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Target Report Card

Target Name and Classification

Target ID CHEMBL1871
Target Type SINGLE PROTEIN
Preferred Name Androgen Receptor
Synonyms AR | Androgen receptor | DHTR | Dihydrotestosterone receptor | NR3C4 | Nuclear receptor subfamily 3 group C member 4
Organism Homo sapiens
Species Group No
Protein Target Classification
  • transcription factor > nuclear receptor > nuclear hormone receptor subfamily 3 > nuclear hormone receptor subfamily 3 group c > nuclear hormone receptor subfamily 3 group c member 4

Target Components

Component Description Relationship Accession
Androgen receptor SINGLE PROTEIN P10275

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL409 BICALUTAMIDE Androgen Receptor antagonist 4 DailyMed
CHEMBL806 FLUTAMIDE Androgen Receptor antagonist 4 DailyMed FDA
CHEMBL1170 TESTOSTERONE PROPIONATE Androgen Receptor agonist 4 PubMed PubMed PubMed PubMed PubMed PubMed
CHEMBL1274 NILUTAMIDE Androgen Receptor antagonist 4 DailyMed
CHEMBL1395 METHYLTESTOSTERONE Androgen Receptor agonist 4 DailyMed
CHEMBL386630 TESTOSTERONE Androgen Receptor agonist 4 DailyMed FDA
CHEMBL1445 FLUOXYMESTERONE Androgen Receptor agonist 4 DailyMed
CHEMBL1479 DANAZOL Androgen Receptor agonist 4 DailyMed FDA ISBN PubMed
CHEMBL1082407 ENZALUTAMIDE Androgen Receptor antagonist 4 Expert
CHEMBL1200335 TESTOSTERONE ENANTHATE Androgen Receptor agonist 4 DailyMed FDA
CHEMBL1200412 NANDROLONE PHENPROPIONATE Androgen Receptor agonist 4 PubMed PubMed PubMed
CHEMBL1200436 OXANDROLONE Androgen Receptor agonist 4 DailyMed
CHEMBL1200585 OXYMETHOLONE Androgen Receptor agonist 4 DailyMed
CHEMBL1200623 ETHYLESTRENOL Androgen Receptor agonist 4 ISBN PubMed
CHEMBL1200946 NANDROLONE DECANOATE Androgen Receptor agonist 4 PubMed
CHEMBL1201048 DROMOSTANOLONE PROPIONATE Androgen Receptor agonist 4 PubMed PubMed
CHEMBL1201101 TESTOSTERONE CYPIONATE Androgen Receptor agonist 4 DailyMed
CHEMBL2079587 STANOZOLOL Androgen Receptor agonist 4 PubMed
CHEMBL2107067 TESTOSTERONE UNDECANOATE Androgen Receptor agonist 4 FDA
CHEMBL1738889 ENOBOSARM Androgen Receptor modulator 3 Other PubMed
CHEMBL2105738 GALETERONE Androgen Receptor antagonist 3 Other PubMed PubMed
CHEMBL3183409 ARN-509 Androgen Receptor antagonist 3 Other PubMed
CHEMBL3545294 ODM-201 Androgen Receptor antagonist 3 Other PubMed
CHEMBL3545016 CB-03-01 Androgen Receptor antagonist 2 Other Other PubMed
CHEMBL3545092 CR 1447 Androgen Receptor agonist 2 Other
CHEMBL3545333 MK-0773 Androgen Receptor modulator 2 PubMed PubMed
CHEMBL37676 APC-100 Androgen Receptor antagonist 1 Other PubMed
CHEMBL467888 LGD-2941 Androgen Receptor modulator 1 PubMed
CHEMBL2346976 AZD3514 Androgen Receptor modulator 1 PubMed PubMed
CHEMBL3542265 LY2452473 Androgen Receptor modulator 1 PubMed
CHEMBL3545046 GSK2849466 Androgen Receptor modulator 1 Other
CHEMBL3545174 GSK2881078 Androgen Receptor modulator 1 Other
CHEMBL3545237 HE3235 Androgen Receptor modulator 1 PubMed
CHEMBL3545356 VK5211 Androgen Receptor modulator 1 Other PubMed PubMed
CHEMBL3545417 GLPG0492 Androgen Receptor modulator 1 Other PubMed
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000169083
Ensembl ENSG00000169083
GO Cellular Component GO:0000790 (nuclear chromatin)
GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005737 (cytoplasm)
GO:0005829 (cytosol)
GO:0043234 (protein complex)
GO Molecular Function GO:0000978 (RNA polymerase II core promoter proximal region sequence-specific DNA binding)
GO:0001077 (transcriptional activator activity, RNA polymerase II core promoter proximal region sequence-specific binding)
GO:0001085 (RNA polymerase II transcription factor binding)
GO:0003677 (DNA binding)
GO:0003682 (chromatin binding)
GO:0003700 (transcription factor activity, sequence-specific DNA binding)
GO:0004879 (RNA polymerase II transcription factor activity, ligand-activated sequence-specific DNA binding)
GO:0004882 (androgen receptor activity)
GO:0005102 (receptor binding)
GO:0005496 (steroid binding)
GO:0005497 (androgen binding)
GO:0005515 (protein binding)
GO:0008013 (beta-catenin binding)
GO:0008134 (transcription factor binding)
GO:0008270 (zinc ion binding)
GO:0008289 (lipid binding)
GO:0019899 (enzyme binding)
GO:0043565 (sequence-specific DNA binding)
GO:0044212 (transcription regulatory region DNA binding)
GO:0046872 (metal ion binding)
GO:0046983 (protein dimerization activity)
GO:0051117 (ATPase binding)
GO Biological Process GO:0006351 (transcription, DNA-templated)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006367 (transcription initiation from RNA polymerase II promoter)
GO:0006810 (transport)
GO:0007165 (signal transduction)
GO:0007267 (cell-cell signaling)
GO:0007548 (sex differentiation)
GO:0008283 (cell proliferation)
GO:0008284 (positive regulation of cell proliferation)
GO:0008285 (negative regulation of cell proliferation)
GO:0010628 (positive regulation of gene expression)
GO:0016049 (cell growth)
GO:0030521 (androgen receptor signaling pathway)
GO:0030522 (intracellular receptor signaling pathway)
GO:0030850 (prostate gland development)
GO:0042327 (positive regulation of phosphorylation)
GO:0043401 (steroid hormone mediated signaling pathway)
GO:0045597 (positive regulation of cell differentiation)
GO:0045720 (negative regulation of integrin biosynthetic process)
GO:0045726 (positive regulation of integrin biosynthetic process)
GO:0045893 (positive regulation of transcription, DNA-templated)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0045945 (positive regulation of transcription from RNA polymerase III promoter)
GO:0051092 (positive regulation of NF-kappaB transcription factor activity)
GO:0051259 (protein oligomerization)
GO:0090003 (regulation of establishment of protein localization to plasma membrane)
GO:2001237 (negative regulation of extrinsic apoptotic signaling pathway)
Wikipedia Androgen_receptor

Target Cross References - Protein

canSAR P10275
CGD Androgen insensitivity; Androgen insensitivity, partial
Human Protein Atlas ENSG00000169083
IntAct P10275
Guide to Pharmacology 628
Open Targets ENSG00000169083
PharmGKB PA57
Pharos P10275 (Tclin)
Reactome R-HSA-383280 (Nuclear Receptor transcription pathway.)
R-HSA-5625886 (Activated PKN1 stimulates transcription of AR (androgen receptor) regulated genes KLK2 and KLK3.)
UniProt A0A0B4J1T2 A2RUN2 B1AKD7 C0JKD3 C0JKD4 E7EVX6 P10275 Q9UD95

Target Cross References - Domain

InterPro IPR000536 (Nucl_hrmn_rcpt_lig-bd.)
IPR001103 (Andrgn_rcpt.)
IPR001628 (Znf_hrmn_rcpt.)
IPR013088 (Znf_NHR/GATA.)
Pfam PF00104 (Hormone_recep)
PF00105 (zf-C4)
PF02166 (Androgen_recep)

Target Cross References - Structure

PDBe 1E3G 1GS4 1T5Z 1T63 1T65 1XJ7 1XOW 1XQ3 1Z95 2AM9 2AMA 2AMB 2AO6 2AX6 2AX7 2AX8 2AX9 2AXA 2HVC 2OZ7 2PIO 2PIP 2PIQ 2PIR More...
CREDO 1E3G 1GS4 1T5Z 1T63 1T65 1XJ7 1XOW 1XQ3 1Z95 2AM9 2AMA 2AMB 2AO6 2AX6 2AX7 2AX8 2AX9 2AXA 2HVC 2OZ7 2PIO 2PIP 2PIQ 2PIR More...
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