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Literature summary for 5.3.99.3 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
Search for more literature for 5.3.99.3

Inhibitors

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

Cofactor

Cofactor Comment Organism Structure
glutathione
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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
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
0.0022
-
 in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens 2(4-(3-biphenyloxypropoxy)phenylthio)hexanoic acid
0.0024
-
 in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C Homo sapiens MK886
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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

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