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Literature summary extracted from

  • Schiffler, M.A.; Antonysamy, S.; Bhattachar, S.N.; Campanale, K.M.; Chandrasekhar, S.; Condon, B.; Desai, P.V.; Fisher, M.J.; Groshong, C.; Harvey, A.; Hickey, M.J.; Hughes, N.E.; Jones, S.A.; Kim, E.J.; Kuklish, S.L.; Luz, J.G.; Norman, B.H.; Rathmell, R.E.; Rizzo, J.R.; Seng, T.W.; Thibodeaux, S.J.; Woods, T.A.
    Discovery and characterization of 2-acylaminoimidazole microsomal prostaglandin E synthase-1 inhibitors (2016), J. Med. Chem., 59, 194-205 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.3 2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile fludrocortisone Homo sapiens
5.3.99.3 2-(difluoromethyl)-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
-
Homo sapiens
5.3.99.3 2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
-
Homo sapiens
5.3.99.3 2-(difluoromethyl)-N-(1H-imidazol-2-yl)-5-([[(2R)-2-methylbutanoyl]amino]methyl)benzamide
-
Homo sapiens
5.3.99.3 2-(difluoromethyl)-N-(1H-imidazol-2-yl)-5-[(2-methylpropanamido)methyl]benzamide
-
Homo sapiens
5.3.99.3 2-(difluoromethyl)-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]-5-(propanamidomethyl)pyridine-3-carboxamide
-
Homo sapiens
5.3.99.3 2-bromo-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
-
Homo sapiens
5.3.99.3 2-chloro-4-fluoro-N-(1H-imidazol-2-yl)-5-[(2-methylpropanamido)methyl]benzamide CEP-32496 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-chloro-5-[(3,3-dimethylbutanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
-
Homo sapiens
5.3.99.3 2-chloro-N-(1H-imidazol-2-yl)-4-methyl-5-[(2-methylpropanamido)methyl]benzamide
-
Homo sapiens
5.3.99.3 2-chloro-N-(1H-imidazol-2-yl)-5-[(2-methylpropanamido)methyl]benzamide
-
Homo sapiens
5.3.99.3 5-(acetamidomethyl)-2-(difluoromethyl)-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
-
Homo sapiens
5.3.99.3 5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)-2-(trifluoromethyl)benzamide
-
Homo sapiens
5.3.99.3 5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)-2-methylbenzamide
-
Homo sapiens
5.3.99.3 N-[5-(4-chlorophenyl)-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]benzamide
-
Homo sapiens
5.3.99.3 N-[5-(4-chlorophenyl)-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]pyridine-3-carboxamide
-
Homo sapiens
5.3.99.3 N-[5-(4-chlorophenyl)-4-methyl-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]pyridine-3-carboxamide
-
Homo sapiens
5.3.99.3 sodium 3-[1-[(4-chlorophenyl)methyl]-5-(2-fluoro[1,1'-biphenyl]-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoate
-
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
-
-
-

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 0.0000009
-
at pH 7.0 and 25°C Homo sapiens 2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
5.3.99.3 0.000003
-
at pH 7.0 and 25°C Homo sapiens N-[5-(4-chlorophenyl)-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]benzamide
5.3.99.3 0.000003
-
at pH 7.0 and 25°C Homo sapiens N-[5-(4-chlorophenyl)-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]pyridine-3-carboxamide
5.3.99.3 0.000003
-
at pH 7.0 and 25°C Homo sapiens N-[5-(4-chlorophenyl)-4-methyl-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]pyridine-3-carboxamide
5.3.99.3 0.0000053
-
at pH 7.0 and 25°C Homo sapiens 2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
5.3.99.3 0.0000103
-
at pH 7.0 and 25°C Homo sapiens 2-(difluoromethyl)-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]-5-(propanamidomethyl)pyridine-3-carboxamide
5.3.99.3 0.0000195
-
at pH 7.0 and 25°C Homo sapiens sodium 3-[1-[(4-chlorophenyl)methyl]-5-(2-fluoro[1,1'-biphenyl]-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoate
5.3.99.3 0.000074
-
at pH 7.0 and 25°C Homo sapiens 5-(acetamidomethyl)-2-(difluoromethyl)-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
5.3.99.3 0.000198
-
at pH 7.0 and 25°C Homo sapiens 2-bromo-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
5.3.99.3 0.000241
-
at pH 7.0 and 25°C Homo sapiens 2-chloro-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
5.3.99.3 0.000385
-
at pH 7.0 and 25°C Homo sapiens 2-chloro-5-[(3,3-dimethylbutanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
5.3.99.3 0.000676
-
at pH 7.0 and 25°C Homo sapiens 2-(difluoromethyl)-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
5.3.99.3 0.000885
-
at pH 7.0 and 25°C Homo sapiens 2-chloro-N-(1H-imidazol-2-yl)-5-[(2-methylpropanamido)methyl]benzamide
5.3.99.3 0.00108
-
at pH 7.0 and 25°C Homo sapiens 5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)-2-(trifluoromethyl)benzamide
5.3.99.3 0.00112
-
at pH 7.0 and 25°C Homo sapiens 2-(difluoromethyl)-N-(1H-imidazol-2-yl)-5-([[(2R)-2-methylbutanoyl]amino]methyl)benzamide
5.3.99.3 0.00232
-
at pH 7.0 and 25°C Homo sapiens 2-chloro-N-(1H-imidazol-2-yl)-4-methyl-5-[(2-methylpropanamido)methyl]benzamide
5.3.99.3 0.00246
-
at pH 7.0 and 25°C Homo sapiens 2-(difluoromethyl)-N-(1H-imidazol-2-yl)-5-[(2-methylpropanamido)methyl]benzamide
5.3.99.3 0.00311
-
at pH 7.0 and 25°C Homo sapiens 5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)-2-methylbenzamide
5.3.99.3 0.00367
-
at pH 7.0 and 25°C Homo sapiens 2-chloro-4-fluoro-N-(1H-imidazol-2-yl)-5-[(2-methylpropanamido)methyl]benzamide