Page last updated: 2024-08-05 15:32:59
aryl hydrocarbon receptor antagonist
An antagonist that binds to and activates aryl hydrocarbon receptors (AhRs).
ChEBI ID: 76998
Members (1)
| Member | Definition | Class |
|---|---|---|
| alpha-naphthoflavone | An extended flavonoid resulting from the formal fusion of a benzene ring with the h side of flavone. A synthetic compound, it is an inhibitor of aromatase (EC 1.14.14.14). | alpha-naphthoflavone |
Research
Studies (638)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 160 (25.08) | 18.7374 |
| 1990's | 162 (25.39) | 18.2507 |
| 2000's | 160 (25.08) | 29.6817 |
| 2010's | 119 (18.65) | 24.3611 |
| 2020's | 37 (5.80) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (0.15%) | 5.53% |
| Reviews | 10 (1.50%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 654 (98.35%) | 84.16% |
Protein Targets (66)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 14.1254 | 1 | 1 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| alpha-galactosidase | Homo sapiens (human) | Potency | 7.0795 | 1 | 1 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 39.8107 | 1 | 1 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 35.7168 | 2 | 2 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 35.7168 | 2 | 2 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 1.9953 | 1 | 1 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 7.9433 | 1 | 1 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 12.5893 | 2 | 2 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 7.9433 | 1 | 3 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 25.1189 | 1 | 1 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 17.7828 | 1 | 1 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 44.6684 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 8.4144 | 1 | 1 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 31.6228 | 2 | 2 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Adenosine receptor A1 | Homo sapiens (human) | IC50 | 1.1325 | 1 | 1 |
| Adenosine receptor A1 | Homo sapiens (human) | Ki | 0.6606 | 1 | 1 |
| Aromatase | Homo sapiens (human) | IC50 | 1.0350 | 2 | 2 |
| Aromatase | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
| Aryl hydrocarbon receptor | Mus musculus (house mouse) | IC50 | 0.0250 | 1 | 1 |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 | 24.6000 | 1 | 1 |
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | IC50 | 1.3550 | 2 | 2 |
| Carboxylic ester hydrolase | Sus scrofa (pig) | IC50 | 0.0478 | 1 | 1 |
| cGMP-specific 3',5'-cyclic phosphodiesterase | Homo sapiens (human) | IC50 | 2.3034 | 1 | 1 |
| Cytochrome P450 1A1 | Homo sapiens (human) | IC50 | 2.4555 | 26 | 26 |
| Cytochrome P450 1A1 | Homo sapiens (human) | Ki | 0.0450 | 1 | 1 |
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 | 2.1195 | 38 | 38 |
| Cytochrome P450 1A2 | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
| Cytochrome P450 1B1 | Homo sapiens (human) | IC50 | 10.8787 | 34 | 34 |
| Cytochrome P450 1B1 | Homo sapiens (human) | Ki | 0.0160 | 1 | 1 |
| Cytochrome P450 2A6 | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| Cytochrome P450 2B6 | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 | 15.0000 | 4 | 4 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 15.0000 | 4 | 4 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 | 13.3333 | 6 | 6 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 13.3333 | 6 | 6 |
| Cytochrome P450 3A6 | Oryctolagus cuniculus (rabbit) | Ki | 80.1000 | 1 | 1 |
| DNA-dependent protein kinase catalytic subunit | Homo sapiens (human) | IC50 | 4.9800 | 1 | 1 |
| Histamine H3 receptor | Cavia porcellus (domestic guinea pig) | IC50 | 20.0000 | 1 | 1 |
| Multidrug resistance-associated protein 1 | Homo sapiens (human) | IC50 | 11.3000 | 1 | 1 |
| Sodium-dependent dopamine transporter | Rattus norvegicus (Norway rat) | IC50 | 0.0100 | 1 | 1 |
| Sodium-dependent serotonin transporter | Rattus norvegicus (Norway rat) | IC50 | 0.0500 | 1 | 1 |
| Substance-K receptor | Homo sapiens (human) | IC50 | 5.8471 | 1 | 1 |
| Substance-K receptor | Homo sapiens (human) | Ki | 1.9490 | 1 | 1 |
| Thromboxane-A synthase | Homo sapiens (human) | IC50 | 6.7608 | 1 | 1 |
| UDP-glucuronosyltransferase 1-6 | Homo sapiens (human) | IC50 | 115.4000 | 1 | 5 |
| UDP-glucuronosyltransferase 1A1 | Homo sapiens (human) | IC50 | 115.4000 | 1 | 5 |
| UDP-glucuronosyltransferase 1A4 | Homo sapiens (human) | IC50 | 115.4000 | 1 | 5 |
| UDP-glucuronosyltransferase 2B10 | Homo sapiens (human) | IC50 | 115.4000 | 1 | 5 |
| UDP-glucuronosyltransferase 2B7 | Homo sapiens (human) | IC50 | 115.4000 | 1 | 5 |
| Xanthine dehydrogenase/oxidase | Bos taurus (cattle) | IC50 | 20.0000 | 1 | 1 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cytochrome P450 1A1 | Homo sapiens (human) | EC50 | 2.5000 | 2 | 2 |
| Cytochrome P450 1B1 | Homo sapiens (human) | EC50 | 26.7000 | 3 | 3 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cytochrome P450 1B1 | Homo sapiens (human) | Ks | 0.7000 | 1 | 1 |