Page last updated: 2024-08-05 15:20:52

androgen antagonist

A compound which inhibits or antagonises the biosynthesis or actions of androgens.

ChEBI ID: 35497

Members (14)

MemberDefinitionClass
bupirimateA member of the class of aminopyrimidines that is 2-ethylaminopyrimidine carrying methyl, butyl and dimethylaminosulfooxy substituents at posiitons 4, 5 and 6 respectively.bupirimate
cyproteronecyproterone
cyproterone acetateA steroid ester resulting from the formal condensation of the carboxy group of acetic acid with the 17-hydroxy group of cyproterone. It is an antiandrogenic drug which has recently been recognized to promote the occurrence and growth of intracranial meningiomas.cyproterone acetate
epi 001The (3-chloro-2-hydroxypropyl) (2,3-dihydroxypropyl) diether of bisphenol A; a small molecule that inhibits transactivation of the AR amino-terminal domain (NTD).bisphenol A (3-chloro-2-hydroxypropyl) (2,3-dihydroxypropyl) ether
epitestosteroneAn androstanoid that is the C-17 epimer of testosterone.epitestosterone
finasterideAn aza-steroid that is a synthetic drug for the treatment of benign prostatic hyperplasia.finasteride
fludioxonilA member of the class of benzodioxoles that is 2,2-difluoro-1,3-benzodioxole substituted at position 4 by a 3-cyanopyrrol-4-yl group. A fungicide seed treatment for control of a range of diseases including Fusarium, Rhizoctonia and Alternaria.fludioxonil
flutamideflutamide
germacroneA germacrane sesquiterpenoid that has formula C15H22O. It is a natural product found in traditional medicinal plants of the family Zingiberaceae. The compound exhibits a range of pharmacological activities including anti-inflammatory, anticancer, antiviral, anti-androgenic, antioxidant, antimicrobial, antifungal, neuroprotective and insecticidal activities.(E,E)-germacrone
mdv 3100A benzamide obtained by formal condensation of the carboxy group of 4-{3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl}-2-fluorobenzoic acid with methylamine. Used for the treatment of of metastatic castration-resistant prostate cancer.enzalutamide
nilutamidenilutamide
nitrogenase stabilizing-protective protein, bacteriaA N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide that is the (R)-enantiomer of bicalutamide.(R)-bicalutamide
raspberry ketoneA ketone that is 4-phenylbutan-2-one in which the phenyl ring is substituted at position 4 by a hydroxy group. It is found in a variety of fruits including raspberries, blackberries and cranberries, and is used in perfumery and cosmetics.raspberry ketone
spongia-13(16),14-dien-19-oic acidA tetracyclic diterpenoid that is 3b,4,5,5a,6,7,8,9,9a,9b,10,11-dodecahydrophenanthro[1,2-c]furan substituted by methyl groups at positions 3b, 6 and 9 and a carboxy group at position 6. Isolated from Spongia, it exhibits inhibitory activity against androgen receptor.spongia-13(16),14-dien-19-oic acid

Research

Studies (9,510)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19901,667 (17.53)18.7374
1990's1,937 (20.37)18.2507
2000's2,192 (23.05)29.6817
2010's2,618 (27.53)24.3611
2020's1,096 (11.52)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials1,574 (13.86%)5.53%
Reviews1,229 (10.83%)6.00%
Case Studies616 (5.43%)4.05%
Observational46 (0.41%)0.25%
Other7,888 (69.48%)84.16%

Protein Targets (173)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-lipoxygenase, partialHomo sapiens (human)Potency39.810711
67.9K proteinVaccinia virusPotency14.555926
acetylcholinesteraseHomo sapiens (human)Potency35.878012
activating transcription factor 6Homo sapiens (human)Potency6.162211
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency35.716812
alpha-galactosidaseHomo sapiens (human)Potency12.589311
Alpha-synucleinHomo sapiens (human)Potency22.387212
AR proteinHomo sapiens (human)Potency18.43481295
aryl hydrocarbon receptorHomo sapiens (human)Potency17.287637
arylsulfatase AHomo sapiens (human)Potency1.510111
ATAD5 protein, partialHomo sapiens (human)Potency14.575023
Ataxin-2Homo sapiens (human)Potency27.556226
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency29.688326
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency21.331311
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency12.197211
caspase-3Homo sapiens (human)Potency12.197211
Cellular tumor antigen p53Homo sapiens (human)Potency45.8076210
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency31.622811
Chain A, Beta-lactamaseEscherichia coli K-12Potency12.875022
Chain A, CruzipainTrypanosoma cruziPotency39.810711
Chain A, Ferritin light chainEquus caballus (horse)Potency39.810711
chromobox protein homolog 1Homo sapiens (human)Potency26.651412
cytochrome P450 2C19 precursorHomo sapiens (human)Potency4.580114
cytochrome P450 2C9 precursorHomo sapiens (human)Potency27.285414
cytochrome P450 2C9, partialHomo sapiens (human)Potency10.390615
cytochrome P450 2D6Homo sapiens (human)Potency27.540411
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency12.589311
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency7.3367210
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency16.558713
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency38.952216
D(1A) dopamine receptorHomo sapiens (human)Potency4.534312
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.125112
endonuclease IVEscherichia coliPotency0.891311
estrogen nuclear receptor alphaHomo sapiens (human)Potency32.99991181
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency49.185414
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency29.3569980
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency4.853916
EWS/FLI fusion proteinHomo sapiens (human)Potency7.761449
farnesoid X nuclear receptorHomo sapiens (human)Potency29.4554411
GVesicular stomatitis virusPotency10.390615
GABA theta subunitRattus norvegicus (Norway rat)Potency7.336715
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency7.336715
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency7.336715
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency7.336715
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency7.336715
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency7.336715
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency7.336715
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency7.336715
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency7.336715
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency7.336715
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency7.336715
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency7.336715
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency7.336715
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency7.336715
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency7.336715
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency7.336715
gemininHomo sapiens (human)Potency7.467424
GLI family zinc finger 3Homo sapiens (human)Potency16.0799223
GLS proteinHomo sapiens (human)Potency5.623411
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency18.0671316
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency38.963618
heat shock protein beta-1Homo sapiens (human)Potency56.548022
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency27.2854112
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency10.390615
huntingtin isoform 2Homo sapiens (human)Potency15.848911
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency43.641211
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency10.3906110
Interferon betaHomo sapiens (human)Potency12.160026
interleukin 8Homo sapiens (human)Potency74.978011
lamin isoform A-delta10Homo sapiens (human)Potency7.270113
M-phase phosphoprotein 8Homo sapiens (human)Potency44.959712
mitogen-activated protein kinase 1Homo sapiens (human)Potency23.060222
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency6.495024
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency20.483912
neuropeptide S receptor isoform AHomo sapiens (human)Potency25.118911
NFKB1 protein, partialHomo sapiens (human)Potency7.079522
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency56.234111
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency36.7363328
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency17.097913
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency43.367915
Nuclear receptor ROR-gammaHomo sapiens (human)Potency30.644012
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency20.3465212
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency10.430412
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency38.0077318
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency42.209012
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency89.125111
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency15.429125
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency95.283411
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency30.6339511
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency26.8416412
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency6.309611
pregnane X nuclear receptorHomo sapiens (human)Potency34.0742314
pregnane X receptorRattus norvegicus (Norway rat)Potency40.370814
progesterone receptorHomo sapiens (human)Potency18.4566318
RAR-related orphan receptor gammaMus musculus (house mouse)Potency33.7280223
ras-related protein Rab-9AHomo sapiens (human)Potency115.821011
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency38.0947320
retinoid X nuclear receptor alphaHomo sapiens (human)Potency23.9193416
SMAD family member 2Homo sapiens (human)Potency31.338529
SMAD family member 3Homo sapiens (human)Potency31.338529
Smad3Homo sapiens (human)Potency35.481311
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency24.582514
survival motor neuron protein isoform dHomo sapiens (human)Potency17.066615
TDP1 proteinHomo sapiens (human)Potency13.7565227
thioredoxin reductaseRattus norvegicus (Norway rat)Potency39.745024
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency39.3701327
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency0.005611
thyroid stimulating hormone receptorHomo sapiens (human)Potency32.302248
USP1 protein, partialHomo sapiens (human)Potency45.991923
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency10.656523
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency13.7797510
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency89.125111
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency38.963618

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomeraseMycobacterium tuberculosis H37RvIC50312.000011
3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)Ki11.000011
3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)IC502.49102224
3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)Ki0.258022
3-oxo-5-alpha-steroid 4-dehydrogenase 1 Rattus norvegicus (Norway rat)IC50180.007857
3-oxo-5-alpha-steroid 4-dehydrogenase 1 Rattus norvegicus (Norway rat)Ki0.059534
3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)IC5024.24342326
3-oxo-5-alpha-steroid 4-dehydrogenase 2Rattus norvegicus (Norway rat)IC500.328657
3-oxo-5-alpha-steroid 4-dehydrogenase 2Rattus norvegicus (Norway rat)Ki0.077023
5-hydroxytryptamine receptor 6Homo sapiens (human)IC5017.814011
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki8.271011
Adenosine receptor A1Rattus norvegicus (Norway rat)IC500.045023
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki0.001022
Adenosine receptor A2aRattus norvegicus (Norway rat)Ki0.336013
Adenosine receptor A2bRattus norvegicus (Norway rat)Ki0.336013
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)IC501.260011
Androgen receptorHomo sapiens (human)GI500.736733
Androgen receptorHomo sapiens (human)IC5014.75644654
Androgen receptorRattus norvegicus (Norway rat)IC5010.9746913
Androgen receptorHomo sapiens (human)Ki1.21521315
Androgen receptorRattus norvegicus (Norway rat)Ki1.29711013
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000012
Bile salt export pumpHomo sapiens (human)IC5074.9580810
Bile salt export pumpRattus norvegicus (Norway rat)IC5078.700011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000012
Cocaine esteraseHomo sapiens (human)Ki2.300011
Cytochrome P450 2A6Homo sapiens (human)GI501.800012
Cytochrome P450 2B6Homo sapiens (human)GI501.800013
Cytochrome P450 2C19Homo sapiens (human)GI501.800014
Cytochrome P450 2C19Homo sapiens (human)IC501.000012
Cytochrome P450 2C8Homo sapiens (human)GI501.800011
Cytochrome P450 2C9 Homo sapiens (human)GI501.800012
Cytochrome P450 2C9 Homo sapiens (human)IC502.000011
Cytochrome P450 3A4Homo sapiens (human)GI501.800015
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC503.000011
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)IC503.000011
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)IC503.000011
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)IC503.000011
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)IC503.000011
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)IC503.000011
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)IC503.000011
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC503.000011
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)IC503.000011
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)IC503.000011
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)IC503.000011
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)IC503.000011
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)IC503.000011
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)IC503.000011
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)IC503.000011
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)IC503.000011
Glucocorticoid receptorHomo sapiens (human)IC5013.075033
Glucocorticoid receptorHomo sapiens (human)Ki7.051022
Glycine receptor subunit alpha-1Rattus norvegicus (Norway rat)IC500.225011
Glycine receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki0.102011
Glycine receptor subunit alpha-2Rattus norvegicus (Norway rat)IC500.225011
Glycine receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki0.102011
Glycine receptor subunit alpha-3Rattus norvegicus (Norway rat)IC500.225011
Glycine receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki0.102011
Glycine receptor subunit betaRattus norvegicus (Norway rat)IC500.225011
Glycine receptor subunit betaRattus norvegicus (Norway rat)Ki0.102011
Glycoprotein IIbOryctolagus cuniculus (rabbit)IC500.850011
Integrin betaOryctolagus cuniculus (rabbit)IC500.850011
Mu-type opioid receptorHomo sapiens (human)IC502.183011
Mu-type opioid receptorHomo sapiens (human)Ki0.886011
Multidrug resistance-associated protein 4Homo sapiens (human)IC5092.000012
Muscarinic acetylcholine receptorCavia porcellus (domestic guinea pig)Ki0.151011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC5025.000011
Progesterone receptorHomo sapiens (human)IC501.000011
Prostate-specific antigenHomo sapiens (human)IC500.130011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Androgen receptorHomo sapiens (human)EC502.62861010
Androgen receptorHomo sapiens (human)Kd114.040033
Cytochrome P450 3A4Homo sapiens (human)EC500.420011
Olfactory receptor 51E2Homo sapiens (human)EC500.000711
ORF73Human gammaherpesvirus 8EC5075.000011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Androgen receptorHomo sapiens (human)Activity0.037011
Androgen receptorRattus norvegicus (Norway rat)Kapp24.000011
Arylacetamide deacetylaseHomo sapiens (human)Km500.000023
Arylacetamide deacetylaseMus musculus (house mouse)Km4,300.000022
Arylacetamide deacetylaseRattus norvegicus (Norway rat)Km5,100.000012
Cocaine esteraseHomo sapiens (human)Km300.000011
Neuropeptide FF receptor 2Rattus norvegicus (Norway rat)Activity0.037011