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Literature summary extracted from

  • Partridge, K.M.; Antonysamy, S.; Bhattachar, S.N.; Chandrasekhar, S.; Fisher, M.J.; Fretland, A.; Gooding, K.; Harvey, A.; Hughes, N.E.; Kuklish, S.L.; Luz, J.G.; Manninen, P.R.; McGee, J.E.; Mudra, D.R.; Navarro, A.; Norman, B.H.; Quimby, S.J.; Schiffler, M.A.; Sloan, A.V.; Warshawsky, A.M.; Weller, J.M.; Yor, Y.o.r.k.
    Discovery and characterization of [(cyclopentyl)ethyl]benzoic acid inhibitors of microsomal prostaglandin E synthase-1 (2017), Bioorg. Med. Chem. Lett., 27, 1478-1483 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.3 1-[5-chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide
-
 Homo sapiens
5.3.99.3 2-chloro-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
-
 Homo sapiens
5.3.99.3 2-[2-[(1S,2S)-2-([1-[4-(trifluoromethoxy)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
 Homo sapiens
5.3.99.3 2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
 Homo sapiens
5.3.99.3 2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]pyridine-3-carboxylic acid
-
 Homo sapiens
5.3.99.3 2-[2-[(1S,2S)-2-([1-[5-(trifluoromethyl)pyridin-2-yl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
 Homo sapiens
5.3.99.3 2-[2-[(1S,2S)-2-[[1-(8-methylquinolin-2-yl)piperidine-4-carbonyl]amino]cyclopentyl]ethyl]benzoic acid
-
 Homo sapiens
5.3.99.3 3-[6-([1,1'-biphenyl]-4-yl)-1-[(4-chlorophenyl)methyl]-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
 Homo sapiens
5.3.99.3 4-chloro-2-([[(1S,2S)-2-(2,2-dimethylpropanamido)cyclopentyl]methyl]amino)benzoic acid
-
 Homo sapiens
5.3.99.3 4-chloro-2-([[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]methyl]amino)benzoic acid
-
 Homo sapiens
5.3.99.3 4-chloro-2-[([(1S,2S)-2-[(1-phenylpiperidine-4-carbonyl)amino]cyclopentyl]methyl)amino]benzoic acid
-
 Homo sapiens
5.3.99.3 4-chloro-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
 Homo sapiens
5.3.99.3 4-chloro-2-[[(1R,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]methoxy]benzoic acid
-
 Homo sapiens
5.3.99.3 4-fluoro-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
 Homo sapiens
5.3.99.3 4-methyl-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
 Homo sapiens
5.3.99.3 N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-1,1-dioxo-1,2-dihydro-1lambda~6~,2-benzothiazine-3-carboxamide
-
 Homo sapiens

Localization

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

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5.3.99.3 Prostaglandin H2 Homo sapiens
-
 Prostaglandin E2
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
5.3.99.3 Homo sapiens O14684
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.3.99.3 Prostaglandin H2
-
 Homo sapiens Prostaglandin E2
-
 ?

Synonyms

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

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.3.99.3 0.000001
-
 pH and temperature not specified in the publication Homo sapiens 2-[2-[(1S,2S)-2-([1-[4-(trifluoromethoxy)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
5.3.99.3 0.000001
-
 pH and temperature not specified in the publication Homo sapiens 2-[2-[(1S,2S)-2-[[1-(8-methylquinolin-2-yl)piperidine-4-carbonyl]amino]cyclopentyl]ethyl]benzoic acid
5.3.99.3 0.000001
-
 pH and temperature not specified in the publication Homo sapiens 4-chloro-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
5.3.99.3 0.000001
-
 pH and temperature not specified in the publication Homo sapiens 4-fluoro-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
5.3.99.3 0.000001
-
 pH and temperature not specified in the publication Homo sapiens 4-methyl-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
5.3.99.3 0.000002
-
 pH and temperature not specified in the publication Homo sapiens 2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
5.3.99.3 0.000002
-
 pH and temperature not specified in the publication Homo sapiens 2-[2-[(1S,2S)-2-([1-[5-(trifluoromethyl)pyridin-2-yl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
5.3.99.3 0.000002
-
 pH and temperature not specified in the publication Homo sapiens 4-chloro-2-[([(1S,2S)-2-[(1-phenylpiperidine-4-carbonyl)amino]cyclopentyl]methyl)amino]benzoic acid
5.3.99.3 0.000002
-
 pH and temperature not specified in the publication Homo sapiens 4-chloro-2-[[(1R,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]methoxy]benzoic acid
5.3.99.3 0.000003
-
 pH and temperature not specified in the publication Homo sapiens 1-[5-chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide
5.3.99.3 0.000004
-
 pH and temperature not specified in the publication Homo sapiens 4-chloro-2-([[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]methyl]amino)benzoic acid
5.3.99.3 0.000006
-
 pH and temperature not specified in the publication Homo sapiens 2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]pyridine-3-carboxylic acid
5.3.99.3 0.000007
-
 pH and temperature not specified in the publication Homo sapiens 3-[6-([1,1'-biphenyl]-4-yl)-1-[(4-chlorophenyl)methyl]-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
5.3.99.3 0.000016
-
 pH and temperature not specified in the publication Homo sapiens N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-1,1-dioxo-1,2-dihydro-1lambda~6~,2-benzothiazine-3-carboxamide
5.3.99.3 0.000043
-
 pH and temperature not specified in the publication Homo sapiens 4-chloro-2-([[(1S,2S)-2-(2,2-dimethylpropanamido)cyclopentyl]methyl]amino)benzoic acid
5.3.99.3 0.000241
-
 pH and temperature not specified in the publication Homo sapiens 2-chloro-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide