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Literature summary extracted from

  • Greiner, C.; Zettl, H.; Koeberle, A.; Pergola, C.; Northoff, H.; Schubert-Zsilavecz, M.; Werz, O.
    Identification of 2-mercaptohexanoic acids as dual inhibitors of 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 (2011), Bioorg. Med. Chem., 19, 3394-3401.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.3 (2E)-2-[4-[3-(2,3-dimethylphenoxy)propoxy]benzylidene]hexanoic acid 28.3% residual activity at 0.01 mM Homo sapiens
5.3.99.3 (2R)-2-([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
 Homo sapiens
5.3.99.3 (2S)-2-([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
 Homo sapiens
5.3.99.3 ([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)acetic acid 75.4% residual activity at 0.01 mM Homo sapiens
5.3.99.3 2(4-(3-biphenyloxypropoxy)phenylthio)hexanoic acid
-
 Homo sapiens
5.3.99.3 2-([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
 Homo sapiens
5.3.99.3 2-([4-[3-(2-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid 88.3% residual activity at 0.01 mM Homo sapiens
5.3.99.3 2-([4-[3-(2-methylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
 Homo sapiens
5.3.99.3 2-([4-[3-(3-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid 59.1% residual activity at 0.01 mM Homo sapiens
5.3.99.3 2-([4-[3-(3-methylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid 58% residual activity at 0.01 mM Homo sapiens
5.3.99.3 2-([4-[3-(4-chloro-2-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
 Homo sapiens
5.3.99.3 2-([4-[3-(4-methylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
 Homo sapiens
5.3.99.3 2-([4-[3-(5,6,7,8-tetrahydronaphthalen-1-yloxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
 Homo sapiens
5.3.99.3 2-([4-[3-(quinolin-6-yloxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
 Homo sapiens
5.3.99.3 2-[(4-[3-[2-(propan-2-yl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
-
 Homo sapiens
5.3.99.3 2-[(4-[3-[3-(propan-2-yl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
-
 Homo sapiens
5.3.99.3 2-[(4-[3-[3-(trifluoromethyl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
-
 Homo sapiens
5.3.99.3 2-[(4-[3-[4-chloro-3-(trifluoromethyl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
-
 Homo sapiens
5.3.99.3 2-[4-[3-(2,3-dimethylphenoxy)propoxy]benzyl]hexanoic acid
-
 Homo sapiens
5.3.99.3 2-[[4-(3-phenoxypropoxy)phenyl]sulfanyl]hexanoic acid 81.9% residual activity at 0.01 mM Homo sapiens
5.3.99.3 3-[4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]propanoic acid 83.9% residual activity at 0.01 mM Homo sapiens
5.3.99.3 ethyl 2-([4-[3-(5,6,7,8-tetrahydronaphthalen-1-yloxy)propoxy]phenyl]sulfanyl)hexanoate
-
 Homo sapiens
5.3.99.3 ethyl 2-([4-[3-(biphenyl-4-yloxy)propoxy]phenyl]sulfanyl)hexanoate
-
 Homo sapiens
5.3.99.3 ethyl 2-([4-[3-(quinolin-6-yloxy)propoxy]phenyl]sulfanyl)hexanoate 83.9% residual activity at 0.01 mM Homo sapiens
5.3.99.3 MK886
-
 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 E2 synthase-1
-
 Homo sapiens
5.3.99.3 mPGES-1
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
5.3.99.3 glutathione
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.3.99.3 0.0017
-
 in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 2-[(4-[3-[4-chloro-3-(trifluoromethyl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
5.3.99.3 0.002
-
 in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 2-[(4-[3-[3-(trifluoromethyl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
5.3.99.3 0.0022
-
 in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 2-([4-[3-(5,6,7,8-tetrahydronaphthalen-1-yloxy)propoxy]phenyl]sulfanyl)hexanoic acid
5.3.99.3 0.0022
-
 in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 2(4-(3-biphenyloxypropoxy)phenylthio)hexanoic acid
5.3.99.3 0.0024
-
 in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens MK886
5.3.99.3 0.0027
-
 in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 2-[(4-[3-[3-(propan-2-yl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
5.3.99.3 0.0029
-
 in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 2-([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
5.3.99.3 0.0041
-
 in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 2-[(4-[3-[2-(propan-2-yl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
5.3.99.3 0.0042
-
 in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens (2R)-2-([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
5.3.99.3 0.0046
-
 in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens (2S)-2-([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
5.3.99.3 0.0071
-
 in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 2-[4-[3-(2,3-dimethylphenoxy)propoxy]benzyl]hexanoic acid
5.3.99.3 0.0088
-
 in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 2-([4-[3-(2-methylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
5.3.99.3 0.0093
-
 in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 2-([4-[3-(4-methylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
5.3.99.3 0.0094
-
 in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 2-([4-[3-(4-chloro-2-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
5.3.99.3 0.01
-
 IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens ([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)acetic acid
5.3.99.3 0.01
-
 IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 3-[4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]propanoic acid
5.3.99.3 0.01
-
 IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens (2E)-2-[4-[3-(2,3-dimethylphenoxy)propoxy]benzylidene]hexanoic acid
5.3.99.3 0.01
-
 IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 2-[[4-(3-phenoxypropoxy)phenyl]sulfanyl]hexanoic acid
5.3.99.3 0.01
-
 IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 2-([4-[3-(3-methylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
5.3.99.3 0.01
-
 IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 2-([4-[3-(2-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
5.3.99.3 0.01
-
 IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 2-([4-[3-(3-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
5.3.99.3 0.01
-
 IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 2-([4-[3-(quinolin-6-yloxy)propoxy]phenyl]sulfanyl)hexanoic acid
5.3.99.3 0.01
-
 IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens ethyl 2-([4-[3-(quinolin-6-yloxy)propoxy]phenyl]sulfanyl)hexanoate

Expression

EC Number Organism Comment Expression
5.3.99.3 Homo sapiens interleukin-1beta (1 ng/ml) induces mPGES-1 expression up