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Literature summary extracted from

  • Wu, T.Y.; Juteau, H.; Ducharme, Y.; Friesen, R.W.; Guiral, S.; Dufresne, L.; Poirier, H.; Salem, M.; Riendeau, D.; Mancini, J.; Brideau, C.
    Biarylimidazoles as inhibitors of microsomal prostaglandin E2 synthase-1 (2010), Bioorg. Med. Chem. Lett., 20, 6978-6982.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.3 2-(2-chloro-6-fluorophenyl)-4-(4-chlorophenyl)-1H-imidazole
-
 Homo sapiens
5.3.99.3 2-(2-chloro-6-fluorophenyl)-4-(4-phenoxyphenyl)-1H-imidazole
-
 Homo sapiens
5.3.99.3 2-(2-chloro-6-fluorophenyl)-4-[4-(2-phenylethyl)phenyl]-1H-imidazole
-
 Homo sapiens
5.3.99.3 2-(2-chloro-6-fluorophenyl)-4-[4-(phenylethynyl)phenyl]-1H-imidazole
-
 Homo sapiens
5.3.99.3 2-(2-chloro-6-fluorophenyl)-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
-
 Homo sapiens
5.3.99.3 2-(2-chloro-6-fluorophenyl)-4-[4-(phenylsulfonyl)phenyl]-1H-imidazole
-
 Homo sapiens
5.3.99.3 2-(2-chloro-6-fluorophenyl)-4-[4-[(E)-2-phenylethenyl]phenyl]-1H-imidazole
-
 Homo sapiens
5.3.99.3 2-(4-bromophenyl)-5-(2-chloro-6-fluorophenyl)-1H-imidazole
-
 Homo sapiens
5.3.99.3 2-[2-(2-chloro-6-fluorophenyl)-4-[6-(phenylethynyl)pyridin-3-yl]-1H-imidazol-5-yl]ethanol
-
 Homo sapiens
5.3.99.3 2-[4-(4-bromophenyl)-1H-imidazol-2-yl]benzonitrile
-
 Homo sapiens
5.3.99.3 2-[4-(4-chlorophenyl)-1H-imidazol-2-yl]-3-fluorobenzonitrile
-
 Homo sapiens
5.3.99.3 2-[4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)phenyl]propan-2-ol
-
 Homo sapiens
5.3.99.3 3-(4-bromophenyl)-5-(2-chloro-6-fluorophenyl)-1H-1,2,4-triazole
-
 Homo sapiens
5.3.99.3 4-(4-benzylphenyl)-2-(2-chloro-6-fluorophenyl)-1H-imidazole
-
 Homo sapiens
5.3.99.3 4-(biphenyl-4-yl)-2-(2-chloro-6-fluorophenyl)-1H-imidazole
-
 Homo sapiens
5.3.99.3 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzamide
-
 Homo sapiens
5.3.99.3 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzoic acid
-
 Homo sapiens
5.3.99.3 5-(4-bromophenyl)-3-(2-chloro-6-fluorophenyl)-1,2,4-oxadiazole
-
 Homo sapiens
5.3.99.3 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(1,3-thiazol-2-ylethynyl)pyridine
-
 Homo sapiens
5.3.99.3 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclohex-1-en-1-ylethynyl)pyridine
-
 Homo sapiens
5.3.99.3 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclohexylethynyl)pyridine
-
 Homo sapiens
5.3.99.3 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclopropylethynyl)pyridine
-
 Homo sapiens
5.3.99.3 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
-
 Homo sapiens
5.3.99.3 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(pyridin-3-ylethynyl)pyridine
-
 Homo sapiens
5.3.99.3 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-ethynylpyridine
-
 Homo sapiens
5.3.99.3 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(2-chlorophenyl)ethynyl]pyridine
-
 Homo sapiens
5.3.99.3 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(3-chlorophenyl)ethynyl]pyridine
-
 Homo sapiens
5.3.99.3 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(4-chlorophenyl)ethynyl]pyridine
-
 Homo sapiens
5.3.99.3 5-[2-(2-chloro-6-fluorophenyl)-5-methyl-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
-
 Homo sapiens
5.3.99.3 5-[5-(2-chloro-6-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-(phenylethynyl)pyridine
-
 Homo sapiens
5.3.99.3 5-[5-bromo-2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
-
 Homo sapiens
5.3.99.3 5-[5-chloro-2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
-
 Homo sapiens
5.3.99.3 aminomethyl 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzenesulfinate
-
 Homo sapiens
5.3.99.3 methyl 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzenesulfinate
-
 Homo sapiens

Organism

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

Source Tissue

EC Number Source Tissue Comment Organism Textmining
5.3.99.3 A-549 cell
-
 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 0.000001
-
 pH and temperature not specified in the publication Homo sapiens 5-[5-bromo-2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
5.3.99.3 0.000004
-
 pH and temperature not specified in the publication Homo sapiens 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(3-chlorophenyl)ethynyl]pyridine
5.3.99.3 0.000005
-
 pH and temperature not specified in the publication Homo sapiens 5-[5-chloro-2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
5.3.99.3 0.000008
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluorophenyl)-4-[4-(phenylethynyl)phenyl]-1H-imidazole
5.3.99.3 0.000009
-
 pH and temperature not specified in the publication Homo sapiens 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(2-chlorophenyl)ethynyl]pyridine
5.3.99.3 0.000013
-
 pH and temperature not specified in the publication Homo sapiens 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclohex-1-en-1-ylethynyl)pyridine
5.3.99.3 0.000016
-
 pH and temperature not specified in the publication Homo sapiens 5-[5-(2-chloro-6-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-(phenylethynyl)pyridine
5.3.99.3 0.00002
-
 pH and temperature not specified in the publication Homo sapiens 5-[2-(2-chloro-6-fluorophenyl)-5-methyl-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
5.3.99.3 0.000023
-
 pH and temperature not specified in the publication Homo sapiens 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
5.3.99.3 0.000031
-
 pH and temperature not specified in the publication Homo sapiens 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(4-chlorophenyl)ethynyl]pyridine
5.3.99.3 0.000033
-
 pH and temperature not specified in the publication Homo sapiens 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclohexylethynyl)pyridine
5.3.99.3 0.000035
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluorophenyl)-4-[4-[(E)-2-phenylethenyl]phenyl]-1H-imidazole
5.3.99.3 0.00011
-
 pH and temperature not specified in the publication Homo sapiens 3-(4-bromophenyl)-5-(2-chloro-6-fluorophenyl)-1H-1,2,4-triazole
5.3.99.3 0.00011
-
 pH and temperature not specified in the publication Homo sapiens 4-(biphenyl-4-yl)-2-(2-chloro-6-fluorophenyl)-1H-imidazole
5.3.99.3 0.00015
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluorophenyl)-4-[4-(2-phenylethyl)phenyl]-1H-imidazole
5.3.99.3 0.00017
-
 pH and temperature not specified in the publication Homo sapiens 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclopropylethynyl)pyridine
5.3.99.3 0.00018
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluorophenyl)-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
5.3.99.3 0.00018
-
 pH and temperature not specified in the publication Homo sapiens 2-[2-(2-chloro-6-fluorophenyl)-4-[6-(phenylethynyl)pyridin-3-yl]-1H-imidazol-5-yl]ethanol
5.3.99.3 0.00032
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluorophenyl)-4-(4-phenoxyphenyl)-1H-imidazole
5.3.99.3 0.00048
-
 pH and temperature not specified in the publication Homo sapiens 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(pyridin-3-ylethynyl)pyridine
5.3.99.3 0.00057
-
 pH and temperature not specified in the publication Homo sapiens 4-(4-benzylphenyl)-2-(2-chloro-6-fluorophenyl)-1H-imidazole
5.3.99.3 0.00066
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluorophenyl)-4-(4-chlorophenyl)-1H-imidazole
5.3.99.3 0.00094
-
 pH and temperature not specified in the publication Homo sapiens 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(1,3-thiazol-2-ylethynyl)pyridine
5.3.99.3 0.001
-
 pH and temperature not specified in the publication Homo sapiens 2-[4-(4-chlorophenyl)-1H-imidazol-2-yl]-3-fluorobenzonitrile
5.3.99.3 0.0014
-
 pH and temperature not specified in the publication Homo sapiens 2-[4-(4-bromophenyl)-1H-imidazol-2-yl]benzonitrile
5.3.99.3 0.0014
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluorophenyl)-4-[4-(phenylsulfonyl)phenyl]-1H-imidazole
5.3.99.3 0.0025
-
 pH and temperature not specified in the publication Homo sapiens 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-ethynylpyridine
5.3.99.3 0.0037
-
 pH and temperature not specified in the publication Homo sapiens 2-(4-bromophenyl)-5-(2-chloro-6-fluorophenyl)-1H-imidazole
5.3.99.3 0.005
-
 IC50 above 0.005 mM, pH and temperature not specified in the publication Homo sapiens 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzoic acid
5.3.99.3 0.005
-
 IC50 above 0.005 mM, pH and temperature not specified in the publication Homo sapiens 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzamide
5.3.99.3 0.005
-
 IC50 above 0.005 mM, pH and temperature not specified in the publication Homo sapiens methyl 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzenesulfinate
5.3.99.3 0.005
-
 IC50 above 0.005 mM, pH and temperature not specified in the publication Homo sapiens aminomethyl 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzenesulfinate
5.3.99.3 0.005
-
 IC50 above 0.005 mM, pH and temperature not specified in the publication Homo sapiens 2-[4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)phenyl]propan-2-ol
5.3.99.3 0.03
-
 IC50 above 0.03 mM, pH and temperature not specified in the publication Homo sapiens 5-(4-bromophenyl)-3-(2-chloro-6-fluorophenyl)-1,2,4-oxadiazole