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Literature summary 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

EC Number Inhibitors Comment Organism Structure
1.10.5.1 2-(2-methoxy-6H-pyrido[2',3':4,5]pyrrolo[2,1-a]isoindol-11-yl)ethylamine IC50: 0.00087 mM Homo sapiens
1.10.5.1 2-iodo-5-methoxycarbonylamino-N-acetyltryptamine
-
 Homo sapiens
1.10.5.1 2-iodo-melatonin IC50: 0.016 mM Homo sapiens
1.10.5.1 5-methoxy-carbonylamino-N-acetyltryptamine IC50: 0.295 mM Homo sapiens
1.10.5.1 dicoumarol IC50: 0.59 mM Homo sapiens
1.10.5.1 Melatonin IC50: 0.13 mM Homo sapiens
1.10.5.1 methyl-1-(2-acetamidoethyl)-7-naphthylcarbamate IC50: 0.015 mM Homo sapiens
1.10.5.1 N-acetylserotonin IC50: 0.099 mM Homo sapiens
1.10.5.1 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
1.10.5.1 N-[2-(2-methoxy-6H-dipyrido[2,3-a:3,2-e]pyrrolizin-11-yl)ethyl]-2-furamide IC50: 14 nM Homo sapiens
1.10.5.1 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
1.10.5.1 N-[2-(5-methoxy-4-nitro-1H-indol-3-yl)ethyl]acetamide IC50: 0.0015 mM Homo sapiens
1.10.5.1 N-[2-(5-methoxy-7-nitro-1H-indol-3-yl)ethyl]acetamide IC50: 0.044 mM Homo sapiens
1.10.5.1 N-[2-(7-methylaminosulfonyl-1-naphthyl)ethyl]acetamide IC50: 0.038 mM Homo sapiens
1.10.5.1 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
1.10.5.1 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
1.10.5.1 S28128 IC50: 0.00091 mM Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.10.5.1 0.0067
-
 menadione pH 8.5, 25°C, fluorescence assay Homo sapiens
1.10.5.1 0.017
-
 menadione pH 8.5, HPLC approach Homo sapiens
1.10.5.1 0.02
-
 dihydrobenzylnicotinamide pH 8.5, 25°C, fluorescence assay Homo sapiens
1.10.5.1 0.04
-
 dihydrobenzylnicotinamide pH 8.5, HPLC approach Homo sapiens

Organism

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

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
1.10.5.1 QR2
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.10.5.1 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
1.10.5.1 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
1.10.5.1 0.00008
-
 N-[2-(2-iodo-5-methoxy-1-methyl-4-nitroindol-3-yl)ethyl]acetamide oxidized form hQR2-FAD Homo sapiens
1.10.5.1 0.00018
-
 S28128 oxidized form hQR2-FAD Homo sapiens
1.10.5.1 0.00031
-
 N-[2-(2-iodo-5-methoxy-1-methyl-4-nitroindol-3-yl)ethyl]acetamide reduced form hQR2-FADH2 Homo sapiens
1.10.5.1 0.0009
-
 S28128 reduced form hQR2-FADH2 Homo sapiens
1.10.5.1 0.004
-
 2-iodo-melatonin reduced form hQR2-FADH2 Homo sapiens
1.10.5.1 0.012
-
 2-iodo-5-methoxycarbonylamino-N-acetyltryptamine oxidized form hQR2-FAD Homo sapiens
1.10.5.1 0.033
-
 2-iodo-5-methoxycarbonylamino-N-acetyltryptamine reduced form hQR2-FADH2 Homo sapiens
1.10.5.1 0.05
-
 2-iodo-melatonin oxidized form hQR2-FAD Homo sapiens
1.10.5.1 0.15
-
 Melatonin reduced form hQR2-FADH2 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.10.5.1 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
1.10.5.1 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
1.10.5.1 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
1.10.5.1 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
1.10.5.1 0.00091
-
 IC50: 0.00091 mM Homo sapiens S28128
1.10.5.1 0.0015
-
 IC50: 0.0015 mM Homo sapiens N-[2-(5-methoxy-4-nitro-1H-indol-3-yl)ethyl]acetamide
1.10.5.1 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
1.10.5.1 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
1.10.5.1 0.015
-
 IC50: 0.015 mM Homo sapiens methyl-1-(2-acetamidoethyl)-7-naphthylcarbamate
1.10.5.1 0.016
-
 IC50: 0.016 mM Homo sapiens 2-iodo-melatonin
1.10.5.1 0.038
-
 IC50: 0.038 mM Homo sapiens N-[2-(7-methylaminosulfonyl-1-naphthyl)ethyl]acetamide
1.10.5.1 0.044
-
 IC50: 0.044 mM Homo sapiens N-[2-(5-methoxy-7-nitro-1H-indol-3-yl)ethyl]acetamide
1.10.5.1 0.099
-
 IC50: 0.099 mM Homo sapiens N-acetylserotonin
1.10.5.1 0.13
-
 IC50: 0.13 mM Homo sapiens Melatonin
1.10.5.1 0.295
-
 IC50: 0.295 mM Homo sapiens 5-methoxy-carbonylamino-N-acetyltryptamine
1.10.5.1 0.59
-
 IC50: 0.59 mM Homo sapiens dicoumarol