General Information of the Protein
Protein ID
PT00838
Protein Name
NAD(P)H dehydrogenase [quinone] 1
Secondarily
Protein Name
Azoreductase
DT-diaphorase
Menadione reductase
NAD(P)H:quinone oxidoreductase 1
Phylloquinone reductase
Quinone reductase 1
Gene Name
NQO1
Secondarily
Gene Name
DIA4
NMOR1
Sequence
MVGRRALIVLAHSERTSFNYAMKEAAAAALKKKGWEVVESDLYAMNFNPIISRKDITGKLKDPANFQYPAESVLAYKEGHLSPDIVAEQKKLEAADLVIFQFPLQWFGVPAILKGWFERVFIGEFAYTYAAMYDKGPFRSKKAVLSITTGGSGSMYSLQGIHGDMNVILWPIQSGILHFCGFQVLEPQLTYSIGHTPADARIQILEGWKKRLENIWDETPLYFAPSSLFDLNFQAGFLMKKEVQDEEKNKKFGLSVGHHLGKSIPTDNQIKARK
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Oxidoreductase
Function
Flavin-containing quinone reductase that catalyzes two-electron reduction of quinones to hydroquinones using either NADH or NADPH as electron donors. In a ping-pong kinetic mechanism, the electrons are sequentially transferred from NAD(P)H to flavin cofactor and then from reduced flavin to the quinone, bypassing the formation of semiquinone and reactive oxygen species (PubMed:8999809, PubMed:9271353) (By similarity). Regulates cellular redox state primarily through quinone detoxification. Reduces components of plasma membrane redox system such as coenzyme Q and vitamin quinones, producing antioxidant hydroquinone forms. In the process may function as superoxide scavenger to prevent hydroquinone oxidation and facilitate excretion (PubMed:8999809, PubMed:9271353, PubMed:15102952). Alternatively, can activate quinones and their derivatives by generating redox reactive hydroquinones with DNA cross-linking antitumor potential (PubMed:8999809). Acts as a gatekeeper of the core 20S proteasome known to degrade proteins with unstructured regions. Upon oxidative stress, interacts with tumor suppressors TP53 and TP73 in a NADH-dependent way and inhibits their ubiquitin-independent degradation by the 20S proteasome (PubMed:15687255, PubMed:28291250).
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Uniprot ID
Primary ID:
P15559

Secondarily ID:
B2R5Y9
B4DNM7
B7ZAD1
Q86UK1
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Ensembl ID
ENSG00000181019
HGNC ID
HGNC:2874
Subcellular Location
Cytoplasm
Cytosol
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000068 , A-549
Compound ID Compound Name Compound Formula
CP0456142
2,2-dimethyl-3-[3-[1-(phenylselanylmethyl)triazol-4-yl]anilino]-3H-benzo[g][1]benzofuran-4,5-dione
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C29H24N4O3Se
 2
1
IC50 = 640 nM
   TI
   LI
   LO
   TS
2
IC50 > 3200 nM
   TI
   LI
   LO
   TS
CP0503890
2,2-dimethyl-3-[4-(phenylselanylmethyl)triazol-1-yl]-3H-benzo[g][1]benzofuran-4,5-dione
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C23H19N3O3Se
 2
1
IC50 = 1200 nM
   TI
   LI
   LO
   TS
2
IC50 > 3200 nM
   TI
   LI
   LO
   TS
CP0522655
3-(4-fluoro-3-nitroanilino)-2,2-dimethyl-3H-benzo[g][1]benzofuran-4,5-dione
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C20H15FN2O5
 2
1
IC50 = 1300 nM
   TI
   LI
   LO
   TS
2
IC50 > 3200 nM
   TI
   LI
   LO
   TS
CP0503889
2,2-dimethyl-3-(4-nitroanilino)-3H-benzo[g][1]benzofuran-4,5-dione
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C20H16N2O5
 2
1
IC50 = 1800 nM
   TI
   LI
   LO
   TS
2
IC50 > 3200 nM
   TI
   LI
   LO
   TS
CP0398276
3-(4-methoxy-2-nitroanilino)-2,2-dimethyl-3H-benzo[g][1]benzofuran-4,5-dione
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C21H18N2O6
 2
1
IC50 = 2400 nM
   TI
   LI
   LO
   TS
2
IC50 > 3200 nM
   TI
   LI
   LO
   TS
CP0427329
2,2-dimethyl-3-(3-nitroanilino)-3H-benzo[g][1]benzofuran-4,5-dione
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C20H16N2O5
 2
1
IC50 = 2600 nM
   TI
   LI
   LO
   TS
2
IC50 > 3200 nM
   TI
   LI
   LO
   TS
CP0393114
3,6,9-trimethylbenzo[g][1]benzofuran-4,5-dione
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C15H12O3
 1
1
IC50 = 2900 nM
   TI
   LI
   LO
   TS
CP0049432
&#946;-Lapachone (A3)
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C15H14O3
 3
1
IC50 = 3000 nM
   TI
   LI
   LO
   TS
2
IC50 = 3400 nM
   TI
   LI
   LO
   TS
3
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0393954
7,8-dimethylbenzo[g][1]benzofuran-4,5-dione
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C14H10O3
 1
1
IC50 = 3100 nM
   TI
   LI
   LO
   TS
CP0517956
3-ethyl-7-methylbenzo[g][1]benzofuran-4,5-dione
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C15H12O3
 1
1
IC50 = 3100 nM
   TI
   LI
   LO
   TS
CP0393115
3,7,8-trimethylbenzo[g][1]benzofuran-4,5-dione
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C15H12O3
 1
1
IC50 = 3300 nM
   TI
   LI
   LO
   TS
CP0476132
3,8-dimethylbenzo[g][1]benzofuran-4,5-dione
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C14H10O3
 1
1
IC50 = 4100 nM
   TI
   LI
   LO
   TS
CP0147298
8-methoxy-2,3,3-trimethyl-2H-benzo[g][1]benzofuran-4,5-dione
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C16H16O4
 1
1
IC50 = 5800 nM
   TI
   LI
   LO
   TS
CP0393953
3,7-dimethylbenzo[g][1]benzofuran-4,5-dione
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C14H10O3
 1
1
IC50 = 8500 nM
   TI
   LI
   LO
   TS
CP0053557
9-methoxy-2,3,3-trimethyl-2H-benzo[g][1]benzofuran-4,5-dione
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C16H16O4
 1
1
IC50 = 11000 nM
   TI
   LI
   LO
   TS
CP0404787
3-ethyl-7,8-dimethylbenzo[g][1]benzofuran-4,5-dione
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C16H14O3
 1
1
IC50 = 11000 nM
   TI
   LI
   LO
   TS
CP0147297
7-methoxy-2,3,3-trimethyl-2H-benzo[g][1]benzofuran-4,5-dione
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C16H16O4
 1
1
IC50 = 12000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0116250
7-[4-(4-methylpiperazin-1-yl)anilino]quinoline-5,8-dione
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C20H20N4O2
 2
1 Km = 40170 nM
2 Km = 55170 nM
CP0116251
6-[4-(4-methylpiperazin-1-yl)anilino]quinoline-5,8-dione
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C20H20N4O2
 2
1 Km = 45270 nM
2 Km = 60150 nM
Clinical Information about the Protein
Target 1 ( Quinone reductase 1 (NQO1) )
Target Type Clinical trial Target