An EC 1.14.14.* (oxidoreductase acting on paired donors, incorporating of 1 atom of oxygen, with reduced flavin or flavoprotein as one donor) inhibitor which interferes with the action of aromatase (EC 1.14.14.14) and so reduces production of estrogenic steroid hormones.
| Member | Definition | Class |
|---|
| 7-hydroxyisoflavone | The simplest member of the class of 7-hydroxyisoflavones that is isoflavone with a hydroxy substituent at position 7. | 7-hydroxyisoflavone |
| 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 |
| aminoglutethimide | A dicarboximide that is a six-membered cyclic compound having ethyl and 4-aminophenyl substituents at the 3-position. | aminoglutethimide |
| anastrozole | A 1,2,4-triazole compound having a 3,5-bis(2-cyano-2-propyl)benzyl group at the 1-position. | anastrozole |
| androsta-1,4,6-triene-3,17-dione | An androstanoid that is androsta-1,4,6-triene substituted by oxo groups at positions 3 and 17. | androsta-1,4,6-triene-3,17-dione |
| aromasil | A 17-oxo steroid that is androsta-1,4-diene-3,17-dione in which the hydrogens at position 6 are replaced by a double bond to a methylene group. A selective inhibitor of the aromatase (oestrogen synthase) system, it is used in the treatment of advanced breast cancer. | exemestane |
| formestane | A 17-oxo steroid that is androst-4-ene-3,17-dione in which the hydrogen at position 4 is replaced by a hydroxy group. Formestane was the first selective, type I steroidal aromatase inhibitor, suppressing oestrogen production from anabolic steroids or prohormones. It was formerly used in the treatment of oestrogen-receptor positive breast cancer in post-meopausal women. As it has poor oral bioavailability, it had to be administered by (fortnightly) intramuscular injection. It fell out of use with the subsequent development of cheaper, orally active aromatase inhibitors. Formestane is listed by the World Anti-Doping Agency as a substance prohibited from use by athletes. | formestane |
| letrozole | | letrozole |
| myosmine | A member of the class of pyridines that is pyridine substituted by a 3,4-dihydro-2H-pyrrol-5-yl group at position 3. It is an alkaloid found in tobacco plants and exhibits genotoxic effects. | myosmine |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 14.1254 | 1 | 1 |
| acid sphingomyelinase | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 1.5484 | 1 | 1 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 25.7232 | 1 | 4 |
| alpha-galactosidase | Homo sapiens (human) | Potency | 7.0795 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 9.9059 | 10 | 29 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 8.9189 | 2 | 2 |
| BRCA1 | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 89.1251 | 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 | 31.8326 | 1 | 2 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 39.8107 | 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 A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 0.0060 | 1 | 2 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 35.7168 | 2 | 2 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| core-binding factor subunit beta isoform 2 | Homo sapiens (human) | Potency | 15.0875 | 1 | 1 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 5.9606 | 1 | 3 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 7.9433 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 15.7188 | 1 | 3 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 16.4080 | 2 | 6 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 10.7062 | 1 | 4 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 3.1089 | 1 | 9 |
| DNA polymerase beta | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| Endothelin receptor type B | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| Endothelin-1 receptor | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 21.0376 | 8 | 23 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 61.1306 | 1 | 1 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 43.3616 | 4 | 9 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 0.8913 | 1 | 1 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 20.0412 | 4 | 4 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 25.2119 | 1 | 3 |
| G | Vesicular stomatitis virus | Potency | 15.7188 | 1 | 3 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 16.4080 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 16.4080 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 16.4080 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 16.4080 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 16.4080 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 16.4080 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 16.4080 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 16.4080 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 16.4080 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 16.4080 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 16.4080 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 16.4080 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 16.4080 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 16.4080 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 16.4080 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 16.4080 | 1 | 3 |
| geminin | Homo sapiens (human) | Potency | 10.6952 | 1 | 2 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 18.2564 | 2 | 6 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 2.6832 | 1 | 1 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 7.9433 | 1 | 3 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 15.7188 | 1 | 3 |
| IDH1 | Homo sapiens (human) | Potency | 16.3601 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 15.7188 | 1 | 6 |
| Interferon beta | Homo sapiens (human) | Potency | 16.1288 | 2 | 6 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 25.1189 | 1 | 1 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 15.1014 | 1 | 1 |
| luciferase | Photuris pensylvanica (Pennsylania firefly) | Potency | 11.2202 | 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 |
| muscleblind-like protein 1 isoform 1 | Homo sapiens (human) | Potency | 0.1000 | 1 | 1 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 11.2202 | 1 | 1 |
| NPC intracellular cholesterol transporter 1 precursor | Homo sapiens (human) | Potency | 3.1623 | 1 | 1 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 2.3468 | 2 | 2 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 29.0929 | 1 | 1 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 54.9477 | 1 | 1 |
| nuclear receptor subfamily 1, group I, member 2 | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1 | 1 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 6.2533 | 3 | 3 |
| parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 44.6684 | 1 | 1 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 6.0120 | 1 | 1 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 84.9214 | 1 | 1 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 33.8992 | 2 | 2 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 44.6684 | 1 | 1 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 5.0119 | 1 | 1 |
| PPM1D protein | Homo sapiens (human) | Potency | 16.5388 | 1 | 2 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 44.0977 | 3 | 5 |
| progesterone receptor | Homo sapiens (human) | Potency | 9.2094 | 1 | 3 |
| pyruvate kinase | Leishmania mexicana mexicana | Potency | 12.5893 | 2 | 2 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 27.3060 | 2 | 2 |
| ras-related protein Rab-9A | Homo sapiens (human) | Potency | 2.8184 | 1 | 1 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 19.2490 | 2 | 2 |
| runt-related transcription factor 1 isoform AML1b | Homo sapiens (human) | Potency | 15.0875 | 1 | 1 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 20.1548 | 2 | 2 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 20.1548 | 2 | 2 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 31.0990 | 1 | 2 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 11.8230 | 1 | 2 |
| TAR DNA-binding protein 43 | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 13.5812 | 2 | 4 |
| thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 39.8107 | 1 | 1 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 21.2365 | 1 | 2 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 30.9133 | 2 | 5 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 17.8404 | 2 | 2 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 25.2158 | 4 | 7 |
| transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 0.8913 | 1 | 1 |
| tyrosine-protein kinase Yes | Homo sapiens (human) | Potency | 38.7088 | 1 | 1 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 24.5412 | 1 | 1 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 24.9592 | 2 | 2 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 14.1254 | 1 | 1 |