NQO2
gene geneOn this page
Also known as QR2DHQVDIA6
Summary
NQO2 (N-ribosyldihydronicotinamide:quinone dehydrogenase 2, HGNC:7856) is a protein-coding gene on chromosome 6p25.2, encoding Ribosyldihydronicotinamide dehydrogenase [quinone] (P16083). The enzyme apparently serves as a quinone reductase in connection with conjugation reactions of hydroquinones involved in detoxification pathways as well as in biosynthetic processes such as the vitamin K-dependent gamma-carboxylation of glutamate residues in prothrombin synthes….
This gene encodes a member of the thioredoxin family of enzymes. It is a cytosolic and ubiquitously expressed flavoprotein that catalyzes the two-electron reduction of quinone substrates and uses dihydronicotinamide riboside as a reducing coenzyme. Mutations in this gene have been associated with neurodegenerative diseases and several cancers. Alternative splicing results in multiple transcript variants.
Source: NCBI Gene 4835 — RefSeq curated summary.
At a glance
- GWAS associations: 3
- Clinical variants (ClinVar): 48 total
- GTEx eGene: eQTL in 50 tissues, sQTL in 50 (q < 0.05)
- Phenotypes (HPO): 3
- ChEMBL bioactivity: 45 clinical-phase molecules tested; no curated mechanism-of-action drug
- Constraint (gnomAD): pLI 0.00 (LoF-tolerant), LOEUF 1.07 (unconstrained)
- MANE Select transcript:
NM_000904
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:7856 |
| Approved symbol | NQO2 |
| Name | N-ribosyldihydronicotinamide:quinone dehydrogenase 2 |
| Location | 6p25.2 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | QR2, DHQV, DIA6 |
| Ensembl gene | ENSG00000124588 |
| Ensembl biotype | protein_coding |
| OMIM | 160998 |
| Entrez | 4835 |
Gene structure
Transcript identifiers
Ensembl transcripts: 109 — 100 protein_coding, 9 nonsense_mediated_decay
MANE Select: ENST00000380455
Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 1, TSL 2: 2, TSL 3: 1, TSL 5: 5
ENST00000380455, ENST00000338130, ENST00000380430, ENST00000380441, ENST00000380454, ENST00000380472, ENST00000397717, ENST00000426637, ENST00000606474, ENST00000892207, ENST00000892208, ENST00000892209, ENST00000892210, ENST00000892211, ENST00000892212, ENST00000892213, ENST00000892214, ENST00000892215, ENST00000892216, ENST00000892217, ENST00000892218, ENST00000892219, ENST00000892220, ENST00000892221, ENST00000892222, ENST00000892223, ENST00000892224, ENST00000892225, ENST00000892226, ENST00000892227, ENST00000892228, ENST00000892229, ENST00000892230, ENST00000892231, ENST00000892232, ENST00000892233, ENST00000892234, ENST00000892235, ENST00000892236, ENST00000892237, ENST00000892238, ENST00000892239, ENST00000892240, ENST00000892241, ENST00000929205, ENST00000929206, ENST00000929207, ENST00000929208, ENST00000929209, ENST00000929210, ENST00000929211, ENST00000929212, ENST00000929213, ENST00000929214, ENST00000929215, ENST00000929216, ENST00000929217, ENST00000929218, ENST00000929219, ENST00000929220, ENST00000929221, ENST00000929222, ENST00000929223, ENST00000929224, ENST00000929225, ENST00000929226, ENST00000929227, ENST00000929228, ENST00000929229, ENST00000952437, ENST00000952438, ENST00000952439, ENST00000952440, ENST00000952441, ENST00000952442, ENST00000952443, ENST00000952444, ENST00000952445, ENST00000952446, ENST00000952447, ENST00000952448, ENST00000952449, ENST00000952450, ENST00000952451, ENST00000952452, ENST00000952453, ENST00000952454, ENST00000952455, ENST00000952456, ENST00000952457, ENST00000998161, ENST00000998162, ENST00000998163, ENST00000998164, ENST00000998165, ENST00000998166, ENST00000998167, ENST00001014418, ENST00001088532, ENST00001088533, ENST00001088534, ENST00001088536, ENST00001095041, ENST00001106026, ENST00001118853, ENST00001118854, ENST00001122522, ENST00001122523, ENST00001139934
RefSeq mRNA: 4 — MANE Select: NM_000904
NM_000904, NM_001290221, NM_001290222, NM_001318940
CCDS: CCDS4481, CCDS75388
Canonical transcript exons
ENST00000380455 — 7 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000680401 | 3016884 | 3016985 |
| ENSE00000847812 | 3012544 | 3012674 |
| ENSE00001083962 | 3010025 | 3010189 |
| ENSE00001398818 | 3019479 | 3019755 |
| ENSE00001728408 | 2999894 | 3000085 |
| ENSE00001777236 | 3006468 | 3006559 |
| ENSE00003785120 | 3015530 | 3015643 |
Expression profiles
Bgee: expression breadth ubiquitous, 281 present calls, max score 97.69.
FANTOM5 (CAGE): breadth broad, TPM avg 1.6852 / max 48.3036, expressed in 882 samples.
Highest expression (Bgee): adrenal gland, adrenal gland cortex, adrenal cortex, adult mammalian kidney, triceps brachii.
Genetic regulation across tissues (GTEx eQTL / sQTL)
NQO2 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 50 tissues and its splicing (sQTL) in 50 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.
showing 20 of 100 significant tissue × QTL associations:
| Tissue | QTL | q-value | Slope | Lead variant |
|---|---|---|---|---|
| Cells Cultured fibroblasts | eqtl | 1.5e-154 | -1.06 | 6:3003736:A:G |
| Skin Sun Exposed Lower leg | sqtl | 4.2e-152 | -1.32 | 6:3003736:A:G |
| Muscle Skeletal | eqtl | 1.8e-146 | -0.92 | 6:3003736:A:G |
| Skin Sun Exposed Lower leg | eqtl | 5.0e-144 | -0.92 | 6:3003736:A:G |
| Skin Not Sun Exposed Suprapubic | sqtl | 9.7e-131 | -1.24 | 6:3003736:A:G |
| Adipose Subcutaneous | sqtl | 1.3e-128 | -1.32 | 6:3003736:A:G |
| Artery Tibial | eqtl | 2.8e-128 | -0.88 | 6:3003736:A:G |
| Artery Tibial | sqtl | 1.8e-124 | -1.25 | 6:3003736:A:G |
| Muscle Skeletal | sqtl | 2.6e-123 | -1.05 | 6:3010915:C:T |
| Thyroid | sqtl | 3.1e-122 | -1.15 | 6:3003736:A:G |
| Skin Not Sun Exposed Suprapubic | eqtl | 6.1e-121 | -0.91 | 6:3003736:A:G |
| Esophagus Muscularis | eqtl | 6.8e-121 | -1.07 | 6:3003736:A:G |
| Adipose Subcutaneous | eqtl | 3.4e-119 | -0.81 | 6:3003736:A:G |
| Esophagus Mucosa | eqtl | 2.9e-118 | -0.97 | 6:3003736:A:G |
| Whole Blood | sqtl | 2.5e-117 | -1.01 | 6:3010915:C:T |
| Nerve Tibial | eqtl | 1.2e-110 | -0.84 | 6:3003736:A:G |
| Nerve Tibial | sqtl | 2.9e-109 | -1.10 | 6:3010915:C:T |
| Heart Left Ventricle | eqtl | 3.2e-104 | -1.05 | 6:3003736:A:G |
| Heart Atrial Appendage | eqtl | 3.4e-104 | -1.11 | 6:3003736:A:G |
| Esophagus Mucosa | sqtl | 3.7e-98 | -1.14 | 6:3013080:C:T |
FANTOM5 promoters
6 alternative TSS:
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 65504 | 15.9179 | 1792 |
| 65505 | 13.3034 | 1704 |
| 65506 | 2.4246 | 1064 |
| 65499 | 1.6852 | 882 |
| 65507 | 0.9466 | 550 |
| 65508 | 0.5207 | 299 |
Top tissues by expression
showing 100 of 293 tissues by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| left adrenal gland | UBERON:0001234 | 97.69 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 97.62 | gold quality |
| right adrenal gland | UBERON:0001233 | 97.46 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 97.39 | gold quality |
| adrenal cortex | UBERON:0001235 | 97.19 | gold quality |
| adult mammalian kidney | UBERON:0000082 | 97.03 | gold quality |
| triceps brachii | UBERON:0001509 | 96.47 | gold quality |
| right lobe of liver | UBERON:0001114 | 96.18 | gold quality |
| adrenal gland | UBERON:0002369 | 96.17 | gold quality |
| gastrocnemius | UBERON:0001388 | 95.75 | gold quality |
| apex of heart | UBERON:0002098 | 95.72 | gold quality |
| nephron tubule | UBERON:0001231 | 95.59 | gold quality |
| adult organism | UBERON:0007023 | 95.54 | gold quality |
| right coronary artery | UBERON:0001625 | 95.40 | gold quality |
| muscle of leg | UBERON:0001383 | 95.30 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 95.23 | gold quality |
| right atrium auricular region | UBERON:0006631 | 94.56 | gold quality |
| heart left ventricle | UBERON:0002084 | 94.46 | gold quality |
| cardiac ventricle | UBERON:0002082 | 94.27 | gold quality |
| kidney | UBERON:0002113 | 94.22 | gold quality |
| left coronary artery | UBERON:0001626 | 94.19 | gold quality |
| adipose tissue | UBERON:0001013 | 94.11 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 94.05 | gold quality |
| connective tissue | UBERON:0002384 | 93.88 | gold quality |
| blood | UBERON:0000178 | 93.86 | gold quality |
| adipose tissue of abdominal region | UBERON:0007808 | 93.86 | gold quality |
| omental fat pad | UBERON:0010414 | 93.85 | gold quality |
| peritoneum | UBERON:0002358 | 93.82 | gold quality |
| coronary artery | UBERON:0001621 | 93.80 | gold quality |
| subcutaneous adipose tissue | UBERON:0002190 | 93.79 | gold quality |
| granulocyte | CL:0000094 | 93.77 | gold quality |
| liver | UBERON:0002107 | 93.76 | gold quality |
| kidney epithelium | UBERON:0004819 | 93.69 | gold quality |
| cortex of kidney | UBERON:0001225 | 93.66 | gold quality |
| muscle organ | UBERON:0001630 | 93.66 | gold quality |
| cardiac atrium | UBERON:0002081 | 93.55 | gold quality |
| right frontal lobe | UBERON:0002810 | 93.45 | gold quality |
| heart | UBERON:0000948 | 93.39 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 93.37 | gold quality |
| periodontal ligament | UBERON:0008266 | 93.36 | gold quality |
| popliteal artery | UBERON:0002250 | 93.25 | gold quality |
| tibial artery | UBERON:0007610 | 93.25 | gold quality |
| skin of leg | UBERON:0001511 | 93.22 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 93.10 | gold quality |
| olfactory segment of nasal mucosa | UBERON:0005386 | 93.09 | gold quality |
| monocyte | CL:0000576 | 93.04 | gold quality |
| aorta | UBERON:0000947 | 93.01 | gold quality |
| cerebellar cortex | UBERON:0002129 | 93.01 | gold quality |
| thoracic aorta | UBERON:0001515 | 92.92 | gold quality |
| ascending aorta | UBERON:0001496 | 92.91 | gold quality |
| stromal cell of endometrium | CL:0002255 | 92.85 | gold quality |
| skin of abdomen | UBERON:0001416 | 92.81 | gold quality |
| mucosa of stomach | UBERON:0001199 | 92.70 | gold quality |
| leukocyte | CL:0000738 | 92.68 | gold quality |
| mononuclear cell | CL:0000842 | 92.65 | gold quality |
| minor salivary gland | UBERON:0001830 | 92.65 | gold quality |
| saliva-secreting gland | UBERON:0001044 | 92.53 | gold quality |
| metanephros cortex | UBERON:0010533 | 92.52 | gold quality |
| skin of hip | UBERON:0001554 | 92.50 | gold quality |
| prefrontal cortex | UBERON:0000451 | 92.46 | gold quality |
| skeletal muscle tissue of biceps brachii | UBERON:0004502 | 92.38 | gold quality |
| heart right ventricle | UBERON:0002080 | 92.30 | gold quality |
| cingulate cortex | UBERON:0003027 | 92.27 | gold quality |
| left uterine tube | UBERON:0001303 | 92.25 | gold quality |
| ectocervix | UBERON:0012249 | 92.21 | gold quality |
| anterior cingulate cortex | UBERON:0009835 | 92.15 | gold quality |
| zone of skin | UBERON:0000014 | 92.11 | gold quality |
| Brodmann (1909) area 9 | UBERON:0013540 | 92.10 | gold quality |
| skeletal muscle tissue of rectus abdominis | UBERON:0004511 | 92.09 | gold quality |
| body of pancreas | UBERON:0001150 | 92.04 | gold quality |
| body of stomach | UBERON:0001161 | 92.04 | gold quality |
| dorsolateral prefrontal cortex | UBERON:0009834 | 92.02 | gold quality |
| right lung | UBERON:0002167 | 91.90 | gold quality |
| upper leg skin | UBERON:0004262 | 91.83 | gold quality |
| esophagogastric junction muscularis propria | UBERON:0035841 | 91.69 | gold quality |
| trabecular bone tissue | UBERON:0002483 | 91.66 | gold quality |
| mouth mucosa | UBERON:0003729 | 91.56 | gold quality |
| cerebellum | UBERON:0002037 | 91.48 | gold quality |
| endocervix | UBERON:0000458 | 91.41 | gold quality |
| lower esophagus muscularis layer | UBERON:0035833 | 91.38 | gold quality |
| lower esophagus | UBERON:0013473 | 91.37 | gold quality |
| tendon of biceps brachii | UBERON:0008188 | 91.29 | gold quality |
| right ovary | UBERON:0002118 | 91.22 | gold quality |
| renal glomerulus | UBERON:0000074 | 91.03 | gold quality |
| gall bladder | UBERON:0002110 | 90.94 | gold quality |
| renal medulla | UBERON:0000362 | 90.86 | gold quality |
| left ovary | UBERON:0002119 | 90.85 | gold quality |
| metanephric glomerulus | UBERON:0004736 | 90.79 | gold quality |
| metanephros | UBERON:0000081 | 90.74 | gold quality |
| biceps brachii | UBERON:0001507 | 90.72 | gold quality |
| amygdala | UBERON:0001876 | 90.72 | gold quality |
| esophagus | UBERON:0001043 | 90.57 | gold quality |
| spleen | UBERON:0002106 | 90.56 | gold quality |
| bone marrow | UBERON:0002371 | 90.51 | gold quality |
| skeletal muscle tissue | UBERON:0001134 | 90.35 | gold quality |
| tibial nerve | UBERON:0001323 | 90.33 | gold quality |
| parotid gland | UBERON:0001831 | 90.31 | gold quality |
| esophagus mucosa | UBERON:0002469 | 90.24 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 90.18 | gold quality |
| lateral nuclear group of thalamus | UBERON:0002736 | 90.14 | gold quality |
Single-cell (SCXA)
Detected in 5 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-6524 | no | 189.63 |
| E-GEOD-109979 | no | 173.69 |
| E-MTAB-8271 | no | 162.96 |
| E-GEOD-124858 | no | 107.97 |
| E-ANND-3 | no | 0.00 |
HPA expression
RNA tissue specificity: Low tissue specificity
showing 60 of 78 HPA tissues / cells by nTPM:
| Tissue / cell | Axis | nTPM | Protein (IHC) |
|---|---|---|---|
| Kidney | tissue | 177.3 | high |
| Tongue | tissue | 135.5 | |
| Liver | tissue | 103.5 | medium |
| Choroid plexus | tissue | 100.8 | |
| Postcentral gyrus | tissue | 98.3 | |
| Bone marrow | tissue | 68.0 | low |
| Locus coeruleus | tissue | 65.1 | |
| Adrenal gland | tissue | 63.7 | medium |
| Salivary gland | tissue | 58.2 | low |
| Skeletal muscle | tissue | 57.2 | medium |
| Adipose tissue | tissue | 56.2 | low |
| Spinal cord | tissue | 52.8 | |
| Hippocampus | tissue | 50.4 | low |
| Corpus callosum | tissue | 50.2 | |
| Skin 1 | tissue | 47.7 | not detected |
| Superior colliculi | tissue | 47.6 | |
| Medulla oblongata | tissue | 47.5 | |
| Nucleus accumbens | tissue | 43.9 | |
| Pons | tissue | 43.1 | |
| Thalamus | tissue | 42.6 | |
| Midbrain | tissue | 40.8 | |
| Pancreas | tissue | 40.2 | not detected |
| Substantia nigra | tissue | 39.3 | |
| Heart muscle | tissue | 38.8 | medium |
| Periaqueductal gray | tissue | 34.1 | |
| Small intestine | tissue | 33.4 | medium |
| Duodenum | tissue | 33.1 | medium |
| Parathyroid gland | tissue | 31.4 | low |
| Cerebral cortex | tissue | 31.3 | low |
| Somatosensory cortex | tissue | 31.3 | |
| Epididymis | tissue | 30.9 | low |
| Ventral forebrain | tissue | 30.7 | |
| Ovary | tissue | 30.4 | not detected |
| Hypothalamus | tissue | 30.1 | |
| Hippocampal formation | tissue | 29.9 | |
| Gallbladder | tissue | 29.4 | low |
| Retina | tissue | 28.7 | |
| Occipital cortex | tissue | 27.7 | |
| Temporal cortex | tissue | 27.4 | |
| Putamen | tissue | 27.2 | |
| Seminal vesicle | tissue | 27.1 | low |
| Breast | tissue | 27.0 | medium |
| Septum | tissue | 27.0 | |
| Placenta | tissue | 26.8 | low |
| Vagina | tissue | 26.4 | not detected |
| Motor cortex | tissue | 26.3 | |
| Prostate | tissue | 26.2 | low |
| Insular cortex | tissue | 25.8 | |
| Lung | tissue | 25.6 | low |
| Retrosplenial cortex | tissue | 25.6 | |
| Amygdala | tissue | 25.5 | |
| Cervix | tissue | 25.4 | not detected |
| Entorhinal cortex | tissue | 25.4 | |
| Appendix | tissue | 25.2 | not detected |
| Esophagus | tissue | 25.1 | not detected |
| Retrosplenial and cingulate cortex | tissue | 25.1 | |
| Prefrontal cortex | tissue | 25.0 | |
| Thyroid gland | tissue | 24.9 | medium |
| Basal ganglia | tissue | 24.2 | low |
| Urinary bladder | tissue | 23.4 | low |
Brain sub-regions (HPA Brain Atlas): detected in 190; highest nTPM — Nucleus raphe magnus (94.4), Nuclei of the trapezoid body (93.6), Precentral gyrus (93.3), Vermis (92.5), Flocculonodular lobe (92.4).
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): JUND, NFE2L2, SP1, SP3
miRNA regulators (miRDB)
Targeting NQO2 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).
15 miRNAs:
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-9-3P | 99.96 | 70.88 | 2068 |
| HSA-MIR-495-3P | 99.96 | 72.81 | 4197 |
| HSA-MIR-5688 | 99.96 | 73.23 | 4504 |
| HSA-MIR-590-3P | 99.96 | 74.34 | 6478 |
| HSA-MIR-4753-3P | 99.90 | 71.03 | 3786 |
| HSA-MIR-320A-3P | 99.77 | 69.73 | 2107 |
| HSA-MIR-320B | 99.77 | 69.73 | 2107 |
| HSA-MIR-320C | 99.77 | 69.73 | 2107 |
| HSA-MIR-320D | 99.77 | 69.73 | 2107 |
| HSA-MIR-4429 | 99.77 | 69.62 | 2111 |
| HSA-MIR-942-5P | 99.41 | 68.40 | 1977 |
| HSA-MIR-193A-3P | 98.59 | 66.36 | 769 |
| HSA-MIR-193B-3P | 98.59 | 66.62 | 748 |
| HSA-MIR-4448 | 97.04 | 66.22 | 752 |
| HSA-MIR-6772-3P | 97.04 | 65.89 | 784 |
Functional genomics
gnomAD constraint: pLI 7.75e-06, LOEUF 1.07, missense Z 0.719 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD
Regional missense constraint (gnomAD RMC): no regional variation along ENST00000380455 — one region, missense o/e 0.93.
Literature-anchored findings (GeneRIF, showing 35)
- polymorphisms associated with idiopathic Parkinson’s disease (PMID:11688992)
- A significant difference was found between alcoholic patients and controls in genotype frequency at an insertion/deletion site in the promoter region of the NQO2 gene (p = 0.0014). (PMID:12960511)
- the level of NQO2 mRNA is low in AGR patients compared with the control group. Such a reduction in message suggests that the NQO2 gene may be involved in the development of clozapine-induced AGR. (PMID:14617031)
- NQO2 gene may confer susceptibility to a certain form of schizophrenia. (PMID:14639047)
- the NQO2 gene is differentially expressed by the polymorphic promoters in human cells transfected with NQO2 gene reporter constructs. Alterations in NQO2 activity might be an important factor in susceptibility to Parkinson’s disease. (PMID:15451063)
- We propose that induction of NQO2 may relate to the observed increased expression of p53 that, in turn, contributes to the observed suppression of cell growth in both melanoma cell lines. (PMID:15993843)
- the nicotinamide adenine dinucleotide phosphate reduced-diaphorase interneurons in the human striatum. (PMID:16025450)
- The results combined demonstrated that Nrf2 associates with JunD, binds to ARE at nucleotide -1433, and regulates human NQO2 gene expression and induction in response to antioxidants. (PMID:16545679)
- an apparent association between an NQO2 exon 3 single-nucleotide polymorphism and lower enzymatic activity (PMID:17332305)
- The crystal structure of melatonin and 2-iodomelatonin in complex with QR2 provide a detailed description of the enzyme active site; the design of inhibitors of the enzyme might be instrumental in discriminating the role of MT1, MT2 and QR2/MT3 (PMID:18254726)
- Parkinson’s disease patients were analyzed for NQO2 gene promoter polymorphisms. Three allelic variants were I-29, I-16 and D. The association of the D promoter with Parkinson’s disease may be due to an increase in expression of the NQO2 gene. (PMID:18314446)
- This first structural analysis of hQR2 should enable to better understand the biological role of melatonin on this enzyme . (PMID:18502195)
- We observed a nominal significant association between the rs1143684 NQO2 polymorphism and the trajectory of delayed memory recall over time (p=0.029). No other associations were seen with the decline of other cognitive abilities. (PMID:18538895)
- Quinone reductase 2 is a catechol quinone reductase. quinone reductase 2 could play important roles in the regulation of catecholamine oxidation processes that may be involved in the etiology of Parkinson disease. (PMID:18579530)
- nmr studies of QR2 catalytic reaction were performed; results led to conclusion that melatonin is not cleaved to form N1-acetyl-N2-formyl-5-methoxykynurenine by a catalytically active QR2, indicating melatonin is neither a substrate nor a co-substrate (PMID:18826489)
- NQO2 is a susceptibility gene for breast carcinogenesis. (PMID:19351655)
- Our findings challenge the previous assumption that the NQo2 I-16 allele is stable only when paired with another I-16 allele (PMID:19495956)
- The first European study of the SOD2, SOD3, NQO1, and NQO2 roles in pancreatic cancer etiology did not find significant associations. (PMID:20966810)
- The NQO1 609C>T TT genotype and T allele were significantly associated with increased risk for gastric cancer (GC), whereas NQO2 -3423G>A polymorphism did not show any association with GC. (PMID:21294640)
- Results suggest that NQO2, SOD2 and SOD3 may significantly modify prognosis of breast cancer patients. (PMID:21351093)
- NQO2 is a target gene of the BACH1 transcription factor according to ChIP-seq analysis in HEK 293 cells. (PMID:21555518)
- Selective inhibition of NQO2 over NQO1 can be attributed to the bulky aminoalkylamino substituent at the 5-position, which blocks entrance of the indolequinones into the NQO1 active site. (PMID:21718050)
- results suggest that the increase in hippocampal QR2 might be a cause of AD or might promote the progression of AD by causing an increase in the toxic quinone levels and consequent loss of cognitive function. (PMID:21803122)
- both NQO1 and NQO2 modulate the efficacy of AC therapy and that NQO2 is associated with tamoxifen toxicity. (PMID:21946896)
- results indicate a role of NQO2 in the control of AKT/GSK-3beta/cyclin D1 and highlight the involvement of NQO2 in degradation of cyclin D1, as part of mechanism of chemoprevention by resveratrol (PMID:22266466)
- NQO1 609C>T and NQO2 -3423G>A polymorphisms do not seem to play any significant role in susceptibility or prognosis of EC in north Indian population. (PMID:22770696)
- Diplotypes of NQO1 (exon 4 and 6), C-T (OR = 1.56, Pc = 0.007) and T-T (OR = 0.011, Pc = 3.86) was associated with an increased risk for prostate cancer (PCa). NQO2 and MTHFR did not show any risk with PCa. (PMID:23054000)
- This first structure of a reduced quinone reductase shows that reduction of the FAD cofactor and binding of a specific inhibitor lead to global changes in NQO2 structure and is consistent with a functional role for NQO2 as a flavin redox switch. (PMID:23471972)
- NQO2-L47 is less stable towards proteolytic digestion and thermal denaturation than NQO2-F47. (PMID:24631540)
- In patients with Alzheimer’s disease, QR2 is overexpressed in the insular cotex. (PMID:26609153)
- The ontogeny and population variability of human hepatic dihydronicotinamide riboside:quinone oxidoreductase (NQO2). (PMID:28346733)
- these data suggest that the overexpression of QR2 in brain cells in the presence of catechol quinones might lead to reactive oxygen species-induced cell death via the rapid conversion of superoxide radicals into hydrogen peroxide and then into highly reactive hydroxyl radicals (PMID:29526807)
- Cancer-associated variants of human NQO1: impacts on inhibitor binding and cooperativity. (PMID:31431515)
- An Axis between the Long Non-Coding RNA HOXA11-AS and NQOs Enhances Metastatic Ability in Oral Squamous Cell Carcinoma. (PMID:36142607)
- Polymorphisms and Pharmacogenomics of NQO2: The Past and the Future. (PMID:38254976)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Nqo2 | ENSMUSG00000046949 |
| rattus_norvegicus | Nqo2 | ENSRNOG00000017820 |
| rattus_norvegicus | AABR07044714.1 | ENSRNOG00000053936 |
Paralogs (1): NQO1 (ENSG00000181019)
Mouse-model phenotypes
Observed phenotypes of the mouse ortholog (MGI:104513) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 9 distinct phenotype terms.
| Mouse phenotype (MP) | Records |
|---|---|
| increased granulocyte number | 1 |
| abnormal spatial learning | 1 |
| abnormal lymphopoiesis | 1 |
| abnormal motor learning | 1 |
| thrombocytosis | 1 |
| abnormal enzyme/coenzyme activity | 1 |
| abnormal spatial working memory | 1 |
| increased skin tumor incidence | 1 |
| enhanced long-term object recognition memory | 1 |
Additional cross-species homologs
Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.
| Organism | UniProt | Identity | Method |
|---|---|---|---|
| Pongo abelii | Q5RD31 | 98.9% | Diamond |
| Cavia porcellus | Q8CHK7 | 86.0% | Diamond |
| Haemophilus influenzae Rd KW20 | P44803 | 58.1% | Diamond |
| Penicillium crustosum | A0A481WNM5 | 41.8% | Diamond |
Genomic neighbors (locus context)
Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).
| Symbol | Type | Entrez |
|---|---|---|
| NQO2-AS1 | ncRNA | 105374888 |
| LINC01011 | ncRNA | 401232 |
| SERPINB9-AS1 | ncRNA | 101927730 |
| SERPINB6 | protein-coding | 5269 |
| SERPINB9 | protein-coding | 5272 |
Protein
Protein identifiers
Ribosyldihydronicotinamide dehydrogenase [quinone] — P16083 (reviewed: P16083)
Alternative names: NRH dehydrogenase [quinone] 2, NRH:quinone oxidoreductase 2, Quinone reductase 2
All UniProt accessions (5): A2A2U4, P16083, Q5TD05, Q5TD07, U3KQG7
UniProt curated annotations — full annotation on UniProt →
Function. The enzyme apparently serves as a quinone reductase in connection with conjugation reactions of hydroquinones involved in detoxification pathways as well as in biosynthetic processes such as the vitamin K-dependent gamma-carboxylation of glutamate residues in prothrombin synthesis.
Subunit / interactions. Homodimer.
Subcellular location. Cytoplasm.
Activity regulation. Inhibited by melatonin, resveratrol and 5-hydroxytryptamine.
Cofactor. Binds 1 zinc ion per subunit.
Miscellaneous. Uses dihydronicotinamide riboside (NRH) rather than NAD(P)H as an electron donor.
Similarity. Belongs to the NAD(P)H dehydrogenase (quinone) family.
RefSeq proteins (4): NP_000895, NP_001277150, NP_001277151, NP_001305869 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR003680 | Flavodoxin_fold | Domain |
| IPR029039 | Flavoprotein-like_sf | Homologous_superfamily |
| IPR051545 | NAD(P)H_dehydrogenase_qn | Family |
Pfam: PF02525
Enzyme classification (BRENDA)
- EC 1.10.5.1 — ribosyldihydronicotinamide dehydrogenase (quinone) (BRENDA: 7 organisms, 82 substrates, 281 inhibitors, 35 Km, 9 kcat entries)
Substrate kinetics (BRENDA)
19 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| MENADIONE | 0.0016–0.0252 | 7 |
| N-BENZYL DIHYDRONICOTINAMIDE | 0.0113–0.0602 | 5 |
| DIHYDROBENZYLNICOTINAMIDE | 0.02–0.0608 | 4 |
| 2,6-DICHLOROPHENOLINDOPHENOL | 0.007–0.019 | 3 |
| 17BETA-17-HYDROXYESTR-1(10)-ENE-3,4-DIONE | 0.0008 | 1 |
| 3-(4,5-DIMETHYLTHIAZAOL-2-YL)-2,5-DIPHENYLTETRAZ | 0.012 | 1 |
| 5-(AZIRIDIN-1-YL)-2,4-DINITROBENZAMIDE | 0.061 | 1 |
| CB 1954 | 0.26 | 1 |
| COENZYME Q0 | 0.0137 | 1 |
| COENZYME Q1 | 0.0517 | 1 |
| COENZYME Q2 | 0.0387 | 1 |
| DIHYDRONICOTINAMIDE RIBOSIDE | 0.028 | 1 |
| ESTRADIOL-3,4-QUINONE | — | 1 |
| MENADIONE/3-(4,5-DIMETHYLTHIAZAOL-2-YL)-2,5-DIPH | 0.0023 | 1 |
| METHYL RED | 0.0047 | 1 |
Catalyzed reactions (Rhea)
- 1-(beta-D-ribofuranosyl)-1,4-dihydronicotinamide + a quinone + H(+) = beta-nicotinamide D-riboside + a quinol (RHEA:12364)
UniProt features (49 total): helix 13, binding site 11, strand 9, turn 6, sequence variant 5, modified residue 2, chain 1, mutagenesis site 1, sequence conflict 1
Structure
Experimental structures (PDB)
showing 30 of 68 structures by resolution:
| PDB | Title | Method | Resolution (Å) |
|---|---|---|---|
| 4FGL | Reduced quinone reductase 2 in complex with chloroquine | X-RAY DIFFRACTION | 1.2 |
| 4FGJ | Oxidized quinone reductase 2 in complex with primaquine | X-RAY DIFFRACTION | 1.35 |
| 4QOD | The value crystal structure of apo quinone reductase 2 at 1.35A | X-RAY DIFFRACTION | 1.35 |
| 4QOG | Crystal structure of fad quinone reductase 2 in complex with melatonin at 1.4A | X-RAY DIFFRACTION | 1.4 |
| 5LBY | Structure of the human quinone reductase 2 (NQO2) in complex with crenolanib | X-RAY DIFFRACTION | 1.4 |
| 5LBZ | Structure of the human quinone reductase 2 (NQO2) in complex with pacritinib | X-RAY DIFFRACTION | 1.4 |
| 4FGK | Oxidized quinone reductase 2 in complex with chloroquine | X-RAY DIFFRACTION | 1.4 |
| 3TEM | Quinone Oxidoreductase (NQ02) bound to the imidazoacridin-6-one 6a1 | X-RAY DIFFRACTION | 1.45 |
| 4QOE | The value ‘crystal structure of fad quinone reductase 2 at 1.45A | X-RAY DIFFRACTION | 1.45 |
| 4U7H | Oxidized quinone reductase 2 in complex with CK2 inhibitor DMAT | X-RAY DIFFRACTION | 1.48 |
| 1SG0 | Crystal structure analysis of QR2 in complex with resveratrol | X-RAY DIFFRACTION | 1.5 |
| 1XI2 | Quinone Reductase 2 in Complex with Cancer Prodrug CB1954 | X-RAY DIFFRACTION | 1.5 |
| 2QWX | Crystal Structure of Quinone Reductase II | X-RAY DIFFRACTION | 1.5 |
| 3UXE | Design, Synthesis and Biological Evaluation of Potent Quinoline and Pyrroloquinoline … | X-RAY DIFFRACTION | 1.5 |
| 4XDG | Crystal Structure of Quinone Reductase II in complex with … | X-RAY DIFFRACTION | 1.5 |
| 3UXH | Design, Synthesis and Biological Evaluation of Potetent Quinoline and Pyrroloquinoline … | X-RAY DIFFRACTION | 1.53 |
| 4QOF | Crystal structure of fmn quinone reductase 2 AT 1.55A | X-RAY DIFFRACTION | 1.55 |
| 4QOI | Crystal structure of FMN quinone reductase 2 in complex with melatonin at 1.55A | X-RAY DIFFRACTION | 1.55 |
| 3NFR | Casimiroin analog inhibitor of quinone reductase 2 | X-RAY DIFFRACTION | 1.57 |
| 3NHL | X-ray Crystallographic Structure Activity Relationship (SAR) of Casimiroin and its … | X-RAY DIFFRACTION | 1.57 |
| 2QX8 | Crystal Structure of Quinone Reductase II | X-RAY DIFFRACTION | 1.6 |
| 3O2N | X-ray Crystallographic Structure Activity Relationship (SAR) of Casimiroin and its … | X-RAY DIFFRACTION | 1.6 |
| 4QOH | Crystal structure of fad quinone reductase 2 in complex with resveratrol at 1.6A | X-RAY DIFFRACTION | 1.6 |
| 2QX4 | Crystal Structure of Quinone Reductase II | X-RAY DIFFRACTION | 1.65 |
| 3NHW | X-ray Crystallographic Structure Activity Relationship (SAR) of Casimiroin and its … | X-RAY DIFFRACTION | 1.65 |
| 5LBU | Structure of the human quinone reductase 2 (NQO2) in complex with to CL097 | X-RAY DIFFRACTION | 1.65 |
| 3NHP | X-ray Crystallographic Structure Activity Relationship (SAR) of Casimiroin and its … | X-RAY DIFFRACTION | 1.7 |
| 3TE7 | Quinone Oxidoreductase (NQ02) bound to the imidazoacridin-6-one 5a1 | X-RAY DIFFRACTION | 1.7 |
| 2QX6 | Crystal Structure of Quinone Reductase II | X-RAY DIFFRACTION | 1.75 |
| 3FW1 | Quinone Reductase 2 | X-RAY DIFFRACTION | 1.75 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P16083-F1 | 98.17 | 0.99 |
Human Protein Atlas
Protein class: Enzymes, ENZYME proteins, Oxidoreductases, Metabolic proteins, Predicted intracellular proteins, Plasma proteins, Human disease related genes
Protein evidence: Evidence at protein level
Subcellular location (HPA, imaging): cytosol; nucleoplasm
Antibody reliability (HPA): IH enhanced · IF supported
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Ligand- & substrate-binding residues (11)
| Position | Role |
|---|---|
| 12 | FAD |
| 201 | FAD |
| 223 | Zn(2+) |
| 18–21 | FAD |
| 104–107 | FAD |
| 127–129 | substrate |
| 148–151 | FAD |
| 156 | FAD |
| 174 | Zn(2+) |
| 178 | Zn(2+) |
| 194 | FAD |
Post-translational modifications (2)
| Type | Positions |
|---|---|
| Phosphoserine | 80, 197 |
Mutagenesis-validated functional residues (1)
| Position | Phenotype |
|---|---|
| 162 | loss of activity toward cb1954, no effect toward menadione. |
Function
Pathways and Gene Ontology
Reactome pathways
1 curated (TAS) of 3; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).
3 pathways:
| ID | Pathway | Evidence |
|---|---|---|
| R-HSA-211945 | Phase I - Functionalization of compounds | curated |
| R-HSA-211859 | Biological oxidations | — |
| R-HSA-1430728 | Metabolism | — |
MSigDB gene sets: 168 (showing top):
GSE18804_SPLEEN_MACROPHAGE_VS_TUMORAL_MACROPHAGE_DN, MODULE_93, REACTOME_BIOLOGICAL_OXIDATIONS, GOBP_KETONE_METABOLIC_PROCESS, chr6p25, CAIRO_HEPATOBLASTOMA_DN, GOBP_SMALL_MOLECULE_CATABOLIC_PROCESS, FLECHNER_BIOPSY_KIDNEY_TRANSPLANT_REJECTED_VS_OK_DN, GOMF_OXIDOREDUCTASE_ACTIVITY_ACTING_ON_NAD_P_H, KAAB_FAILED_HEART_VENTRICLE_DN, ACEVEDO_LIVER_CANCER_UP, GCM_BECN1, GRADE_COLON_AND_RECTAL_CANCER_UP, GOBP_QUINONE_METABOLIC_PROCESS, MARSON_BOUND_BY_FOXP3_UNSTIMULATED
GO Biological Process (1): quinone catabolic process (GO:1901662)
GO Molecular Function (12): dihydronicotinamide riboside quinone reductase activity (GO:0001512), NAD(P)H dehydrogenase (quinone) activity (GO:0003955), zinc ion binding (GO:0008270), electron transfer activity (GO:0009055), oxidoreductase activity (GO:0016491), oxidoreductase activity, acting on other nitrogenous compounds as donors (GO:0016661), chloride ion binding (GO:0031404), protein homodimerization activity (GO:0042803), FAD binding (GO:0071949), melatonin binding (GO:1904408), protein binding (GO:0005515), metal ion binding (GO:0046872)
GO Cellular Component (3): cytosol (GO:0005829), extracellular exosome (GO:0070062), cytoplasm (GO:0005737)
Reactome top-level categories
2 top-level categories:
| Category | Pathways |
|---|---|
| Biological oxidations | 1 |
| Metabolism | 1 |
GO top-level categories
18 GO namespaces:
| Category | Terms |
|---|---|
| binding | 2 |
| cellular anatomical structure | 2 |
| ketone catabolic process | 1 |
| quinone metabolic process | 1 |
| oxidoreductase activity, acting on diphenols and related substances as donors | 1 |
| oxidoreductase activity, acting on NAD(P)H, quinone or similar compound as acceptor | 1 |
| transition metal ion binding | 1 |
| molecular_function | 1 |
| catalytic activity | 1 |
| oxidoreductase activity | 1 |
| anion binding | 1 |
| identical protein binding | 1 |
| protein dimerization activity | 1 |
| flavin adenine dinucleotide binding | 1 |
| cation binding | 1 |
| cytoplasm | 1 |
| extracellular vesicle | 1 |
| intracellular anatomical structure | 1 |
Experimentally-supported GO annotations
GO terms backed by direct experimental evidence (ECO experimental codes) — 12 of 17 annotations. The rest are phylogenetic / computational / electronic (IEA).
12 experimentally-supported GO terms:
| GO term | NS | Evidence |
|---|---|---|
| quinone catabolic process | BP | direct assay |
| cytosol | CC | direct assay |
| extracellular exosome | CC | high-throughput assay |
| FAD binding | MF | direct assay |
| chloride ion binding | MF | direct assay |
| dihydronicotinamide riboside quinone reductase activity | MF | direct assay |
| electron transfer activity | MF | direct assay |
| melatonin binding | MF | direct assay |
| oxidoreductase activity | MF | direct assay |
| oxidoreductase activity, acting on other nitrogenous compounds as donors | MF | direct assay |
| protein homodimerization activity | MF | physical interaction |
| zinc ion binding | MF | direct assay |
Protein interactions and networks
STRING
showing 15 of 658 interactions by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| NQO2 | CRYZ | Q08257 | 581 |
| NQO2 | COMT | P21964 | 514 |
| NQO2 | ARHGEF5 | Q12774 | 490 |
| NQO2 | PALB2 | Q86YC2 | 484 |
| NQO2 | GPR50 | Q13585 | 444 |
| NQO2 | ASMT | P46597 | 442 |
| NQO2 | CYP19A1 | P11511 | 437 |
| NQO2 | AANAT | Q16613 | 429 |
| NQO2 | TCIM | Q9NR00 | 428 |
| NQO2 | TXNDC17 | Q9BRA2 | 423 |
| NQO2 | MTNR1A | P48039 | 409 |
| NQO2 | GSR | P00390 | 407 |
| NQO2 | GCLC | P48506 | 406 |
| NQO2 | LSM1 | O15116 | 390 |
| NQO2 | ADGRB3 | O60242 | 390 |
IntAct
Human interaction partners of NQO2 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).
11 partners by confidence:
| Partner | Interaction type | MIscore | Records |
|---|---|---|---|
| GORASP2 | physical association | 0.740 | 5 |
| LRRC7 | physical association | 0.720 | 6 |
| DDIT4L | physical association | 0.560 | 3 |
| EFHC1 | physical association | 0.560 | 3 |
| SPG21 | physical association | 0.560 | 3 |
| HSCB | association | 0.550 | 4 |
| DGCR6 | physical association | 0.370 | 1 |
| PA | physical association | 0.370 | 1 |
| RHOB | physical association | 0.370 | 1 |
| NSF | association | 0.350 | 1 |
| RELB | physical association | 0.000 | 1 |
BioGRID (34 interactions; top human partners by supporting records): GORASP2 (Two-hybrid; 2 records), LRRC7 (Two-hybrid; 2 records), CENPF (Co-fractionation), CHUK (Affinity Capture-MS), COPS5 (Affinity Capture-MS), CRAT (Co-fractionation), CTBP2 (Affinity Capture-MS), DDIT4L (Two-hybrid), DGCR6 (Two-hybrid), EFHC1 (Two-hybrid), ELMO2 (Co-fractionation), HNRNPL (Affinity Capture-RNA), IGF2BP3 (Affinity Capture-RNA), IKBKB (Affinity Capture-MS), IL32 (Two-hybrid)
Protein complexes (CORUM) (1)
Experimentally-characterized complexes this protein is a subunit of (★ = the complex contains a known drug target).
1 complexes by size:
| Complex | Subunits | Members |
|---|---|---|
| ★ AKT1-NQO2 complex | 2 | AKT1, NQO2 |
Disease & clinical
Genetic variants
Variant evidence for NQO2: 48 ClinVar records (0 pathogenic / likely pathogenic); 1 PharmGKB clinical annotation; 3 GWAS associations.
ClinVar
48 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 33 |
| Likely benign | 2 |
| Benign | 2 |
SpliceAI
Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 28 predictions of 808):
| Position(s) | Effect | Δscore | Sites |
|---|---|---|---|
| 6:3000086 | donor_loss | 1.0000 | |
| 6:3016882–3016883 | acceptor_loss | 1.0000 | 2 |
| 6:3000067 | donor_gain | 0.9900 | |
| 6:3000086–3000087 | donor_loss | 0.9900 | 4 |
| 6:3004595 | donor_gain | 0.9900 | |
| 6:3006466–3006467 | acceptor_loss | 0.9900 | 6 |
| 6:3006557 | donor_gain | 0.9900 | |
| 6:3006560–3006561 | donor_loss | 0.9900 | 5 |
| 6:3010190–3010191 | donor_loss | 0.9900 | 6 |
| 6:3010194 | donor_loss | 0.9900 |
HPA cancer prognostics
RNA cancer specificity: Low cancer specificity
Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.
4 prognostic cancer types:
| Cancer | Prognostic | p-value |
|---|---|---|
| Kidney Renal Papillary Cell Carcinoma (TCGA) | favorable | 0.000359 |
| Cervical Squamous Cell Carcinoma and Endocervical Adenocarcinoma (TCGA) | favorable | 0.000483 |
| Breast Invasive Carcinoma (TCGA) | unfavorable | 0.000687 |
| Kidney Chromophobe (TCGA) | unfavorable | 0.000941 |
Disease associations
OMIM: gene MIM:160998 | disease phenotypes:
HPO phenotypes
3 phenotypes (HPO-id order):
| HPO | Term |
|---|---|
| HP:0000006 | Autosomal dominant inheritance |
| HP:0001442 | Typified by somatic mosaicism |
| HP:0003002 | Breast carcinoma |
GWAS associations
3 associations:
| Study | Trait | p-value |
|---|---|---|
| GCST009733_90 | Urinary metabolite levels in chronic kidney disease | 3e-88 |
| GCST006585_673 | Blood protein levels | 4e-64 |
| GCST009733_118 | Urinary metabolite levels in chronic kidney disease | 1e-29 |
EFO canonical traits (from GWAS)
1 canonical traits:
| EFO ID | Trait name |
|---|---|
| EFO:0005116 | urinary metabolite measurement |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL3959 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 465,096 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
45 molecules by phase:
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL3187723 | BINIMETINIB | 4 | 7,655 |
| CHEMBL76 | CHLOROQUINE | 4 | 59,347 |
| CHEMBL1287853 | FEDRATINIB | 4 | 3,770 |
| CHEMBL3301622 | GILTERITINIB | 4 | 2,542 |
| CHEMBL941 | IMATINIB | 4 | 113,105 |
| CHEMBL1289601 | LENVATINIB | 4 | 9,224 |
| CHEMBL45 | MELATONIN | 4 | 57,288 |
| CHEMBL255863 | NILOTINIB | 4 | 39,362 |
| CHEMBL3353410 | OSIMERTINIB | 4 | 9,448 |
| CHEMBL2035187 | PACRITINIB | 4 | 3,544 |
| CHEMBL2 | PRAZOSIN | 4 | 31,292 |
| CHEMBL506 | PRIMAQUINE | 4 | 10,353 |
| CHEMBL535 | SUNITINIB | 4 | 80,232 |
| CHEMBL3402762 | TEPOTINIB | 4 | 1,359 |
| CHEMBL3989868 | TUCATINIB | 4 | 3,355 |
| CHEMBL2105728 | CRENOLANIB | 3 | 2,278 |
| CHEMBL48361 | DABIGATRAN | 3 | 13,643 |
| CHEMBL522892 | DOVITINIB | 3 | 5,162 |
| CHEMBL38380 | FASUDIL | 3 | 12,137 |
| CHEMBL603469 | LESTAURTINIB | 3 | |
| CHEMBL1908391 | MASITINIB | 3 | |
| CHEMBL165 | RESVERATROL | 3 | |
| CHEMBL1241855 | RIGOSERTIB | 3 | |
| CHEMBL3426621 | RIPASUDIL | 3 | |
| CHEMBL3334567 | SAVOLITINIB | 3 | |
| CHEMBL43184 | AMINACRINE | 2 | |
| CHEMBL206834 | BAFETINIB | 2 | |
| CHEMBL3545215 | BMS-911543 | 2 | |
| CHEMBL338604 | C-1311 | 2 | |
| CHEMBL1614713 | CC-401 | 2 | |
| CHEMBL1822792 | MK-2461 | 2 | |
| CHEMBL1232461 | MOLIBRESIB | 2 | |
| CHEMBL3120215 | OSI-027 | 2 | |
| CHEMBL521851 | PICTILISIB | 2 | |
| CHEMBL83527 | PTEROSTILBENE | 2 | |
| CHEMBL2386889 | SCH-900776 | 2 | |
| CHEMBL514201 | TALMAPIMOD | 2 | |
| CHEMBL2140408 | AMG-900 | 1 | |
| CHEMBL3545360 | ASP-3026 | 1 | |
| CHEMBL482967 | CYC-116 | 1 | |
| CHEMBL2133806 | JNJ-38877605 | 1 | |
| CHEMBL1908397 | KW-2449 | 1 | |
| CHEMBL3286797 | PF-04418948 | 1 | |
| CHEMBL1236107 | SGX-523 | 1 | |
| CHEMBL3544932 | TAK-901 | 1 |
PharmGKB: 1 entry (CPIC guideline: no)
PharmGKB clinical annotations
1 annotations by evidence level (1 strongest → 4):
| Variant | Association | Level | Drugs | Phenotypes |
|---|---|---|---|---|
| rs1143684 | Efficacy | 3 | cyclophosphamide;doxorubicin | Breast Neoplasms |
PharmGKB variants
1 variants:
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs1143684 | NQO2 | 3 | 1.00 | 1 | cyclophosphamide;doxorubicin |
PharmGKB variant annotations
Per-publication pharmacogenomic findings for this gene (significant associations).
2 published findings:
| Variant | Drug(s) | Category | Finding | PMID |
|---|---|---|---|---|
| rs1143684 | cytarabine, idarubicin | Toxicity | Genotype CC is associated with increased risk of gastrointestinal toxicity when treated with cytarabine and idarubicin in people with Leukemia, Myeloid, Acute as compared to genotype TT. | PMID:33675324 |
| rs1143684 | cyclophosphamide, doxorubicin | Efficacy | Allele C is associated with worse prognosis (overall survival and progression-free survival) in patients who were ER-ve/PR-ve negative when treated with cyclophosphamide and doxorubicin in people with Breast Neoplasms as compared to allele T. | PMID:21946896 |
Binding affinities (BindingDB)
331 measured of 367 human assays (377 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| 2,2,2-Trifluoro-N-[2-(6-methoxy-2-phenyl-3H-inden-1-yl)-ethyl]-acetamide | KI | 0.00602 nM |
| 2,2,2-Trifluoro-N-[2-(6-methoxy-indan-1-yl)-ethyl]-acetamide | KI | 0.0123 nM |
| 2,2,2-Trifluoro-N-[2-(6-methoxy-indan-1-yl)-ethyl]-acetamide | KI | 0.0225 nM |
| N-[2-(6-Methoxy-3H-inden-1-yl)-ethyl]-propionamide | KI | 0.0231 nM |
| (S) N-[2-(6-Methoxy-indan-1-yl)-ethyl]-butyramide | KI | 0.0321 nM |
| 2,2,2-Trifluoro-N-[2-(6-methoxy-3H-inden-1-yl)-ethyl]-acetamide | KI | 0.0408 nM |
| (S) N-[2-(6-Methoxy-indan-1-yl)-ethyl]-propionamide | KI | 0.041 nM |
| 2,2,2-Trifluoro-N-[2-(7-methoxy-1,2,3,4-tetrahydro-naphthalen-1-yl)-ethyl]-acetamide | KI | 0.0469 nM |
| N-[2-(6-Methoxy-indan-1-yl)-ethyl]-butyramide | KI | 0.0553 nM |
| N-[2-(6-Methoxy-indan-1-yl)-ethyl]-propionamide | KI | 0.0728 nM |
| (S) N-[2-(6-Methoxy-indan-1-yl)-ethyl]-acetamide | KI | 0.0733 nM |
| N-[2-(2-Iodo-5-methoxy-1-methyl-1H-indol-3-yl)-ethyl]-acetamide | KI | 0.08 nM |
| 2,2,2-Trifluoro-N-[2-(6-methoxy-5-methyl-indan-1-yl)-ethyl]-acetamide | KI | 0.0984 nM |
| N-[2-(6-Ethoxy-indan-1-yl)-ethyl]-propionamide | KI | 0.1 nM |
| N-[2-(6-Methoxy-indan-1-yl)-ethyl]-acetamide | KI | 0.131 nM |
| Melatonin,2-Chloro | KI | 0.2 nM |
| (E) N-[2-(6-Methoxy-indan-1-ylidene)-ethyl]-propionamide | KI | 0.208 nM |
| N-[2-(6-Methoxy-indan-1-yl)-ethyl]-isobutyramide | KI | 0.25 nM |
| N-[2-(2-Iodo-5-methoxy-6-nitro-1H-indol-3-yl)-ethyl]-acetamide | KI | 0.3 nM |
| CHEMBL511675 | IC50 | 0.302 nM |
| N-[2-(6-Propoxy-indan-1-yl)-ethyl]-propionamide | KI | 0.425 nM |
| 2,2,2-Trifluoro-N-[3-(6-methoxy-indan-1-yl)-propyl]-acetamide | KI | 0.526 nM |
| N-[2-(5-Methoxy-benzofuran-3-yl)-ethyl]-acetamide | IC50 | 0.6 nM |
| N-(2-(7-(methylthio)naphthalen-1-yl)ethyl)acetamide | IC50 | 0.875 nM |
| (Z) N-[2-(6-Methoxy-indan-1-ylidene)-ethyl]-propionamide | KI | 0.927 nM |
| Melatonin,2-Iodo | IC50 | 1 nM |
| N-[2-(2-Iodo-5-methoxy-1-methyl-6-nitro-1H-indol-3-yl)-ethyl]-acetamide | KI | 1.1 nM |
| Pentanoic acid [2-(6-methoxy-indan-1-yl)-ethyl]-amide | KI | 1.3 nM |
| N-[2-(6-Isopropoxy-indan-1-yl)-ethyl]-propionamide | KI | 1.5 nM |
| 2,2,2-Trifluoro-N-[2-(6-methoxy-2-phenyl-indan-1-yl)-ethyl]-acetamide | KI | 1.6 nM |
| 2,2,2-Trifluoro-N-[2-(3-methoxy-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-yl)-ethyl]-acetamide | KI | 1.7 nM |
| N-[2-(5-Methoxy-1-methyl-1H-indol-3-yl)-ethyl]-acetamide | KI | 2.2 nM |
| CHEMBL37703 | IC50 | 2.51 nM |
| CHEMBL6074469 | IC50 | 3 nM |
| CHEMBL457126 | IC50 | 3.02 nM |
| N-[2-(5,6-Dimethoxy-indan-1-yl)-ethyl]-acetamide | KI | 4.1 nM |
| CHEMBL1945729 | IC50 | 4.1 nM |
| CHEMBL6082944 | IC50 | 5 nM |
| NSC-660841 | IC50 | 6 nM |
| (R) 2,2,2-Trifluoro-N-[2-(6-methoxy-indan-1-yl)-ethyl]-acetamide | KI | 6.4 nM |
| N-[2-(2-Benzyl-6-methoxy-3H-inden-1-yl)-ethyl]-2,2,2-trifluoro-acetamide | KI | 6.8 nM |
| CHEMBL465378 | IC50 | 7.76 nM |
| 5-(2-Diethylamino-ethylamino)-8-methoxy-1-methyl-2,10b-diaza-aceanthrylen-6-one(2.0MHCl) | IC50 | 9 nM |
| CHEMBL4514167 | IC50 | 10 nM |
| CHEMBL457541 | IC50 | 11 nM |
| (R) N-[2-(6-Methoxy-indan-1-yl)-ethyl]-acetamide | KI | 11 nM |
| 2,2,2-Trifluoro-N-(2-indan-1-yl-ethyl)-acetamide | KI | 12 nM |
| CHEMBL455339 | IC50 | 12 nM |
| CHEMBL1836819 | IC50 | 14 nM |
| CHEMBL495399 | IC50 | 14.1 nM |
ChEMBL bioactivities
403 potent at pChembl≥5 of 463 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 10.06 | Ki | 0.088 | nM | CHEMBL300056 |
| 10.05 | IC50 | 0.08913 | nM | CHEMBL300056 |
| 9.89 | Ki | 0.13 | nM | CHEMBL300728 |
| 9.89 | IC50 | 0.1288 | nM | CHEMBL300728 |
| 9.74 | Ki | 0.18 | nM | CHEMBL52559 |
| 9.70 | IC50 | 0.1995 | nM | CHEMBL52559 |
| 9.52 | IC50 | 0.302 | nM | CHEMBL511675 |
| 9.52 | Ki | 0.3 | nM | CHEMBL300728 |
| 9.51 | Ki | 0.31 | nM | CHEMBL53622 |
| 9.51 | IC50 | 0.309 | nM | CHEMBL53622 |
| 9.41 | IC50 | 0.39 | nM | CHEMBL1770214 |
| 8.96 | Ki | 1.1 | nM | CHEMBL300195 |
| 8.92 | IC50 | 1.202 | nM | CHEMBL300195 |
| 8.57 | IC50 | 2.7 | nM | CHEMBL504585 |
| 8.55 | Ki | 2.8 | nM | CHEMBL33700 |
| 8.55 | IC50 | 2.818 | nM | CHEMBL33700 |
| 8.52 | IC50 | 3.02 | nM | CHEMBL457126 |
| 8.52 | IC50 | 3 | nM | CHEMBL6074469 |
| 8.40 | Kd | 4 | nM | PACRITINIB |
| 8.39 | IC50 | 4.1 | nM | CHEMBL1945729 |
| 8.31 | IC50 | 4.9 | nM | CHEMBL1738752 |
| 8.30 | IC50 | 5 | nM | CHEMBL6082944 |
| 8.22 | IC50 | 6 | nM | CHEMBL8602 |
| 8.21 | Ki | 6.1 | nM | CHEMBL55084 |
| 8.19 | Ki | 6.5 | nM | IODOMELATONIN |
| 8.11 | IC50 | 7.762 | nM | CHEMBL465378 |
| 8.11 | IC50 | 7.7 | nM | CHEMBL6078562 |
| 8.11 | IC50 | 7.8 | nM | PRAZOSIN |
| 8.05 | IC50 | 9 | nM | CHEMBL124254 |
| 8.04 | Ki | 9.09 | nM | CHEMBL134447 |
| 8.04 | IC50 | 9.12 | nM | CHEMBL457992 |
| 8.04 | IC50 | 9.1 | nM | CHEMBL457992 |
| 8.00 | IC50 | 10 | nM | CHEMBL4514167 |
| 7.96 | IC50 | 10.96 | nM | CHEMBL457541 |
| 7.96 | IC50 | 10.96 | nM | CHEMBL493424 |
| 7.92 | IC50 | 12.02 | nM | CHEMBL455339 |
| 7.89 | IC50 | 13 | nM | CHEMBL1967497 |
| 7.85 | IC50 | 14.13 | nM | CHEMBL457539 |
| 7.85 | IC50 | 14.13 | nM | CHEMBL495399 |
| 7.85 | IC50 | 14 | nM | CHEMBL1836819 |
| 7.84 | IC50 | 14.5 | nM | CHEMBL3770674 |
| 7.82 | IC50 | 15.2 | nM | CHEMBL3770366 |
| 7.82 | IC50 | 15 | nM | CHEMBL4435240 |
| 7.80 | IC50 | 15.85 | nM | CHEMBL446329 |
| 7.80 | IC50 | 16 | nM | CHEMBL125082 |
| 7.77 | IC50 | 17 | nM | CHEMBL8150 |
| 7.75 | IC50 | 18 | nM | CHEMBL1237241 |
| 7.75 | IC50 | 18 | nM | CHEMBL456727 |
| 7.74 | IC50 | 18.2 | nM | CHEMBL456727 |
| 7.74 | IC50 | 18.2 | nM | CHEMBL494566 |
PubChem BioAssay actives
414 with measured affinity, of 933 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| N-[2-(2-iodo-5-methoxy-1-methyl-4-nitroindol-3-yl)ethyl]acetamide | 107724: Inhibition of 2-[125I]iodomelatonin binding to Melatonin receptor 3 (MT3) of Syrian hamster brain membrane | ki | 0.0001 | uM |
| N-[2-(2-iodo-5-methoxy-1-methylindol-3-yl)ethyl]acetamide | 107724: Inhibition of 2-[125I]iodomelatonin binding to Melatonin receptor 3 (MT3) of Syrian hamster brain membrane | ki | 0.0001 | uM |
| N-[2-(2-iodo-5-methoxy-4-nitro-1H-indol-3-yl)ethyl]acetamide | 107724: Inhibition of 2-[125I]iodomelatonin binding to Melatonin receptor 3 (MT3) of Syrian hamster brain membrane | ki | 0.0002 | uM |
| methyl N-[3-(2-acetamidoethyl)-2-iodo-1H-indol-5-yl]carbamate | 396398: Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells | ic50 | 0.0003 | uM |
| N-[2-(5-methoxy-1-methyl-4-nitroindol-3-yl)ethyl]acetamide | 107724: Inhibition of 2-[125I]iodomelatonin binding to Melatonin receptor 3 (MT3) of Syrian hamster brain membrane | ki | 0.0003 | uM |
| methyl N-[8-(2-acetamidoethyl)naphthalen-2-yl]carbamate | 594258: Binding affinity to human low affinity melatonin (MT3) site of quinone reductase 2 | ic50 | 0.0004 | uM |
| N-[2-(5-methoxy-4-nitro-1H-indol-3-yl)ethyl]acetamide | 107724: Inhibition of 2-[125I]iodomelatonin binding to Melatonin receptor 3 (MT3) of Syrian hamster brain membrane | ki | 0.0011 | uM |
| methyl N-[3-(2-acetamidoethyl)-1H-indol-5-yl]carbamate | 594262: Binding affinity to low affinity melatonin (MT3) site of quinone reductase 2 | ic50 | 0.0027 | uM |
| N-[2-(5-methoxy-1-methylindol-3-yl)ethyl]acetamide | 107724: Inhibition of 2-[125I]iodomelatonin binding to Melatonin receptor 3 (MT3) of Syrian hamster brain membrane | ki | 0.0028 | uM |
| 8-methyl-2-(4-methyl-3-piperazin-1-ylsulfonylphenyl)imidazo[1,2-a]pyridine | 2203527: Inhibition of QR2 (unknown origin) | ic50 | 0.0030 | uM |
| ethyl 3-(2-acetamidoethyl)-5-methoxy-1H-indole-2-carboxylate | 396398: Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells | ic50 | 0.0030 | uM |
| Pacritinib | 1425093: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0040 | uM |
| 11-amino-10-chloro-2-methyl-9-(methylamino)-3-oxo-2,7-diazatricyclo[6.3.1.04,12]dodeca-1(11),4,6,8(12),9-pentaene-6-carboxamide | 643961: Inhibition of human quinone reductase 2 using NMeH as substrate by MTT assay | ic50 | 0.0041 | uM |
| N-[2-[7-(methylsulfamoyl)naphthalen-1-yl]ethyl]acetamide | 594258: Binding affinity to human low affinity melatonin (MT3) site of quinone reductase 2 | ic50 | 0.0049 | uM |
| N-[2-(5-methoxy-1,6,11-triazatetracyclo[7.7.0.02,7.010,15]hexadeca-2(7),3,5,8,10(15),11,13-heptaen-8-yl)ethyl]furan-2-carboxamide | 2203526: Inhibition of human QR2 expressed in Escherichia coli preincubated with BNAH or NRH followed by menadione addition by FLUOstar plate reader assay | ic50 | 0.0050 | uM |
| 10-[2-(diethylamino)ethylamino]-8-hydroxy-4,5-dimethoxy-1,14-diazatetracyclo[7.6.1.02,7.013,16]hexadeca-2,4,7,9,11,13(16),14-heptaen-6-one | 479979: Inhibition of human recombinant NQO2 assessed as reduction of DCPIP by spectrophotometry | ic50 | 0.0060 | uM |
| N-[2-(2-iodo-5-methoxy-1-methyl-6-nitroindol-3-yl)ethyl]acetamide | 107724: Inhibition of 2-[125I]iodomelatonin binding to Melatonin receptor 3 (MT3) of Syrian hamster brain membrane | ki | 0.0061 | uM |
| N-[2-(2-iodo-5-methoxy-1H-indol-3-yl)ethyl]acetamide | 107724: Inhibition of 2-[125I]iodomelatonin binding to Melatonin receptor 3 (MT3) of Syrian hamster brain membrane | ki | 0.0065 | uM |
| 5-methoxy-3-(5-methoxy-2,3-dihydro-1H-indol-2-yl)-1H-indole | 2203497: Displacement of 2-[125I]iodomelatonin from QR2 (unknown origin) extracted from hamster brain membrane incubated for 30 mins relative to control | ic50 | 0.0077 | uM |
| N-[2-(7-hydroxynaphthalen-1-yl)ethyl]but-3-enamide | 396398: Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells | ic50 | 0.0078 | uM |
| Prazosin | 594262: Binding affinity to low affinity melatonin (MT3) site of quinone reductase 2 | ic50 | 0.0078 | uM |
| 10-[2-(diethylamino)ethylamino]-5-methoxy-15-methyl-1,14-diazatetracyclo[7.6.1.02,7.013,16]hexadeca-2(7),3,5,9,11,13(16),14-heptaen-8-one | 479979: Inhibition of human recombinant NQO2 assessed as reduction of DCPIP by spectrophotometry | ic50 | 0.0090 | uM |
| 2,2,2-trifluoro-N-[2-(6-methoxy-3H-inden-1-yl)ethyl]acetamide | 107722: Ability to inhibit 2-[125I]iodomelatonin specific binding to melatonin receptor 3 (MT3) of Syrian hamster brain. | ki | 0.0091 | uM |
| N-[2-[7-(methylsulfamoyl)naphthalen-1-yl]ethyl]furan-2-carboxamide | 396398: Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells | ic50 | 0.0091 | uM |
| 6-methoxy-2-methyl-N-[(E)-pyridin-3-ylmethylideneamino]quinolin-4-amine | 1566052: Inhibition of recombinant human NQO2 expressed in Escherichia coli using DCPIP as substrate by spectrophotometry | ic50 | 0.0100 | uM |
| N-[2-(7-hydroxynaphthalen-1-yl)ethyl]furan-2-carboxamide | 396398: Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells | ic50 | 0.0110 | uM |
| methyl N-[3-[2-(but-3-enoylamino)ethyl]-1-benzofuran-5-yl]carbamate | 396398: Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells | ic50 | 0.0110 | uM |
| 8-(acetamidomethyl)-N-methylnaphthalene-2-carboxamide | 396398: Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells | ic50 | 0.0120 | uM |
| 2-methoxy-6-[(E)-[(6-methoxy-2-methylquinolin-4-yl)hydrazinylidene]methyl]phenol | 1566052: Inhibition of recombinant human NQO2 expressed in Escherichia coli using DCPIP as substrate by spectrophotometry | ic50 | 0.0130 | uM |
| 2-[(5-methoxy-8-oxo-1,14-diazatetracyclo[7.6.1.02,7.013,16]hexadeca-2(7),3,5,9,11,13(16),14-heptaen-10-yl)amino]-N,N-dimethylethanamine oxide | 621612: Inhibition of human recombinant NQO2 assessed as reduction of DCPIP by spectrophotometry | ic50 | 0.0140 | uM |
| methyl 3-(2-acetamidoethyl)-1-benzofuran-5-carboxylate | 396398: Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells | ic50 | 0.0141 | uM |
| 3-[2-(7-methoxynaphthalen-1-yl)ethyl]-1,3-oxazolidin-2-one | 396398: Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells | ic50 | 0.0141 | uM |
| acetic acid;4-[5-(3-nitrophenyl)furan-2-yl]benzenecarboximidamide | 1281396: Inhibition of human recombinant NQO2 using DCPIPas substrate and NRH as cofactor measured for 1 min by spectrophotometry in the absence of BSA | ic50 | 0.0145 | uM |
| 6-methoxy-2-methyl-N-[(E)-2-phenylethylideneamino]quinolin-4-amine | 1566052: Inhibition of recombinant human NQO2 expressed in Escherichia coli using DCPIP as substrate by spectrophotometry | ic50 | 0.0150 | uM |
| acetic acid;4-[5-(4-nitrophenyl)furan-2-yl]benzenecarboximidamide | 1281396: Inhibition of human recombinant NQO2 using DCPIPas substrate and NRH as cofactor measured for 1 min by spectrophotometry in the absence of BSA | ic50 | 0.0152 | uM |
| methyl N-[3-(2-acetamidoethyl)-1-benzofuran-5-yl]carbamate | 396398: Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells | ic50 | 0.0158 | uM |
| 10-[2-(diethylamino)ethylamino]-5-hydroxy-15-methyl-1,14-diazatetracyclo[7.6.1.02,7.013,16]hexadeca-2(7),3,5,9,11,13(16),14-heptaen-8-one | 479979: Inhibition of human recombinant NQO2 assessed as reduction of DCPIP by spectrophotometry | ic50 | 0.0160 | uM |
| 10-[2-(diethylamino)ethylamino]-3,6-dimethoxy-1,14-diazatetracyclo[7.6.1.02,7.013,16]hexadeca-2,4,6,9,11,13(16),14-heptaen-8-one | 479979: Inhibition of human recombinant NQO2 assessed as reduction of DCPIP by spectrophotometry | ic50 | 0.0170 | uM |
| 6-methoxy-2-methyl-N-[(E)-(5-nitrofuran-2-yl)methylideneamino]quinolin-4-amine | 1566052: Inhibition of recombinant human NQO2 expressed in Escherichia coli using DCPIP as substrate by spectrophotometry | ic50 | 0.0180 | uM |
| N-[2-(7-methylsulfanylnaphthalen-1-yl)ethyl]acetamide | 594258: Binding affinity to human low affinity melatonin (MT3) site of quinone reductase 2 | ic50 | 0.0180 | uM |
| 4,5,6,7-tetrabromo-1H-benzimidazole | 1801064: Fluorescence Titration Assay from Article 10.1021/bi500959t: “Quinone reductase 2 is an adventitious target of protein kinase CK2 inhibitors TBBz (TBI) and DMAT.” | kd | 0.0181 | uM |
| methyl 3-[2-(cyclopentanecarbonylamino)ethyl]-1-benzofuran-5-carboxylate | 396398: Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells | ic50 | 0.0182 | uM |
| N-[2-(7-methylsulfonylnaphthalen-1-yl)ethyl]acetamide | 396398: Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells | ic50 | 0.0209 | uM |
| methyl N-[3-[2-(2-methylpropanoylamino)ethyl]-1-benzofuran-5-yl]carbamate | 396398: Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells | ic50 | 0.0229 | uM |
| methyl N-[8-[(cyclopropanecarbonylamino)methyl]naphthalen-2-yl]carbamate | 396398: Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells | ic50 | 0.0240 | uM |
| acetic acid;4-[5-(4-bromophenyl)furan-2-yl]benzenecarboximidamide | 1281396: Inhibition of human recombinant NQO2 using DCPIPas substrate and NRH as cofactor measured for 1 min by spectrophotometry in the absence of BSA | ic50 | 0.0270 | uM |
| Melatonin | 107722: Ability to inhibit 2-[125I]iodomelatonin specific binding to melatonin receptor 3 (MT3) of Syrian hamster brain. | ki | 0.0276 | uM |
| N-(2-naphthalen-1-ylethyl)methanesulfonamide | 396398: Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells | ic50 | 0.0282 | uM |
| N-[2-(7-methoxynaphthalen-1-yl)ethyl]benzamide | 396398: Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells | ic50 | 0.0288 | uM |
| 10-[2-(diethylamino)ethylamino]-8-hydroxy-3-methoxy-1,14-diazatetracyclo[7.6.1.02,7.013,16]hexadeca-2,4,7,9,11,13(16),14-heptaen-6-one | 479979: Inhibition of human recombinant NQO2 assessed as reduction of DCPIP by spectrophotometry | ic50 | 0.0310 | uM |
CTD chemical–gene interactions
96 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Resveratrol | decreases expression, affects binding, increases oxidation, increases reduction, affects localization (+5 more) | 9 |
| Valproic Acid | increases expression, affects expression, decreases methylation, affects cotreatment | 8 |
| sodium arsenite | increases expression | 5 |
| Cyclosporine | affects cotreatment, increases expression, decreases expression | 4 |
| Benzo(a)pyrene | decreases methylation, increases expression, increases methylation | 3 |
| Clozapine | decreases reaction, increases reduction, increases activity, increases expression, affects response to substance | 3 |
| Quercetin | affects binding, decreases reaction, increases reduction, decreases expression | 3 |
| Tetrachlorodibenzodioxin | increases expression | 3 |
| bisphenol A | increases expression | 2 |
| trichostatin A | affects expression, increases expression | 2 |
| sulforaphane | increases expression | 2 |
| nicotinamide-beta-riboside | decreases reaction, increases oxidation, increases reduction | 2 |
| entinostat | increases expression, affects cotreatment | 2 |
| N-(2-(2-methoxy-6H-dipyrido(2,3-a-3,2-e)pyrrolizin-11-yl)ethyl)-2-furamide | decreases reaction, increases oxidation, increases reduction, increases activity, decreases activity | 2 |
| Panobinostat | affects cotreatment, increases expression | 2 |
| Estradiol | affects cotreatment, increases expression | 2 |
| Melatonin | affects activity, decreases reaction, increases oxidation, increases reduction | 2 |
| Phenylmercuric Acetate | affects cotreatment, increases expression | 2 |
| Smoke | decreases expression | 2 |
| Tobacco Smoke Pollution | increases expression | 2 |
| Zinc | affects cotreatment, increases expression, affects expression | 2 |
| 2,6-Dichloroindophenol | increases oxidation, increases reduction, decreases reaction | 2 |
| Aflatoxin B1 | affects expression, increases methylation | 2 |
| Vitamin K 3 | increases oxidation, decreases reaction, increases reduction | 2 |
| bisphenol F | increases expression | 1 |
| methylmercuric chloride | increases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| chrysoeriol | decreases reaction, increases oxidation, increases reduction | 1 |
| hesperetin | affects binding | 1 |
| beta-lapachone | increases expression | 1 |
ChEMBL screening assays
93 unique, capped per target: 93 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1016924 | Binding | Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells | A novel quantitative structure-activity relationship method to predict the affinities of MT3 melatonin binding site. — *Eur J Med Chem* |
Cellosaurus cell lines
7 cell lines: 6 cancer cell line, 1 transformed cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_D1PD | Abcam K-562 NQO2 KO | Cancer cell line | Female |
| CVCL_D2KZ | Abcam Raji NQO2 KO | Cancer cell line | Male |
| CVCL_D8RM | Ubigene HCT 116 NQO2 KO | Cancer cell line | Male |
| CVCL_E1KG | HyCyte HEK293T KO-hNQO2 | Transformed cell line | Female |
| CVCL_TA99 | HAP1 NQO2 (-) 1 | Cancer cell line | Male |
| CVCL_WQ16 | Abcam Jurkat NQO2 KO | Cancer cell line | Male |
| CVCL_XR07 | HAP1 NQO2 (-) 2 | Cancer cell line | Male |
Clinical trials (associated diseases)
Via MONDO — disease-level, not drug-specific.
showing 60 of 300 trials:
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00190697 | Phase 4 | COMPLETED | A Study of LY353381 (Arzoxifene) for Patients Who Benefitted From This Drug in Other Oncology Trials and Wished to Continue Treatment |
| NCT00277160 | Phase 4 | COMPLETED | A Study of Primary Prophylaxis With Neulasta (Pegfilgrastim) Versus Secondary Prophylaxis After Chemotherapy in Elderly Subjects (>/= 65 Years Old) With Cancer |
| NCT00727961 | Phase 4 | COMPLETED | A Study to Evaluate Efficacy and Tolerance of Caelyx in Patients With Epithelial Ovarian Cancer. (Study P04072)(COMPLETED) |
| NCT00740116 | Phase 4 | COMPLETED | Tranexamic Acid in Surgery of Advanced Ovarian Cancer |
| NCT00817479 | Phase 4 | COMPLETED | Tumor Gene Expression in Women With Ovarian Cancer |
| NCT01432015 | Phase 4 | COMPLETED | Fosaprepitant Versus Aprepitant in the Prevention of Chemotherapy Induced Nausea and Vomiting |
| NCT01706120 | Phase 4 | UNKNOWN | Study of Clinical and Biological Prognostic Factors in Patients With Ovarian Cancer Receiving Carboplatin +Paclitaxel With Bevacizumab |
| NCT01932125 | Phase 4 | COMPLETED | An Interventional Study of Avastin (Bevacizumab) in Patients With Advanced/Metastatic Epithelial Ovarian Cancer, Fallopian Tube Cancer or Primary Peritoneal Cancer |
| NCT01953107 | Phase 4 | COMPLETED | Oral Iron vs. Placebo in Newly Diagnosed Gynecologic Oncology Patients Who Are Surgical Candidates. |
| NCT02035345 | Phase 4 | TERMINATED | Slowed Carboplatin Infusion for Ovarian Cancer Patients Receiving Carboplatin Re-Treatment |
| NCT02243059 | Phase 4 | WITHDRAWN | Magnetic Resonance Imaging for Lymph Node Staging in Ovarian Cancer |
| NCT03164980 | Phase 4 | TERMINATED | QoL-Comparison Between Trabectedin/PLD and Pt-based Therapy in Patients With Pt-sensitive Recurrent Ovarian Cancer |
| NCT03384511 | Phase 4 | COMPLETED | The Use of 18F-ALF-NOTA-PRGD2 PET/CT Scan to Predict the Efficacy and Adverse Events of Apatinib in Malignancies. |
| NCT03543462 | Phase 4 | COMPLETED | Diaphragmatic Resection And Gynecological Ovarian Neoplasm |
| NCT03752216 | Phase 4 | COMPLETED | NIraparib and Quality of LifE is a Longitudinal Study Evaluating in Real Life the Tolerability of Niraparib. |
| NCT03858166 | Phase 4 | TERMINATED | Efficacy and Safety of PEG-rhG-CSF Secondary Prophylaxis vs. Therapeutic Administration in Patients With Ovarian Cancer |
| NCT04024254 | Phase 4 | COMPLETED | A Study of Serum Folate Levels in Patients Treated With Olaparib |
| NCT04330040 | Phase 4 | COMPLETED | Prospective Multicentre Phase-IV Clinical Trial of Olaparib in Indian Patients With Ovarian and Metastatic Breast Cancer |
| NCT04352439 | Phase 4 | COMPLETED | Aspirin for Prevention of Venous Thromboembolism Among Ovarian Cancer Patients Receiving Neoadjuvant Chemotherapy |
| NCT05187208 | Phase 4 | UNKNOWN | PARP Inhibitor Oral Maintenance in Low-Risk Ovarian Cancer |
| NCT05606692 | Phase 4 | RECRUITING | Influences of Propofol and Sevoflurane Anesthesia in Ovarian Cancer (Anesthetics) |
| NCT05926336 | Phase 4 | UNKNOWN | The Effects of Using Different Anesthetics on the Prognosis of Primary Tumors and Its Mechanism of Action |
| NCT06412120 | Phase 4 | RECRUITING | Study Evaluating Safety, Tolerability, and Metabolism of Niraparib |
| NCT06871787 | Phase 4 | NOT_YET_RECRUITING | Near-Infrared Fluorescence Imaging With Indocyanine Green to Evaluate Bowel Anastomoses in Gynecologic Oncology Surgery |
| NCT06887933 | Phase 4 | NOT_YET_RECRUITING | A Trial to Evaluate the Safety of Niraparib Tablets in Adult Female Participants With Advanced or Relapsed Epithelial Ovarian Cancer |
| NCT07469202 | Phase 4 | NOT_YET_RECRUITING | CYTALUX Dose Extension Study |
| NCT00001806 | Phase 3 | COMPLETED | Methods in Education for Breast Cancer Genetics |
| NCT00002477 | Phase 3 | UNKNOWN | Adjuvant Chemotherapy Compared With Observation in Treating Patients With Resected Early Stage Ovarian Epithelial Cancer |
| NCT00002568 | Phase 3 | COMPLETED | Combination Chemotherapy With or Without Surgery in Treating Patients With Stage III Ovarian Epithelial Cancer |
| NCT00002641 | Phase 3 | COMPLETED | Surgery With or Without Chemotherapy in Treating Patients With Soft Tissue Sarcoma |
| NCT00002717 | Phase 3 | COMPLETED | Paclitaxel and Cisplatin in Treating Patients With Stage III or Stage IV Ovarian Cancer or Primary Peritoneal Cancer |
| NCT00002764 | Phase 3 | COMPLETED | Surgery With or Without Combination Chemotherapy in Treating Patients With Lung Metastases From Soft Tissue Sarcoma |
| NCT00002819 | Phase 3 | TERMINATED | Chemotherapy With or Without Peripheral Stem Cell Transplantation in Treating Patients With Persistent Ovarian Epithelial Cancer |
| NCT00002894 | Phase 3 | COMPLETED | Platinum-based Chemotherapy With or Without Paclitaxel in Treating Patients With Relapsed Ovarian Cancer |
| NCT00002895 | Phase 3 | COMPLETED | Early Chemotherapy Based on CA 125 Level Alone Compared With Delayed Chemotherapy in Treating Patients With Recurrent Ovarian Epithelial , Fallopian Tube, or Primary Peritoneal Cancer |
| NCT00003120 | Phase 3 | COMPLETED | S9701 Paclitaxel in Treating Patients With Advanced Ovarian, Fallopian Tube, or Primary Peritoneal Cancer in Remission |
| NCT00003214 | Phase 3 | COMPLETED | Chemosensitivity Testing to Assign Treatment for Patients With Stage III or Stage IV Ovarian Cancer |
| NCT00003322 | Phase 3 | COMPLETED | Combination Chemotherapy in Treating Patients With Primary Peritoneal or Stage III Epithelial Ovarian Cancer |
| NCT00003636 | Phase 3 | COMPLETED | Chemotherapy Plus Surgery in Treating Patients With Stage III or Stage IV Ovarian, Peritoneal, or Fallopian Tube Cancer |
| NCT00003644 | Phase 3 | COMPLETED | Carboplatin Plus Paclitaxel With or Without Continued Low-Dose Paclitaxel in Treating Patients With Early-Stage Ovarian Cancer |
| NCT00003695 | Phase 3 | COMPLETED | Chemotherapy With or Without Surgery in Treating Patients With Stage II or Stage III Ovarian Cancer |
| NCT00003998 | Phase 3 | COMPLETED | Carboplatin Plus Paclitaxel or Docetaxel in Treating Patients With Ovarian Epithelial Cancer |
| NCT00004115 | Phase 3 | UNKNOWN | Monoclonal Antibody Therapy in Treating Patients With Ovarian Cancer or Primary Peritoneal Cancer in Remission Following Surgery and Chemotherapy |
| NCT00004166 | Phase 3 | COMPLETED | Amifostine in Treating Patients With Ovarian Epithelial Cancer Who Are Receiving Chemotherapy |
| NCT00004921 | Phase 3 | COMPLETED | High-Dose Chemotherapy Compared With Standard Chemotherapy in Treating Patients With Stage III or Stage IV Ovarian Epithelial Cancer That Has Been Removed During Surgery |
| NCT00004934 | Phase 3 | COMPLETED | Paclitaxel and Carboplatin With or Without Epirubicin in Treating Patients With Stage IIB, Stage III, or Stage IV Invasive Ovarian Epithelial, Fallopian Tube, or Peritoneal Cancer |
| NCT00005590 | Phase 3 | COMPLETED | Levofloxacin to Prevent Infection Following Chemotherapy in Treating Patients With Solid Tumors or Lymphoma |
| NCT00006356 | Phase 3 | TERMINATED | Chemotherapy With or Without Surgery in Treating Patients With Recurrent Ovarian Cancer |
| NCT00006453 | Phase 3 | COMPLETED | Carboplatin With or Without Gemcitabine in Treating Patients With Advanced Ovarian Epithelial Cancer That Has Not Responded to Previous Chemotherapy |
| NCT00006454 | Phase 3 | COMPLETED | Paclitaxel Plus Carboplatin With or Without Topotecan in Treating Patients With Stage IIB, Stage III, or Stage IV Ovarian Epithelial Cancer |
| NCT00011986 | Phase 3 | COMPLETED | Combination Chemotherapy in Treating Patients With Stage III or Stage IV Ovarian Epithelial Cancer or Primary Peritoneal Cancer |
| NCT00028743 | Phase 3 | COMPLETED | Combination Chemotherapy Regimens in Ovarian Epithelial Cancer, Primary Peritoneal Cancer, or Fallopian Tube Cancer |
| NCT00033605 | Phase 3 | COMPLETED | Octreotide in Preventing Diarrhea in Patients Who Are Undergoing Radiation Therapy to the Pelvis |
| NCT00043082 | Phase 3 | COMPLETED | S0200 Carboplatin With or Without Doxil in Patients With Recurrent Ovarian Cancer |
| NCT00050375 | Phase 3 | TERMINATED | Clinical Trial for Ovarian Cancer (OvaRex®) |
| NCT00052468 | Phase 3 | COMPLETED | Carboplatin/Paclitaxel +/-Gemcitabine in Treating Patients With Ovarian Epithelial or Fallopian Tube Cancer |
| NCT00057720 | Phase 3 | COMPLETED | TLK286 (Telcyta) vs. Doxil/Caelyx or Hycamtin in Platinum Refractory or Resistant Ovarian Cancer |
| NCT00098878 | Phase 3 | COMPLETED | Carboplatin in Treating Patients With Stage IC-IV Ovarian, Fallopian Tube, or Primary Peritoneal Cancer |
| NCT00102375 | Phase 3 | COMPLETED | Paclitaxel, Carboplatin, and Topotecan in Patients With Ovarian Cancer |
| NCT00102414 | Phase 3 | COMPLETED | Gemcitabine Plus Carboplatin Versus Carboplatin Monotherapy in Patients With Advanced Ovarian Cancer |
Predicted chemistry — Sugi Predict
The predicted patent-compound landscape for NQO2 across ~30M SureChEMBL compounds — explore on Sugi Predict.
Related Atlas pages
- Pharmacogenomically associated drugs (drugs whose metabolism/response is associated with variants in this gene (PharmGKB) — not drugs that target it): Idarubicin