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Literature summary for 1.13.11.31 extracted from

  • Kenyon, V.; Rai, G.; Jadhav, A.; Schultz, L.; Armstrong, M.; Jameson, J.B.; Perry, S.; Joshi, N.; Bougie, J.M.; Leister, W.; Taylor-Fishwick, D.A.; Nadler, J.L.; Holinstat, M.; Simeonov, A.; Maloney, D.J.; Holman, T.R.
    Discovery of potent and selective inhibitors of human platelet-type 12- lipoxygenase (2011), J. Med. Chem., 54, 5485-5497.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 1.13.11.31

Inhibitors

Inhibitors Comment Organism Structure
N-([5-chloro-2-(dimethylamino)-8-hydroxyquinolin-7-yl](furan-2-yl)methyl)acetamide
-
 Homo sapiens
N-([5-chloro-8-hydroxy-2-(piperidin-1-yl)quinolin-7-yl](furan-2-yl)methyl)acetamide
-
 Homo sapiens
N-[(2,5-dichloro-8-hydroxyquinolin-7-yl)(furan-2-yl)methyl]acetamide
-
 Homo sapiens
N-[(4-chloro-1-hydroxynaphthalen-2-yl)(furan-2-yl)methyl]acetamide
-
 Homo sapiens
N-[(5-bromo-8-hydroxyquinolin-7-yl)(furan-2-yl)methyl]acetamide
-
 Homo sapiens
N-[(5-bromo-8-hydroxyquinolin-7-yl)(furan-2-yl)methyl]propanamide
-
 Homo sapiens
N-[(5-bromo-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]acetamide
-
 Homo sapiens
N-[(5-bromo-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]propanamide
-
 Homo sapiens
N-[(5-bromofuran-2-yl)(5-chloro-8-hydroxyquinolin-7-yl)methyl]propanamide
-
 Homo sapiens
N-[(5-chloro-8-hydroxy-1,2,3,4,4a,8a-hexahydroquinolin-7-yl)(furan-2-yl)methyl]propanamide
-
 Homo sapiens
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-fluorophenyl)methyl]propanamide
-
 Homo sapiens
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]propanamide
-
 Homo sapiens
N-[(5-chloro-8-hydroxyquinolin-7-yl)(5-methylthiophen-2-yl)methyl]propanamide
-
 Homo sapiens
N-[(5-chloro-8-hydroxyquinolin-7-yl)(cyclopropyl)methyl]acetamide
-
 Homo sapiens
N-[(5-chloro-8-hydroxyquinolin-7-yl)(cyclopropyl)methyl]propanamide
-
 Homo sapiens
N-[(5-chloro-8-hydroxyquinolin-7-yl)(furan-2-yl)methyl]-4-methylbenzamide
-
 Homo sapiens
N-[(5-chloro-8-hydroxyquinolin-7-yl)(furan-2-yl)methyl]acetamide
-
 Homo sapiens
N-[(5-chloro-8-hydroxyquinolin-7-yl)(furan-2-yl)methyl]benzamide
-
 Homo sapiens
N-[(5-chloro-8-hydroxyquinolin-7-yl)(furan-2-yl)methyl]propanamide
-
 Homo sapiens
N-[(5-chloro-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]acetamide
-
 Homo sapiens
N-[(5-chloro-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]propanamide
-
 Homo sapiens
N-[(5-chloro-8-hydroxyquinolin-7-yl)methyl]acetamide
-
 Homo sapiens
N-[(5-chloro-8-methoxyquinolin-7-yl)(furan-2-yl)methyl]propanamide
-
 Homo sapiens
N-[(5-fluoro-8-hydroxyquinolin-7-yl)(furan-2-yl)methyl]acetamide
-
 Homo sapiens
N-[(5-fluoro-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]acetamide
-
 Homo sapiens
N-[(8-hydroxy-5-nitroquinolin-7-yl)(thiophen-2-yl)methyl]propanamide
-
 Homo sapiens
N-[(8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]propanamide
-
 Homo sapiens
N-[(R)-(5-bromo-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]acetamide
-
 Homo sapiens
N-[(R)-(5-bromo-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]propanamide
-
 Homo sapiens
N-[(S)-(5-bromo-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]acetamide
-
 Homo sapiens
N-[(S)-(5-bromo-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]propanamide
-
 Homo sapiens
N-[1-(5-chloro-8-hydroxyquinolin-7-yl)-2-methylpropyl]acetamide
-
 Homo sapiens
N-[1-(5-chloro-8-hydroxyquinolin-7-yl)-2-methylpropyl]propanamide
-
 Homo sapiens
N-[1-(5-chloro-8-hydroxyquinolin-7-yl)ethyl]acetamide
-
 Homo sapiens
N-[1-(5-chloro-8-hydroxyquinolin-7-yl)ethyl]propanamide
-
 Homo sapiens
N-[1-(5-fluoro-8-hydroxyquinolin-7-yl)ethyl]acetamide
-
 Homo sapiens
N-[furan-2-yl(8-hydroxy-5-nitroquinolin-7-yl)methyl]propanamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
arachidonic acid + O2
-
 Homo sapiens (5Z,8Z,10E,14Z)-(12S)-12-hydroperoxyicosa-5,8,10,14-tetraenoate
-
 ?

Synonyms

Synonyms Comment Organism
12-LOX
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
23
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00038
-
 pH 8.0, 23°C Homo sapiens N-[(S)-(5-bromo-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]propanamide
0.00043
-
 pH 8.0, 23°C Homo sapiens N-[(S)-(5-bromo-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]acetamide
0.0008
-
 pH 8.0, 23°C Homo sapiens N-[(8-hydroxy-5-nitroquinolin-7-yl)(thiophen-2-yl)methyl]propanamide
0.001
-
 pH 8.0, 23°C Homo sapiens N-[(5-bromo-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]acetamide
0.001
-
 pH 8.0, 23°C Homo sapiens N-[(5-chloro-8-hydroxyquinolin-7-yl)(furan-2-yl)methyl]propanamide
0.001
-
 pH 8.0, 23°C Homo sapiens N-[(5-chloro-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]acetamide
0.001
-
 pH 8.0, 23°C Homo sapiens N-[(5-chloro-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]propanamide
0.0012
-
 pH 8.0, 23°C Homo sapiens N-[1-(5-chloro-8-hydroxyquinolin-7-yl)-2-methylpropyl]propanamide
0.0012
-
 pH 8.0, 23°C Homo sapiens N-[furan-2-yl(8-hydroxy-5-nitroquinolin-7-yl)methyl]propanamide
0.0016
-
 pH 8.0, 23°C Homo sapiens N-[(5-chloro-8-hydroxyquinolin-7-yl)(cyclopropyl)methyl]propanamide
0.002
-
 pH 8.0, 23°C Homo sapiens N-[(5-bromo-8-hydroxyquinolin-7-yl)(furan-2-yl)methyl]acetamide
0.002
-
 pH 8.0, 23°C Homo sapiens N-[(5-bromo-8-hydroxyquinolin-7-yl)(furan-2-yl)methyl]propanamide
0.002
-
 pH 8.0, 23°C Homo sapiens N-[(5-fluoro-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]acetamide
0.0026
-
 pH 8.0, 23°C Homo sapiens N-[1-(5-chloro-8-hydroxyquinolin-7-yl)-2-methylpropyl]acetamide
0.003
-
 pH 8.0, 23°C Homo sapiens N-[(5-chloro-8-hydroxy-1,2,3,4,4a,8a-hexahydroquinolin-7-yl)(furan-2-yl)methyl]propanamide
0.003
-
 pH 8.0, 23°C Homo sapiens N-[(5-chloro-8-hydroxyquinolin-7-yl)(cyclopropyl)methyl]acetamide
0.003
-
 pH 8.0, 23°C Homo sapiens N-[(5-chloro-8-hydroxyquinolin-7-yl)(furan-2-yl)methyl]acetamide
0.0034
-
 pH 8.0, 23°C Homo sapiens N-[(8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]propanamide
0.0035
-
 pH 8.0, 23°C Homo sapiens N-[(5-chloro-8-hydroxyquinolin-7-yl)(5-methylthiophen-2-yl)methyl]propanamide
0.005
-
 pH 8.0, 23°C Homo sapiens N-[(5-fluoro-8-hydroxyquinolin-7-yl)(furan-2-yl)methyl]acetamide
0.014
-
 pH 8.0, 23°C Homo sapiens N-[(5-bromo-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]propanamide
0.025
-
 pH 8.0, 23°C Homo sapiens N-[(R)-(5-bromo-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]acetamide
0.025
-
 pH 8.0, 23°C Homo sapiens N-[(R)-(5-bromo-8-hydroxyquinolin-7-yl)(thiophen-2-yl)methyl]propanamide
0.025
-
 value above, pH 8.0, 23°C Homo sapiens N-[(5-chloro-8-hydroxyquinolin-7-yl)(furan-2-yl)methyl]-4-methylbenzamide
0.025
-
 value above, pH 8.0, 23°C Homo sapiens N-[(5-chloro-8-hydroxyquinolin-7-yl)(furan-2-yl)methyl]benzamide
0.05
-
 value above, pH 8.0, 23°C Homo sapiens N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-fluorophenyl)methyl]propanamide
0.05
-
 value above, pH 8.0, 23°C Homo sapiens N-[1-(5-chloro-8-hydroxyquinolin-7-yl)ethyl]propanamide
0.075
-
 value above, pH 8.0, 23°C Homo sapiens N-([5-chloro-2-(dimethylamino)-8-hydroxyquinolin-7-yl](furan-2-yl)methyl)acetamide
0.075
-
 value above, pH 8.0, 23°C Homo sapiens N-([5-chloro-8-hydroxy-2-(piperidin-1-yl)quinolin-7-yl](furan-2-yl)methyl)acetamide
0.075
-
 value above, pH 8.0, 23°C Homo sapiens N-[(2,5-dichloro-8-hydroxyquinolin-7-yl)(furan-2-yl)methyl]acetamide
0.075
-
 value above, pH 8.0, 23°C Homo sapiens N-[(4-chloro-1-hydroxynaphthalen-2-yl)(furan-2-yl)methyl]acetamide
0.075
-
 value above, pH 8.0, 23°C Homo sapiens N-[(5-bromofuran-2-yl)(5-chloro-8-hydroxyquinolin-7-yl)methyl]propanamide
0.075
-
 value above, pH 8.0, 23°C Homo sapiens N-[(5-chloro-8-methoxyquinolin-7-yl)(furan-2-yl)methyl]propanamide
0.075
-
 value above, pH 8.0, 23°C Homo sapiens N-[1-(5-fluoro-8-hydroxyquinolin-7-yl)ethyl]acetamide
0.15
-
 value above, pH 8.0, 23°C Homo sapiens N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]propanamide
0.15
-
 value above, pH 8.0, 23°C Homo sapiens N-[(5-chloro-8-hydroxyquinolin-7-yl)methyl]acetamide
0.15
-
 value above, pH 8.0, 23°C Homo sapiens N-[1-(5-chloro-8-hydroxyquinolin-7-yl)ethyl]acetamide