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Literature summary for 1.10.5.1 extracted from

  • Mailliet, F.; Ferry, G.; Vella, F.; Berger, S.; Coge, F.; et.al.
    Characterization of the melatoninergic MT3 binding site on the NRH:quinone oxidoreductase 2 enzyme (2005), Biochem. Pharmacol., 71, 74-88.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-(2-methoxy-6H-pyrido[2',3':4,5]pyrrolo[2,1-a]isoindol-11-yl)ethylamine IC50: 0.00087 mM Homo sapiens
2-iodo-5-methoxycarbonylamino-N-acetyltryptamine
-
Homo sapiens
2-iodo-melatonin IC50: 0.016 mM Homo sapiens
5-methoxy-carbonylamino-N-acetyltryptamine IC50: 0.295 mM Homo sapiens
dicoumarol IC50: 0.59 mM Homo sapiens
Melatonin IC50: 0.13 mM Homo sapiens
methyl-1-(2-acetamidoethyl)-7-naphthylcarbamate IC50: 0.015 mM Homo sapiens
N-acetylserotonin IC50: 0.099 mM Homo sapiens
N-[2-(2-iodo-5-methoxy-1-methyl-4-nitroindol-3-yl)ethyl]acetamide inhibits enzymatic mechanism of the enzyme through the MT3 binding site, IC50: 0.0003 mM Homo sapiens
N-[2-(2-methoxy-6H-dipyrido[2,3-a:3,2-e]pyrrolizin-11-yl)ethyl]-2-furamide IC50: 14 nM Homo sapiens
N-[2-(2-methoxy-6H-pyrido[2',3':4,5]pyrrolo[2,1-a]isoindol-11-yl)ethyl]2-furamide IC50: 0.0002 mM Homo sapiens
N-[2-(5-methoxy-4-nitro-1H-indol-3-yl)ethyl]acetamide IC50: 0.0015 mM Homo sapiens
N-[2-(5-methoxy-7-nitro-1H-indol-3-yl)ethyl]acetamide IC50: 0.044 mM Homo sapiens
N-[2-(7-methylaminosulfonyl-1-naphthyl)ethyl]acetamide IC50: 0.038 mM Homo sapiens
N-[2-(8-methoxy-3,4-dihydro-2H-pyrido[2',3':4,5]pyrrolo[2,1-b][1,3]oxazin-10-yl)ethyl]-2-furamide IC50: 0.005 mM Homo sapiens
N1-[2-(2-methoxy-6H-pyrido[2',3':4,5]pyrrolo[2,1-a]isoindol-11-yl)ethyl]-acetamide IC50: 0.0019 mM Homo sapiens
S28128 IC50: 0.00091 mM Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0067
-
menadione pH 8.5, 25°C, fluorescence assay Homo sapiens
0.017
-
menadione pH 8.5, HPLC approach Homo sapiens
0.02
-
dihydrobenzylnicotinamide pH 8.5, 25°C, fluorescence assay Homo sapiens
0.04
-
dihydrobenzylnicotinamide pH 8.5, HPLC approach Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
stably expressed in CHO cells
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
dihydrobenzylnicotinamide + menadione
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
QR2
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00003
-
N-[2-(2-methoxy-6H-dipyrido[2,3-a:3,2-e]pyrrolizin-11-yl)ethyl]-2-furamide reduced form hQR2-FADH2 Homo sapiens
0.00004
-
N-[2-(2-methoxy-6H-dipyrido[2,3-a:3,2-e]pyrrolizin-11-yl)ethyl]-2-furamide oxidized form hQR2-FAD Homo sapiens
0.00008
-
N-[2-(2-iodo-5-methoxy-1-methyl-4-nitroindol-3-yl)ethyl]acetamide oxidized form hQR2-FAD Homo sapiens
0.00018
-
S28128 oxidized form hQR2-FAD Homo sapiens
0.00031
-
N-[2-(2-iodo-5-methoxy-1-methyl-4-nitroindol-3-yl)ethyl]acetamide reduced form hQR2-FADH2 Homo sapiens
0.0009
-
S28128 reduced form hQR2-FADH2 Homo sapiens
0.004
-
2-iodo-melatonin reduced form hQR2-FADH2 Homo sapiens
0.012
-
2-iodo-5-methoxycarbonylamino-N-acetyltryptamine oxidized form hQR2-FAD Homo sapiens
0.033
-
2-iodo-5-methoxycarbonylamino-N-acetyltryptamine reduced form hQR2-FADH2 Homo sapiens
0.05
-
2-iodo-melatonin oxidized form hQR2-FAD Homo sapiens
0.15
-
Melatonin reduced form hQR2-FADH2 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000014
-
IC50: 14 nM Homo sapiens N-[2-(2-methoxy-6H-dipyrido[2,3-a:3,2-e]pyrrolizin-11-yl)ethyl]-2-furamide
0.0002
-
IC50: 0.0002 mM Homo sapiens N-[2-(2-methoxy-6H-pyrido[2',3':4,5]pyrrolo[2,1-a]isoindol-11-yl)ethyl]2-furamide
0.0003
-
inhibits enzymatic mechanism of the enzyme through the MT3 binding site, IC50: 0.0003 mM Homo sapiens N-[2-(2-iodo-5-methoxy-1-methyl-4-nitroindol-3-yl)ethyl]acetamide
0.00087
-
IC50: 0.00087 mM Homo sapiens 2-(2-methoxy-6H-pyrido[2',3':4,5]pyrrolo[2,1-a]isoindol-11-yl)ethylamine
0.00091
-
IC50: 0.00091 mM Homo sapiens S28128
0.0015
-
IC50: 0.0015 mM Homo sapiens N-[2-(5-methoxy-4-nitro-1H-indol-3-yl)ethyl]acetamide
0.0019
-
IC50: 0.0019 mM Homo sapiens N1-[2-(2-methoxy-6H-pyrido[2',3':4,5]pyrrolo[2,1-a]isoindol-11-yl)ethyl]-acetamide
0.005
-
IC50: 0.005 mM Homo sapiens N-[2-(8-methoxy-3,4-dihydro-2H-pyrido[2',3':4,5]pyrrolo[2,1-b][1,3]oxazin-10-yl)ethyl]-2-furamide
0.015
-
IC50: 0.015 mM Homo sapiens methyl-1-(2-acetamidoethyl)-7-naphthylcarbamate
0.016
-
IC50: 0.016 mM Homo sapiens 2-iodo-melatonin
0.038
-
IC50: 0.038 mM Homo sapiens N-[2-(7-methylaminosulfonyl-1-naphthyl)ethyl]acetamide
0.044
-
IC50: 0.044 mM Homo sapiens N-[2-(5-methoxy-7-nitro-1H-indol-3-yl)ethyl]acetamide
0.099
-
IC50: 0.099 mM Homo sapiens N-acetylserotonin
0.13
-
IC50: 0.13 mM Homo sapiens Melatonin
0.295
-
IC50: 0.295 mM Homo sapiens 5-methoxy-carbonylamino-N-acetyltryptamine
0.59
-
IC50: 0.59 mM Homo sapiens dicoumarol