AR
ENSG00000169083
Target class
Nuclear receptor
Chromosome
X
Approved drugs
23
Clinical candidates (approved and in development)
42
- Approved drugs
- 23
- ClinGen gene-disease validity
- Definitive
- Clinical candidates (approved and in development)
- 42
- Chemical probe available
- Yes
- Target name
- AR
- Gene name
- Androgen receptor
- Gene symbol
- AR
- Protein name
- Androgen receptor (Dihydrotestosterone receptor) (Nuclear receptor subfamily 3 group C member 4)
- AIS
- NR3C4
- SMAX1
- HUMARA
- DHTR
- SBMA
- Gene biotype
- Protein coding
- Gene family
- Nuclear receptor subfamily 3 group C
- Target class
- Nuclear receptor
- Target type
- Human gene
- Tissues expressed in
- 38
- Protein localisation evidence grade
- Supported
- Highest tissue expression
- 41.07
- Tissue specificity (Gini)
- 0.648
- Tissue specificity (tau)
- 0.857
- KEGG gene identifiers
- hsa:367
- Protein interaction confidence
- 0.844571
- Protein interaction partners
- 140
- R-HSA-3371497
- R-HSA-383280
- R-HSA-4090294
- R-HSA-5625886
- R-HSA-5689880
- R-HSA-8940973
- End position
- 67730619
- Start position
- 67543353
- Chromosome
- X
- Strand
- Forward
- Nucleus . Cytoplasm . Note=Detected at the promoter of target genes (PubMed:25091737). Predominantly cytoplasmic in unligated form but translocates to the nucleus upon ligand-binding. Can also translocate to the nucleus in unligated form in the presence of RACK1. .
- Cytosol
- PubMed 12958311
- PubMed 15634333
- PubMed 17587566
- PubMed 19244107
- PubMed 19345326
- PubMed 25091737
- Tissue specificity (tau)
- 0.856678
- Expression inequality (Gini)
- 0.648227
Expression in transcripts per million
- Cervix - Endocervix
- 41.07
- Cervix - Ectocervix
- 38.53
- Uterus
- 26.78
- Fallopian Tube
- 22.23
- Vagina
- 22.17
Expression in transcripts per million
- Cervix - Endocervix41.07
- Cervix - Ectocervix38.53
- Uterus26.78
- Fallopian Tube22.23
- Vagina22.17
- Prostate21.05
- Ovary16.84
- Liver14.9
- Cells - Cultured fibroblasts14.7
- Artery - Aorta12.65
- Breast - Mammary Tissue11.46
- Adipose - Subcutaneous10.39
- Artery - Tibial10.03
- Artery - Coronary7.5
- Bladder7.39
- Testis7.02
- Nerve - Tibial5.57
- Skin - Not Sun Exposed (Suprapubic)5.13
- Adipose - Visceral (Omentum)4.75
- Thyroid4.58
- Muscle - Skeletal4.08
- Skin - Sun Exposed (Lower leg)3.89
- Esophagus - Gastroesophageal Junction3.65
- Heart - Atrial Appendage3.22
- Colon - Sigmoid3.18
And 29 more, listed on the interactive page.
- GO:0000122
- GO:0007165
- GO:0007267
- GO:0008284
- GO:0008285
- GO:0010628
- GO:0030520
- GO:0030521
- GO:0030522
- GO:0045597
- GO:0045726
- GO:0045893
- GO:0045944
- GO:0045945
- GO:0071383
- GO:0071391
- GO:0071394
- GO:0140694
- GO:1902895
- GO:1903076
- GO:2001237
- GO:0000785
- GO:0005634
- GO:0005654
- GO:0005737
- GO:0005829
- GO:0016607
- GO:0032991
- GO:0000976
- GO:0000977
- GO:0000978
- GO:0001091
- GO:0001223
- GO:0001228
- GO:0003682
- GO:0003700
- GO:0003707
- GO:0004879
- GO:0005102
- GO:0005497
- GO:0005515
- GO:0008013
- GO:0019899
- GO:0051117
- GO:0060090
- GO:0061629
- GO:0140693
increased body weight
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: increased body weight
- central nervous system
- endocrine
PubMed 28216264N/A, Impairment of reproductive capacity
Effects
- Inhibition/Decrease/Downregulation
Studies
- cell-based
Evidence sourceDecrease, Population growth rate
Effects
- Activation/Increase/Upregulation
Studies
- cell-based
Evidence sourcedepression
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: depression
- central nervous system
- endocrine
PubMed 28216264osteoporosis
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: osteoporosis
- central nervous system
- endocrine
PubMed 28216264death
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: death
- central nervous system
- endocrine
PubMed 28216264decreased anxiety
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: decreased anxiety
- central nervous system
- endocrine
PubMed 28216264hot flashes
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: hot flashes
- central nervous system
- endocrine
PubMed 28216264bone pain
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: bone pain
- central nervous system
- endocrine
PubMed 28216264Decrease, Population growth rate
Effects
- Activation/Increase/Upregulation
Studies
- cell-based
Evidence sourcedecreased attention
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: decreased attention
- central nervous system
- endocrine
PubMed 28216264decreased memory
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: decreased memory
- central nervous system
- endocrine
PubMed 28216264bone metastasis
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: bone metastasis
- central nervous system
- endocrine
PubMed 28216264heart attack
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: heart attack
- central nervous system
- endocrine
PubMed 28216264anemia
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: anemia
- central nervous system
- endocrine
PubMed 28216264Impaired recruitment , Population trajectory
Effects
- Inhibition/Decrease/Downregulation
Studies
- cell-based
Evidence sourceinsulin resistance
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: insulin resistance
- central nervous system
- endocrine
PubMed 28216264sexual dysfunction
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: sexual dysfunction
- central nervous system
- endocrine
PubMed 28216264drug abuse/dependence
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: drug abuse/dependence
- central nervous system
- endocrine
PubMed 28216264Increase, Leydig cell tumors
Effects
- Inhibition/Decrease/Downregulation
Studies
- cell-based
Evidence sourceincreased triglycerides
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: increased triglycerides
- central nervous system
- endocrine
PubMed 28216264Increase, hepatocellular adenomas and carcinomas
Effects
- Activation/Increase/Upregulation
Studies
- cell-based
Evidence source
increased muscle mass
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: increased muscle mass
Biological samples
- endocrine
PubMed 23197038decreased spermatogenesis
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- preclinical: decreased spermatogenesis
Biological samples
- endocrine
PubMed 23197038regulation of transcription factor activity
- cell-based: TOX21_AR_LUC_MDAKB2_Antagonist_Specificity, is one of one assay component(s) measured or calculated from the TOX21_AR_LUC_MDAkb2_Antagonist_Specificity assay. It is designed to make measurements of luciferase induction, a form of inducible reporter, as detected with bioluminescence signals by luciferase-coupled ATP quantitation technology.
- cell-based: TOX21_AR_BLA_Agonist_ratio is an assay readout measuring reporter gene via receptor activity and designed using inducible reporter (beta lactamase induction) detected with GAL4 b-lactamase reporter gene. The signal is derived from the ratio of cleaved (ch2) to uncleaved (ch1) substrate used as the measure of target activity.
- cell-based: TOX21_AR_LUC_MDAKB2_Agonist, is one of one assay component(s) measured or calculated from the TOX21_AR_LUC_MDAkb2_Agonist assay. It is designed to make measurements of luciferase induction, a form of inducible reporter, as detected with bioluminescence signals by luciferase-coupled ATP quantitation technology.
- cell-based: ATG_AR_TRANS, is one of 30 assay component(s) measured or calculated from the ATG_TRANS assay. It is designed to make measurements of mRNA induction, a form of inducible reporter, as detected with fluorescence intensity signals by Reverse transcription polymerase chain reaction (RT-PCR) and Capillary electrophoresis technology.
- cell-based: TOX21_AR_LUC_MDAKB2_Antagonist is one of one assay component(s) measured or calculated from the TOX21_AR_LUC_MDAkb2_Antagonist. It is designed to make measurements of luciferase induction, a form of inducible reporter, as detected with bioluminescence signals following addition of luciferin substrate and ATP.
- cell-based: TOX21_AR_BLA_Antagonist_ratio is an assay readout measuring reporter gene via receptor activity and designed using inducible reporter (beta lactamase induction) detected with GAL4 b-lactamase reporter gene. The signal is derived from the ratio of cleaved (ch2) to uncleaved (ch1) reporter gene substrate used as the measure of target activity.
- cell-based: ATG_AR_TRANS, is one of 30 assay component(s) measured or calculated from the ATG_TRANS assay. It is designed to make measurements of mRNA induction, a form of inducible reporter, as detected with fluorescence intensity signals by Reverse transcription polymerase chain reaction (RT-PCR) and Capillary electrophoresis technology.
- MDA-kb2, cell line
- HEK293T, cell line
- HepG2, cell line
Evidence sourceandrogenicity females
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: androgenicity females
Biological samples
- endocrine
PubMed 23197038receptor binding
Studies
- biochemical: NVS_NR_hAR, is one of one assay component(s) measured or calculated from the NVS_NR_hAR assay. It is designed to make measurements of radioligand binding, a form of binding reporter, as detected with scintillation counting signals by Lysate-based radiodetection technology.
Biological samples
- cell-free
Evidence sourceregulation of steroid biosynthetic process
- cell-based: CEETOX_H295R_ANDR, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
- cell-based: CEETOX_H295R_TESTO, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
- cell-based: CEETOX_H295R_TESTO, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
- cell-based: CEETOX_H295R_ANDR, is one of 23 assay component(s) measured or calculated from the CEETOX_H295R assay. It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology.
Biological samples
- H295R, cell line
Evidence sourcegynecomastia
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- preclinical: gynecomastia
Biological samples
- endocrine
PubMed 23197038cell proliferation
- cell-based: ACEA_AR_80hr, is one of two assay component(s) measured or calculated from the ACEA_AR assay. It is designed to make measurements of real-time cell-growth kinetics, a form of growth reporter, as detected with electrical impedance signals by Real-Time Cell Electrode Sensor (RT-CES) technology.
- cell-based: ACEA_AR_80hr, is one of two assay component(s) measured or calculated from the ACEA_ER assay. It is designed to make measurements of real-time cell-growth kinetics, a form of growth reporter, as detected with electrical impedance signals by Real-Time Cell Electrode Sensor (RT-CES) technology.
Biological samples
- 22Rv1, cell line
Evidence sourceoedema
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: oedema
Biological samples
- endocrine
PubMed 23197038regulation of steroid hormone biosynthetic process
- cell-based: one of 12 assay component(s) measured or calculated from the CEETOX_H295R assay (11 hormones and 1 viability assay). It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology. The concentrations for these components have not been pre-filtered for the maximum tolerated concentration (MTC) based on the MTT assay (_noMTC).
- cell-based: one of 12 assay component(s) measured or calculated from the CEETOX_H295R assay (11 hormones and 1 viability assay). It is designed to make measurements of hormone induction, a form of inducible reporter, as detected with absorbance signals by HPLC-MS-MS technology. The concentrations for these components have not been pre-filtered for the maximum tolerated concentration (MTC) based on the MTT assay (_noMTC).
Biological samples
- H295R, cell line
Evidence sourceliver complications
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: liver complications
Biological samples
- endocrine
PubMed 23197038sleep apnoea
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: sleep apnoea
Biological samples
- endocrine
PubMed 23197038increased hostility
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: increased hostility
Biological samples
- endocrine
PubMed 23197038impotence
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- preclinical: impotence
Biological samples
- endocrine
PubMed 23197038mastodynia
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- preclinical: mastodynia
Biological samples
- endocrine
PubMed 23197038protein stabilization
- cell-based: OT_AR_ARSRC1_0960, is one of one assay component(s) measured or calculated from the OT_AR_ARSRC1_0960 assay. It is designed to make measurements of protein fragment complementation, a form of binding reporter, as detected with fluorescence intensity signals by Protein-fragment Complementation technology.
- cell-based: OT_AR_ARSRC1_0480, is one of one assay component(s) measured or calculated from the OT_AR_ARSRC1_0480 assay. It is designed to make measurements of protein fragment complementation, a form of binding reporter, as detected with fluorescence intensity signals by Protein-fragment Complementation technology.
Biological samples
- HEK293T, cell line
Evidence sourceincreased breast carcinoma
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- preclinical: increased breast carcinoma
Biological samples
- endocrine
PubMed 23197038increased prostate carcinoma
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: increased prostate carcinoma
Biological samples
- endocrine
PubMed 23197038
Related records
Trials (1,381)
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- A 2 Part, Phase 2 Trial of Galeterone in the Treatment of Castration Resistant Prostate Cancer
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Drugs (42)
- Abiraterone Androgen Receptor antagonist
- Apalutamide Androgen Receptor antagonist
- APC-100 Androgen Receptor antagonist
- AZD3514 Androgen Receptor modulator
- Bicalutamide Androgen Receptor antagonist
- Clascoterone Androgen Receptor antagonist
- CR 1447 Androgen Receptor agonist
- Cyproterone acetate Androgen Receptor antagonist
- Danazol Androgen Receptor agonist
- Darolutamide Androgen Receptor antagonist
- Dimethylcurcumin Androgen Receptor degrader
- Dromostanolone propionate Androgen Receptor agonist
- Enobosarm Androgen Receptor modulator
- Enzalutamide Androgen Receptor antagonist
- Ethylestrenol Androgen Receptor agonist
- Fluoxymesterone Androgen Receptor agonist
- Flutamide Androgen Receptor antagonist
- Galeterone Androgen Receptor antagonist
- GLPG0492 Androgen Receptor modulator
- GSK2849466 Androgen Receptor modulator