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Literature summary for 5.3.99.3 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

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-549 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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
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
0.000008
-
pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluorophenyl)-4-[4-(phenylethynyl)phenyl]-1H-imidazole
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
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
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
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
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
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
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
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
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
0.00011
-
pH and temperature not specified in the publication Homo sapiens 4-(biphenyl-4-yl)-2-(2-chloro-6-fluorophenyl)-1H-imidazole
0.00015
-
pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluorophenyl)-4-[4-(2-phenylethyl)phenyl]-1H-imidazole
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
0.00018
-
pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluorophenyl)-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
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
0.00032
-
pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluorophenyl)-4-(4-phenoxyphenyl)-1H-imidazole
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
0.00057
-
pH and temperature not specified in the publication Homo sapiens 4-(4-benzylphenyl)-2-(2-chloro-6-fluorophenyl)-1H-imidazole
0.00066
-
pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluorophenyl)-4-(4-chlorophenyl)-1H-imidazole
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
0.001
-
pH and temperature not specified in the publication Homo sapiens 2-[4-(4-chlorophenyl)-1H-imidazol-2-yl]-3-fluorobenzonitrile
0.0014
-
pH and temperature not specified in the publication Homo sapiens 2-[4-(4-bromophenyl)-1H-imidazol-2-yl]benzonitrile
0.0014
-
pH and temperature not specified in the publication Homo sapiens 2-(2-chloro-6-fluorophenyl)-4-[4-(phenylsulfonyl)phenyl]-1H-imidazole
0.0025
-
pH and temperature not specified in the publication Homo sapiens 5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-ethynylpyridine
0.0037
-
pH and temperature not specified in the publication Homo sapiens 2-(4-bromophenyl)-5-(2-chloro-6-fluorophenyl)-1H-imidazole
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
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
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
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
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
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