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Literature summary extracted from

  • Wiegard, A.; Hanekamp, W.; Griessbach, K.; Fabian, J.; Lehr, M.
    Pyrrole alkanoic acid derivatives as nuisance inhibitors of microsomal prostaglandin E2 synthase-1 (2012), Eur. J. Med. Chem., 48, 153-163.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.3 (1-benzyl-4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl)acetic acid 35% inhibition at 0.001 mM Homo sapiens
5.3.99.3 (4-dodecanoyl-1,3,5-trimethyl-1H-pyrrol-2-yl)acetic acid 22% inhibition at 0.001 mM Homo sapiens
5.3.99.3 (4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl)acetic acid 17% inhibition at 0.001 mM Homo sapiens
5.3.99.3 1-benzyl-4-dodecanoyl-3,5-dimethyl-1H-pyrrole-2-carboxylic acid 65% inhibition at 0.001 mM Homo sapiens
5.3.99.3 2-(4-dodecanoyl-3,5-dimethyl-1-phenylpyrrol-2-yl)acetic acid 23% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-(1,3,5-trimethyl-4-octadecanoyl-1H-pyrrol-2-yl)propanoic acid 97% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-(1,3,5-trimethyl-4-tetradecanoyl-1H-pyrrol-2-yl)propanoic acid 91% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-(1-benzyl-4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl)propanoic acid 62% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-(1-benzyl-4-dodecanoyl-5-methyl-3-phenylpyrrol-2-yl)propionic acid 64% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-(4-dodecanoyl-1,3,5-trimethyl-1H-pyrrol-2-yl)propanoic acid 54% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)-N-(benzenesulfonyl)propanamide 77% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)-N-(methanesulfonyl)propanamide 52% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)propanamide 39% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)propanehydrazide 35% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)propanenitrile 22% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-(4-dodecanoyl-1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)propanoic acid 90% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-(4-dodecanoyl-3,5-dimethyl-1-phenylpyrrol-2-yl)propionic acid 65% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-(4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl)propanoic acid 38% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-(4-hexadecanoyl-1,3,5-trimethyl-1H-pyrrol-2-yl)propanoic acid 97% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-[1-(4-carbamoylbenzyl)-4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl]propanoic acid 28% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-[1-(4-chlorobenzyl)-4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl]propanoic acid 78% inhibition at 0.001 mM Homo sapiens
5.3.99.3 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 Homo sapiens
5.3.99.3 3-[4-(4-butoxybenzoyl)-1,3,5-trimethyl-1H-pyrrol-2-yl]propanoic acid 32% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-[4-dodecanoyl-1-(4-hydroxybenzyl)-3,5-dimethyl-1H-pyrrol-2-yl]propanoic acid 53% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-[4-dodecanoyl-1-(4-methoxybenzyl)-3,5-dimethyl-1H-pyrrol-2-yl]propanoic acid 72% inhibition at 0.001 mM Homo sapiens
5.3.99.3 3-[4-dodecanoyl-3,5-dimethyl-1-(4-methylbenzyl)-1H-pyrrol-2-yl]propanoic acid 52% inhibition at 0.001 mM Homo sapiens
5.3.99.3 4-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)butanoic acid 70% inhibition at 0.001 mM Homo sapiens
5.3.99.3 4-dodecanoyl-1,3,5-trimethyl-1H-pyrrole-2-carboxylic acid 37% inhibition at 0.001 mM; 59% inhibition at 0.001 mM Homo sapiens
5.3.99.3 4-dodecanoyl-3,5-dimethyl-1-phenylpyrrole-2-carboxylic acid 99% inhibition at 0.001 mM Homo sapiens
5.3.99.3 4-dodecanoyl-3,5-dimethyl-1H-pyrrole-2-carboxylic acid 62% inhibition at 0.001 mM Homo sapiens
5.3.99.3 4-[[2-(2-carboxyethyl)-4-dodecanoyl-3,5-dimethyl-1H-pyrrol-1-yl]methyl]benzoic acid 27% inhibition at 0.001 mM Homo sapiens
5.3.99.3 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 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
5.3.99.3 microsome isozyme mPGES-1 Homo sapiens
-
-

Organism

EC Number Organism UniProt Comment Textmining
5.3.99.3 Homo sapiens
-
 microsomal isozyme mPGES-1
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.3.99.3 (5Z,13E,15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
 Homo sapiens (5Z,13E,15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
 ?

Synonyms

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

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
5.3.99.3 22
-
 assay at room temperature Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
5.3.99.3 7.2
-
 assay at Homo sapiens