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Literature summary extracted from

  • Borbely, G.; Szabadkai, I.; Horvath, Z.; Marko, P.; Varga, Z.; Breza, N.; Baska, F.; Vantus, T.; Huszar, M.; Geiszt, M.; Hunyady, L.; Buday, L.; Orfi, L.; Keri, G.
    Small-molecule inhibitors of NADPH oxidase 4 (2010), J. Med. Chem., 53, 6758-6762.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.6.3.1 (2Z)-2-(5-hydroxy-4,6-dimethyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N,N-di(prop-2-en-1-yl)hydrazinecarbothioamide complete inhibition at 0.01 mM Homo sapiens
1.6.3.1 (3Z)-3-(3,4-dihydroxybenzylidene)-5-nitro-1,3-dihydro-2H-indol-2-one complete inhibition at 0.01 mM Homo sapiens
1.6.3.1 (3Z)-3-[4-hydroxy-3,5-di(propan-2-yl)benzylidene]-1,3-dihydro-2H-indol-2-one complete inhibition at 0.01 mM Homo sapiens
1.6.3.1 2,3,8,9-tetrahydroxy-5-(2-hydroxy-5-nitrobenzyl)phenanthridin-6(5H)-one complete inhibition at 0.01 mM Homo sapiens
1.6.3.1 2,3,8,9-tetrahydroxy-5-(3-nitrobenzyl)phenanthridin-6(5H)-one complete inhibition at 0.01 mM Homo sapiens
1.6.3.1 2,3,8,9-tetrahydroxy-5-(4-nitrobenzyl)phenanthridin-6(5H)-one 93% inhibition at 0.01 mM Homo sapiens
1.6.3.1 2,3,8,9-tetrahydroxy-5-[2-(phenylsulfonyl)benzyl]phenanthridin-6(5H)-one 95% inhibition at 0.01 mM Homo sapiens
1.6.3.1 2-(1,3-benzothiazol-2-yl)-4-ethyl-5-(2-methoxyethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
 Homo sapiens
1.6.3.1 2-(3,4-dihydroxyphenyl)-3,7-dihydroxy-6-methoxy-4H-chromen-4-one complete inhibition at 0.01 mM Homo sapiens
1.6.3.1 2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4H-chromen-4-one complete inhibition at 0.01 mM Homo sapiens
1.6.3.1 2-(3,4-dihydroxyphenyl)-5-hydroxy-3,7-dimethoxy-4H-chromen-4-one 88% inhibition at 0.01 mM Homo sapiens
1.6.3.1 2-hydroxy-5-[(2-hydroxybenzyl)amino]benzoic acid 89% inhibition at 0.01 mM Homo sapiens
1.6.3.1 2-[(2,3,8,9-tetrahydroxy-6-oxophenanthridin-5(6H)-yl)methyl]benzonitrile 97% inhibition at 0.01 mM Homo sapiens
1.6.3.1 2-[(2E)-2-(3,4-dihydroxybenzylidene)hydrazinyl]-N-(3-nitrophenyl)-2-oxoacetamide 96% inhibition at 0.01 mM Homo sapiens
1.6.3.1 3,5,7-trihydroxy-2-(4-hydroxy-3-methylphenyl)-4H-chromen-4-one 94% inhibition at 0.01 mM Homo sapiens
1.6.3.1 3,5,7-trihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one complete inhibition at 0.01 mM Homo sapiens
1.6.3.1 3-(3,4-dihydroxycyclohexa-2,4-dien-1-yl)-2,7-dihydroxy-4H-chromen-4-one 86% inhibition at 0.01 mM Homo sapiens
1.6.3.1 3-(3-chlorophenyl)-N-[4-(piperidin-4-yl)phenyl]pyrazolo[1,5-a]pyrimidine-5-carboxamide
-
 Homo sapiens
1.6.3.1 5,7-dihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one complete inhibition at 0.01 mM Homo sapiens
1.6.3.1 5-[(2,5-dihydroxybenzyl)amino]-2-hydroxybenzoic acid 82% inhibition at 0.01 mM Homo sapiens
1.6.3.1 abruquinone C
-
 Homo sapiens
1.6.3.1 apocynin
-
 Homo sapiens
1.6.3.1 gliotoxin
-
 Homo sapiens
1.6.3.1 gomisin C
-
 Homo sapiens
1.6.3.1 honokiol
-
 Homo sapiens
1.6.3.1 magnolol
-
 Homo sapiens
1.6.3.1 methyl 2-hydroxy-5-[(2-hydroxybenzyl)amino]benzoate 91% inhibition at 0.01 mM Homo sapiens
1.6.3.1 N'1,N'2-bis[(E)-(2,3-dihydroxyphenyl)methylidene]ethanedihydrazide complete inhibition at 0.01 mM Homo sapiens
1.6.3.1 N'1,N'2-bis[(E)-(3,4-dihydroxyphenyl)methylidene]ethanedihydrazide complete inhibition at 0.01 mM Homo sapiens
1.6.3.1 N-(1-cyclohexylethyl)-4-phenylphthalazin-1-amine
-
 Homo sapiens
1.6.3.1 N-(3-aminophenyl)-N'-[1-(4-hydroxy-3-methoxyphenyl)ethyl]ethanediamide complete inhibition at 0.01 mM Homo sapiens
1.6.3.1 N-[(3Z)-3-(4-hydroxy-3-methoxybenzylidene)-2-oxo-2,3-dihydro-1H-indol-5-yl]acetamide complete inhibition at 0.01 mM Homo sapiens
1.6.3.1 N-[1-(3,4-dihydroxyphenyl)ethyl]-N'-(3-nitrophenyl)ethanediamide complete inhibition at 0.01 mM Homo sapiens
1.6.3.1 N4-(3-aminophenyl)[1]benzothieno[3,2-d]pyrimidine-4,8-diamine 98% inhibition at 0.01 mM Homo sapiens
1.6.3.1 N4-(4-aminophenyl)[1]benzothieno[3,2-d]pyrimidine-4,8-diamine complete inhibition at 0.01 mM Homo sapiens
1.6.3.1 neopterin
-
 Homo sapiens
1.6.3.1 norathyriol
-
 Homo sapiens
1.6.3.1 perhexilline
-
 Homo sapiens
1.6.3.1 prodigiosin
-
 Homo sapiens
1.6.3.1 quercetin 3-O-alpha-D-glucopyranoside complete inhibition at 0.01 mM Homo sapiens
1.6.3.1 S17834
-
 Homo sapiens
1.6.3.1 VAS2870
-
 Homo sapiens

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
1.6.3.1 65000
-
 SDS-PAGE Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.6.3.1 NADPH + H+ + O2 Homo sapiens
-
 NADP+ + H2O2
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.6.3.1 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.6.3.1 293-F FreeStyle cell
-
 Homo sapiens
-
1.6.3.1 HEK-293F cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.6.3.1 NADPH + H+ + O2
-
 Homo sapiens NADP+ + H2O2
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.6.3.1 NADPH oxidase 4
-
 Homo sapiens
1.6.3.1 Nox4
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.6.3.1 0.00017
-
 pH and temperature not specified in the publication Homo sapiens 2,3,8,9-tetrahydroxy-5-(2-hydroxy-5-nitrobenzyl)phenanthridin-6(5H)-one
1.6.3.1 0.00024
-
 pH and temperature not specified in the publication Homo sapiens N4-(3-aminophenyl)[1]benzothieno[3,2-d]pyrimidine-4,8-diamine
1.6.3.1 0.00026
-
 pH and temperature not specified in the publication Homo sapiens 2,3,8,9-tetrahydroxy-5-(3-nitrobenzyl)phenanthridin-6(5H)-one
1.6.3.1 0.00059
-
 pH and temperature not specified in the publication Homo sapiens 2-[(2,3,8,9-tetrahydroxy-6-oxophenanthridin-5(6H)-yl)methyl]benzonitrile
1.6.3.1 0.00063
-
 pH and temperature not specified in the publication Homo sapiens (3Z)-3-[4-hydroxy-3,5-di(propan-2-yl)benzylidene]-1,3-dihydro-2H-indol-2-one
1.6.3.1 0.00068
-
 pH and temperature not specified in the publication Homo sapiens 3,5,7-trihydroxy-2-(4-hydroxy-3-methylphenyl)-4H-chromen-4-one
1.6.3.1 0.00074
-
 pH and temperature not specified in the publication Homo sapiens 2-(3,4-dihydroxyphenyl)-3,7-dihydroxy-6-methoxy-4H-chromen-4-one
1.6.3.1 0.00079
-
 pH and temperature not specified in the publication Homo sapiens 3-(3,4-dihydroxycyclohexa-2,4-dien-1-yl)-2,7-dihydroxy-4H-chromen-4-one
1.6.3.1 0.00083
-
 pH and temperature not specified in the publication Homo sapiens quercetin 3-O-alpha-D-glucopyranoside
1.6.3.1 0.00085
-
 pH and temperature not specified in the publication Homo sapiens 2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4H-chromen-4-one
1.6.3.1 0.00091
-
 pH and temperature not specified in the publication Homo sapiens N'1,N'2-bis[(E)-(2,3-dihydroxyphenyl)methylidene]ethanedihydrazide
1.6.3.1 0.00096
-
 pH and temperature not specified in the publication Homo sapiens 2-hydroxy-5-[(2-hydroxybenzyl)amino]benzoic acid
1.6.3.1 0.001
-
 pH and temperature not specified in the publication Homo sapiens (2Z)-2-(5-hydroxy-4,6-dimethyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N,N-di(prop-2-en-1-yl)hydrazinecarbothioamide
1.6.3.1 0.00102
-
 pH and temperature not specified in the publication Homo sapiens 2-[(2E)-2-(3,4-dihydroxybenzylidene)hydrazinyl]-N-(3-nitrophenyl)-2-oxoacetamide
1.6.3.1 0.00102
-
 pH and temperature not specified in the publication Homo sapiens 2-(3,4-dihydroxyphenyl)-5-hydroxy-3,7-dimethoxy-4H-chromen-4-one
1.6.3.1 0.00107
-
 pH and temperature not specified in the publication Homo sapiens N4-(4-aminophenyl)[1]benzothieno[3,2-d]pyrimidine-4,8-diamine
1.6.3.1 0.00113
-
 pH and temperature not specified in the publication Homo sapiens 5,7-dihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one
1.6.3.1 0.00113
-
 pH and temperature not specified in the publication Homo sapiens (3Z)-3-(3,4-dihydroxybenzylidene)-5-nitro-1,3-dihydro-2H-indol-2-one
1.6.3.1 0.00116
-
 pH and temperature not specified in the publication Homo sapiens N'1,N'2-bis[(E)-(3,4-dihydroxyphenyl)methylidene]ethanedihydrazide
1.6.3.1 0.0012
-
 pH and temperature not specified in the publication Homo sapiens 3,5,7-trihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one
1.6.3.1 0.00127
-
 pH and temperature not specified in the publication Homo sapiens methyl 2-hydroxy-5-[(2-hydroxybenzyl)amino]benzoate
1.6.3.1 0.0013
-
 pH and temperature not specified in the publication Homo sapiens N-(3-aminophenyl)-N'-[1-(4-hydroxy-3-methoxyphenyl)ethyl]ethanediamide
1.6.3.1 0.00134
-
 pH and temperature not specified in the publication Homo sapiens 5-[(2,5-dihydroxybenzyl)amino]-2-hydroxybenzoic acid
1.6.3.1 0.0014
-
 pH and temperature not specified in the publication Homo sapiens N-[(3Z)-3-(4-hydroxy-3-methoxybenzylidene)-2-oxo-2,3-dihydro-1H-indol-5-yl]acetamide
1.6.3.1 0.00158
-
 pH and temperature not specified in the publication Homo sapiens 2,3,8,9-tetrahydroxy-5-(4-nitrobenzyl)phenanthridin-6(5H)-one
1.6.3.1 0.00158
-
 pH and temperature not specified in the publication Homo sapiens 2,3,8,9-tetrahydroxy-5-[2-(phenylsulfonyl)benzyl]phenanthridin-6(5H)-one
1.6.3.1 0.00164
-
 pH and temperature not specified in the publication Homo sapiens N-[1-(3,4-dihydroxyphenyl)ethyl]-N'-(3-nitrophenyl)ethanediamide