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Literature summary for 5.3.99.3 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

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

Localization

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
(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

Organism UniProt Comment Textmining
Mus musculus Q9JM51
-
-

Source Tissue

Source Tissue Comment Organism Textmining
RAW-264.7 cell
-
Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(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

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

IC50 Value

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