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Literature summary for 1.13.11.34 extracted from

  • Shang, E.; Liu, Y.; Wu, Y.; Zhu, W
    ; He, C.; Lai, L. Development of 3,5-dinitrobenzoate-based 5-lipoxygenase inhibitors (2014), Bioorg. Med. Chem., 22, 2396-2402 .
    View publication on PubMed

Application

Application Comment Organism
drug development human 5-lipoxygenase is a well-validated target for anti-inflammatory therapy. Development of 5-LOX inhibitors with higher activities is highly required Homo sapiens
pharmacology human 5-lipoxygenase is a well-validated target for anti-inflammatory therapy. Development of 5-LOX inhibitors with higher activities is highly required Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2,3-dichlorophenyl 3,5-dinitrobenzoate
-
Homo sapiens
3-((naphthalene-1-yloxy)carbonyl)benzoic acid
-
Homo sapiens
3-(benzyloxycarbonyl)benzoic acid
-
Homo sapiens
3-(naphhthalen-1-ylcarbmoyl)benzoic acid
-
Homo sapiens
3-(phenylcarbamoyl)benzoic acid
-
Homo sapiens
3-propylphenyl 3,5-dinitrobenzoate
-
Homo sapiens
3-tolyl 3,5-dinitrobenzoate
-
Homo sapiens
biphenyl-3-yl 3,5-dinitrobenzoate
-
Homo sapiens
biphenyl-4-yl 3,5-dinitrobenzoate
-
Homo sapiens
additional information development of 3,5-dinitrobenzoate-based 5-lipoxygenase inhibitors, structure-activity relationship study, overview Homo sapiens
N-(3,4-dimethoxyphenyl)-3,5-dinitrobenzamide
-
Homo sapiens
N-(3-bromobenzyl)-3,5-dinitrobenzamide
-
Homo sapiens
N-(3-bromophenyl)-3,5-dinitrobenzamide
-
Homo sapiens
N-(3-chlorophenyl)-3,5-dinitrobenzamide
-
Homo sapiens
N-(4-methoxyphenyl)-3,5-dinitrobenzamide
-
Homo sapiens
N-(biphenyl-3-yl)-3,5-dinitrobenzamide
-
Homo sapiens
N-(naphthalene-1-yl)-3,5-dinitrobenzamide
-
Homo sapiens
N-3-tolyl-3,5-dinitrobenzamide
-
Homo sapiens
N-phenyl-3,5-dinitrobenzamide
-
Homo sapiens
naphthalen-1-yl 3,5-dinitrobenzoate JMC-4, identified from virtual inhibitor screening Homo sapiens
naphthalene-1-yl 3-nitrobenzoate
-
Homo sapiens
phenyl 3,5-dinitrobenzoate
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
arachidonate + O2 Homo sapiens
-
(5S,6S,7E,9E,11Z,14Z)-5,6-epoxyicosa-7,9,11,14-tetraenoate + H2O
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P09917
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
arachidonate + O2
-
Homo sapiens (5S,6S,7E,9E,11Z,14Z)-5,6-epoxyicosa-7,9,11,14-tetraenoate + H2O
-
?

Synonyms

Synonyms Comment Organism
5-lipoxygenase
-
Homo sapiens
5-LOX
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0005
-
pH 7.4, 37°C Homo sapiens 3-tolyl 3,5-dinitrobenzoate
0.0027
-
pH 7.4, 37°C Homo sapiens N-(4-methoxyphenyl)-3,5-dinitrobenzamide
0.0065
-
pH 7.4, 37°C Homo sapiens 3-propylphenyl 3,5-dinitrobenzoate
0.0144
-
pH 7.4, 37°C Homo sapiens N-(3-bromobenzyl)-3,5-dinitrobenzamide
0.0152
-
pH 7.4, 37°C Homo sapiens N-phenyl-3,5-dinitrobenzamide
0.0158
-
pH 7.4, 37°C Homo sapiens phenyl 3,5-dinitrobenzoate
0.0246
-
pH 7.4, 37°C Homo sapiens naphthalene-1-yl 3-nitrobenzoate
0.038
-
pH 7.4, 37°C Homo sapiens biphenyl-3-yl 3,5-dinitrobenzoate
0.05
-
pH 7.4, 37°C Homo sapiens 2,3-dichlorophenyl 3,5-dinitrobenzoate
0.05
-
pH 7.4, 37°C Homo sapiens biphenyl-4-yl 3,5-dinitrobenzoate
0.05
-
pH 7.4, 37°C Homo sapiens N-(naphthalene-1-yl)-3,5-dinitrobenzamide
0.05
-
pH 7.4, 37°C Homo sapiens N-3-tolyl-3,5-dinitrobenzamide
0.05
-
pH 7.4, 37°C Homo sapiens N-(3-chlorophenyl)-3,5-dinitrobenzamide
0.05
-
pH 7.4, 37°C Homo sapiens N-(3-bromophenyl)-3,5-dinitrobenzamide
0.05
-
pH 7.4, 37°C Homo sapiens N-(3,4-dimethoxyphenyl)-3,5-dinitrobenzamide
0.05
-
pH 7.4, 37°C Homo sapiens N-(biphenyl-3-yl)-3,5-dinitrobenzamide
0.05
-
pH 7.4, 37°C Homo sapiens 3-(benzyloxycarbonyl)benzoic acid
0.05
-
pH 7.4, 37°C Homo sapiens 3-((naphthalene-1-yloxy)carbonyl)benzoic acid
0.05
-
pH 7.4, 37°C Homo sapiens 3-(naphhthalen-1-ylcarbmoyl)benzoic acid
0.05
-
pH 7.4, 37°C Homo sapiens 3-(phenylcarbamoyl)benzoic acid

General Information

General Information Comment Organism
additional information modeling of the active conformation of human 5-LOX, overview Homo sapiens