(4E)-4-[2-(3-bromophenyl)hydrazin-1-ylidene]-1-ethanethioyl-3-methyl-4,5-dihydro-1H-pyrazol-5-one
-
-
(4E)-4-[2-(3-bromophenyl)hydrazin-1-ylidene]-1-ethanethioyl-3-methyl-4,5-dihydro-1H-pyrazol-5-one
-
-
1-[5-chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide
PF-4693627
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
-
-
2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
MF-63
2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
-
fludrocortisone
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
-
2-chloro-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
-
-
2-chloro-N-[3-(naphthalen-1-ylcarbamoyl)phenyl]benzamide
-
selective for human over rat MPGES1
2-chloro-N-[3-(naphthalen-1-ylcarbamoyl)phenyl]benzamide
-
inhibitor of mutant enzyme V131T/F135L/F138A, but not of the wild type enzyme
3-(4-dodecanoyl-1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)propanoic acid
-
90% inhibition at 0.001 mM
3-(4-dodecanoyl-1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)propanoic 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-[1-(4-chlorobenzyl)-5-(2-fluorobiphenyl-4-yl)-3-methyl-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
-
12% residual activity at 0.03 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
4-hydroxymercuribenzoate
-
4-hydroxymercuribenzoate
-
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
-
AF3442
-
dexamethasone
-
inhibition of cytokine-induced expression of isoform mPGES-1, while isoforms mPGES-2 and cPGES remain unaffected
dexamethasone
-
anti-inflammatory glucocorticoid
Indocyanine green
-
-
indomethacin
-
-
MF63
-
-
MF63
i.e. 2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-isophthalonitrile
MK 886
-
inhibits microsomal PGE2
MK 886
-
inhibits microsomal PGE2
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
MK-886
-
glutamate-induced PGE2 production is suppressed almost completely by MK-886 at a concentration of 0.003 mM or higher
MK-886
-
glutamate-induced PGE2 production is suppressed almost completely by MK-886 at a concentration of 0.003 mM or higher
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
N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-1,1-dioxo-1,2-dihydro-1lambda~6~,2-benzothiazine-3-carboxamide
-
NEM
-
-
NS-398
-
COX-2 inhibitor, IC50: 0.01-0.02 mM
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
PF-9184
-
poor mPGES-1 inhibitor, i.e. N-(3',4'-dichlorobiphenyl-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide
SC-236
-
-
additional information
-
glucocorticosteroids, down-regulation of the enzyme
-
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
-
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
-
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
-
anti-inflammatory glucocorticoids
-