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Literature summary extracted from

  • Aquino, M.; Guerrero, M.D.; Bruno, I.; Terencio, M.C.; Paya, M.; Riccio, R.
    Development of a second generation of inhibitors of microsomal prostaglandin E synthase 1 expression bearing the gamma-hydroxybutenolide scaffold (2008), Bioorg. Med. Chem., 16, 9056-9064.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.3 3,4-bis-(3-benzo[b]thiophen-3-yl-phenyl)-5-hydroxy-5H-furan-2-one
-
 Mus musculus
5.3.99.3 3-bromo-4-(4'-butyl-biphenyl-4-yl)-5-hydroxy-5H-furan-2-one
-
 Mus musculus
5.3.99.3 3-bromo-5-hydroxy-4-[1,1':4',1'']terphenyl-4-yl-5H-furan-2-one
-
 Mus musculus
5.3.99.3 4-(4'-butyl-biphenyl-4-yl)-3-(4-butyl-phenyl)-5-hydroxy-5H-furan-2-one
-
 Mus musculus
5.3.99.3 5-hydroxy-3-naphthalen-2-yl-4-(3-naphthalen-2-yl-phenyl)-5H-furan-2-one
-
 Mus musculus
5.3.99.3 benzothiophene gamma-hydroxybutenolide
-
 Mus musculus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
5.3.99.3 membrane
-
 Mus musculus 16020
-
5.3.99.3 microsome
-
 Mus musculus
-
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5.3.99.3 (5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate Mus musculus
-
 (5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
5.3.99.3 Mus musculus Q9JM51
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
5.3.99.3 RAW-264.7 cell
-
 Mus musculus
-

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
-
 Mus musculus (5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
5.3.99.3 microsomal prostaglandin E synthase 1
-
 Mus musculus
5.3.99.3 mPGES-1
-
 Mus musculus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.3.99.3 0.00084
-
-
 Mus musculus 5-hydroxy-3-naphthalen-2-yl-4-(3-naphthalen-2-yl-phenyl)-5H-furan-2-one
5.3.99.3 0.0018
-
-
 Mus musculus benzothiophene gamma-hydroxybutenolide
5.3.99.3 0.00224
-
-
 Mus musculus 3-bromo-4-(4'-butyl-biphenyl-4-yl)-5-hydroxy-5H-furan-2-one
5.3.99.3 0.00323
-
-
 Mus musculus 3,4-bis-(3-benzo[b]thiophen-3-yl-phenyl)-5-hydroxy-5H-furan-2-one
5.3.99.3 0.00361
-
-
 Mus musculus 3-bromo-5-hydroxy-4-[1,1':4',1'']terphenyl-4-yl-5H-furan-2-one
5.3.99.3 0.00459
-
-
 Mus musculus 4-(4'-butyl-biphenyl-4-yl)-3-(4-butyl-phenyl)-5-hydroxy-5H-furan-2-one