AR

Summary

AR (androgen receptor, HGNC:644) is a protein-coding gene on chromosome Xq12, encoding Androgen receptor (P10275). Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues.

The androgen receptor gene is more than 90 kb long and codes for a protein that has 3 major functional domains: the N-terminal domain, DNA-binding domain, and androgen-binding domain. The protein functions as a steroid-hormone activated transcription factor. Upon binding the hormone ligand, the receptor dissociates from accessory proteins, translocates into the nucleus, dimerizes, and then stimulates transcription of androgen responsive genes. This gene contains 2 polymorphic trinucleotide repeat segments that encode polyglutamine and polyglycine tracts in the N-terminal transactivation domain of its protein. Expansion of the polyglutamine tract from the normal 9-34 repeats to the pathogenic 38-62 repeats causes spinal bulbar muscular atrophy (SBMA, also known as Kennedy’s disease). Mutations in this gene are also associated with complete androgen insensitivity (CAIS). Alternative splicing results in multiple transcript variants encoding different isoforms.

Source: NCBI Gene 367 — RefSeq curated summary.

At a glance

• Gene–disease (curated): Kennedy disease (Definitive, ClinGen) — +3 more curated relationships
• Clinical variants (ClinVar): 1,090 total — 251 pathogenic, 109 likely-pathogenic
• Druggable target: yes — 116 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_000044

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:644
Approved symbol	AR
Name	androgen receptor
Location	Xq12
Locus type	gene with protein product
Status	Approved
Aliases	AIS, NR3C4, SMAX1, HUMARA
Ensembl gene	ENSG00000169083
Ensembl biotype	protein_coding
OMIM	313700
Entrez	367

Gene structure

Transcript identifiers

Ensembl transcripts: 10 — 5 protein_coding, 4 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000374690, ENST00000396043, ENST00000396044, ENST00000504326, ENST00000513847, ENST00000514029, ENST00000612452, ENST00000613054, ENST00000853518, ENST00000853519

RefSeq mRNA: 5 — MANE Select: NM_000044 NM_000044, NM_001011645, NM_001348061, NM_001348063, NM_001348064

CCDS: CCDS14387, CCDS87754, CCDS87755

Canonical transcript exons

ENST00000374690 — 8 exons

Exon	Start	End
ENSE00001165458	67721833	67721963
ENSE00001165476	67711402	67711689
ENSE00001282597	67717478	67717622
ENSE00001316881	67722827	67722984
ENSE00001930911	67723686	67730619
ENSE00003606052	67643256	67643407
ENSE00003625235	67686010	67686126
ENSE00003901971	67544021	67546762

Expression profiles

Bgee: expression breadth ubiquitous, 250 present calls, max score 97.53.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 4.1307 / max 221.0612, expressed in 1026 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter ID	TPM avg	Samples expressed
196580	2.0469	746
196579	1.2313	636
196581	0.5429	245
196585	0.2294	101
196582	0.0801	28

Top tissues by expression

291 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
seminal vesicle	UBERON:0000998	97.53	gold quality
urethra	UBERON:0000057	96.69	gold quality
nipple	UBERON:0002030	96.13	gold quality
mammalian vulva	UBERON:0000997	94.97	gold quality
corpus epididymis	UBERON:0004359	94.70	gold quality
penis	UBERON:0000989	93.15	gold quality
caput epididymis	UBERON:0004358	92.58	gold quality
cauda epididymis	UBERON:0004360	90.91	gold quality
mammary duct	UBERON:0001765	90.78	gold quality
liver	UBERON:0002107	89.24	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	89.22	gold quality
buccal mucosa cell	CL:0002336	89.09	gold quality
saphenous vein	UBERON:0007318	88.92	gold quality
right lobe of liver	UBERON:0001114	87.87	gold quality
skin of hip	UBERON:0001554	87.47	gold quality
synovial joint	UBERON:0002217	87.40	gold quality
epithelium of mammary gland	UBERON:0003244	86.96	gold quality
mammary gland	UBERON:0001911	86.73	gold quality
calcaneal tendon	UBERON:0003701	86.66	gold quality
thoracic mammary gland	UBERON:0005200	86.65	gold quality
left ventricle myocardium	UBERON:0006566	85.78	gold quality
endocervix	UBERON:0000458	85.48	gold quality
heart right ventricle	UBERON:0002080	85.47	gold quality
prostate gland	UBERON:0002367	85.46	gold quality
tendon	UBERON:0000043	84.65	gold quality
fallopian tube	UBERON:0003889	84.36	gold quality
endometrium epithelium	UBERON:0004811	83.90	silver quality
ectocervix	UBERON:0012249	83.88	gold quality
vagina	UBERON:0000996	83.84	gold quality
vena cava	UBERON:0004087	83.75	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	no	0.00

Regulation

Is transcription factor: yes

JASPAR motifs

Motif	Name	Family
MA0007.2	AR	Steroid hormone receptors (NR3)

JASPAR matrix evidence (PMIDs): PMID:20943813

miRNA regulators (miRDB)

316 targeting AR, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-9-5P	100.00	72.28	2361
HSA-MIR-3924	100.00	72.09	2394
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-7110-3P	100.00	73.18	2486
HSA-MIR-6833-3P	100.00	70.63	3197
HSA-MIR-4768-5P	100.00	69.49	2861
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-6873-3P	100.00	71.42	2626
HSA-MIR-8485	100.00	77.57	4731
HSA-MIR-6867-5P	100.00	82.21	3464
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-5193	100.00	67.26	1744
HSA-MIR-4692	100.00	67.32	2066
HSA-MIR-30A-5P	100.00	76.31	3233
HSA-MIR-30B-5P	100.00	76.29	3248
HSA-MIR-30C-5P	100.00	76.29	3248
HSA-MIR-30D-5P	100.00	76.32	3233
HSA-MIR-30E-5P	100.00	76.32	3242
HSA-MIR-29A-3P	100.00	73.11	1835
HSA-MIR-29B-3P	100.00	73.18	1833
HSA-MIR-29C-3P	100.00	73.15	1833
HSA-MIR-656-3P	100.00	72.15	2788
HSA-MIR-196A-1-3P	99.99	72.15	2772
HSA-MIR-520G-5P	99.99	66.76	658
HSA-MIR-4534	99.99	66.58	1907
HSA-MIR-181A-5P	99.99	72.96	2995
HSA-MIR-181B-5P	99.99	72.97	2996

Literature-anchored findings (GeneRIF, showing 40)

• Androgens induce neuroprotection directly through the androgen receptor. (PMID:11389183)
• Almost all of the amino acids located at the 13-residue C-terminal end of the androgen receptor participate in its ligand binding function and consequently in its transcriptional activation. (PMID:11456479)
• androgen receptor and DXS15-134 markers show a high rate of discordance for germline X chromosome inactivation in patients with breast or ovarian cancer (PMID:11474658)
• Molecular studies performed on eight individuals with AIS were reported. Exon-specific polymerase chain reaction (PCR), single-strand conformation polymorphism, and sequencing analyses, were performed in exons 2 to 8 of the AR gene. (PMID:11587068)
• androgen receptor CAG repeats in both black and white patients do not appear to be a strong indicator of prostatic cancer risk (PMID:11720249)
• The aggregation and localization of the truncated form, with or without an expanded polyglutamine tract, is differentially controlled by Glucocorticoid receptor mutants. (PMID:11751688)
• These results demonstrate that activation of the human AR NTD by IL-6 was mediated through MAPK and STAT3 signal transduction pathways in LNCaP prostate cancer cells (PMID:11751884)
• The AR gene (CAG)n exhibits polymorphism among normal male population and the present work could serve as a basis for further exploration of its pathological and genetic significance. (PMID:11774215)
• The FXXLF motif mediates androgen receptor-specific interactions with coregulators (PMID:11779876)
• poor reproductive performance observed in women with PCOS may be due to the concomitant increase and elevations in endometrial AR (PMID:11804942)
• Domain interactions between coregulator ARA(70) and the androgen receptor (AR); structure activity relationship (PMID:11818501)
• Missense substitution at M807 is associated with androgen insensitivity syndrome (PMID:11818512)
• stained sections throughout male genital development documented the expression of AR and 5 alpha-reductase type 2 in the phallus. (PMID:11845321)
• can promote nuclear translocation of beta-catenin in LNCaP and PC3 prostate cancer cells (PMID:11856748)
• function inhibited by the reproductive orphan nuclear receptor DAX-1 (PMID:11875111)
• Two de novo mutations in the AR gene cause the complete androgen insensitivity syndrome in a pair of monozygotic twins. (PMID:11889162)
• Conformational analysis of the androgen receptor amino-terminal domain involved in transactivation. Influence of structure-stabilizing solutes and protein-protein interactions (PMID:11896058)
• role in blood pressure (PMID:11903314)
• Structural basis for the glucocorticoid response in a mutant human androgen receptor (PMID:11906285)
• presence of both the amino- and carboxyl-terminal domains in the AR is essential for the completion of a transcriptionally active form with coactivators and intranuclear compartmentalization common to the steroid hormone receptors (PMID:11923466)
• CAG/CAA repeat lengths in androgen receptor gene may provide useful marker for clinically significant prostate cancer (PMID:11927493)
• These results suggest a model for the functional coordination between the promoter and enhancer in which communication between these elements is established through shared coactivators in the AR transcription complex. (PMID:11931767)
• CAG polymorphic repeat lengths in androgen receptor gene among Japanese prostate cancer patients: potential predictor of prognosis after endocrine therapy. (PMID:11967956)
• regulation of androgen receptor by PI3 kinase (PMID:11971763)
• Results suggest that the conserved AR acetylation site contributes to a pathway governing prostate cancer cellular survival, as AR acetylation mutants are defective in MEKK1-induced apoptosis. (PMID:11971970)
• androgen receptor has a capacity to activate transcription in a ligand-independent manner (PMID:11981028)
• The binding of HuR, CP1, and CP2 to AR mRNA suggests a role for each of these proteins in the post-transcriptional regulation of AR expression in cancer cells. (PMID:12011088)
• major sites of AR phosphorylation (PMID:12015328)
• contribution of genetic polymorphism of oestrogen and androgen receptor (AR) genes in male infertility (PMID:12031042)
• activation function-1 domain of androgen receptor contributes to the interaction between subnuclear splicing factor compartment and nuclear receptor compartment (PMID:12039962)
• identification as a coactivator for the androgen receptor [p102 U5 small nuclear ribonucleoprotein particle-binding protein] (PMID:12039962)
• An androgen receptor gene mutation (E653K) in a family with congenital adrenal hyperplasia due to steroid 21-hydroxylase deficiency as well as in partial androgen insensitivity. (PMID:12050225)
• review of NH(2)-terminal and carboxyl-terminal interaction in the androgen receptor (PMID:12051960)
• Stabilization of androgen receptor protein is induced by agonist, not by antagonists. (PMID:12061774)
• significance for endocrine therapy in prostatic cancer (REVIEW) (PMID:12083956)
• the androgen receptor-CAG alleles may contribute to hepatocellular carcinoma predisposition among women through a mechanism different from that for men (PMID:12085360)
• Our study thus suggests a functional cooperation between AR and Stat5. (PMID:12089361)
• Polymorphisms within the gene are biomarkers for the development of benign prostatic hyperplasia and benign prostatic enlargement(SRD5A2) (PMID:12111704)
• DHT may play more important roles than testosterone in the regulation of androgen action in endometrial cancer and normal human endometrium, especially in the secretory phase, in which both AR and 5alpha-reductase are increased (PMID:12115497)
• Androgen Receptor requires proteasome activity in prostate tumor cells (PMID:12119296)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	ar	ENSDARG00000067976
mus_musculus	Ar	ENSMUSG00000046532
rattus_norvegicus	Ar	ENSRNOG00000005639
drosophila_melanogaster	ERR	FBGN0035849

Paralogs (8): PGR (ENSG00000082175), ESR1 (ENSG00000091831), NR3C1 (ENSG00000113580), ESRRB (ENSG00000119715), ESR2 (ENSG00000140009), NR3C2 (ENSG00000151623), ESRRA (ENSG00000173153), ESRRG (ENSG00000196482)

Protein

Protein identifiers

Androgen receptor — P10275 (reviewed: P10275)

Alternative names: Dihydrotestosterone receptor, Nuclear receptor subfamily 3 group C member 4

All UniProt accessions (6): A0A087WUX9, A0A087X1B6, A0A7I2PS51, E9PEG3, P10275, F5GZG9

UniProt curated annotations — full annotation on UniProt →

Function. Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription factor activity is modulated by bound coactivator and corepressor proteins like ZBTB7A that recruits NCOR1 and NCOR2 to the androgen response elements/ARE on target genes, negatively regulating androgen receptor signaling and androgen-induced cell proliferation. Transcription activation is also down-regulated by NR0B2. Activated, but not phosphorylated, by HIPK3 and ZIPK/DAPK3. Lacks the C-terminal ligand-binding domain and therefore constitutively regulates the transcription of a specific set of canonical AR-target genes, including PSA/KLK3 and TMPRSS2, independently of steroid hormones. However, some genes are differentially regulated by full-length AR (isoform 1) and isoform 3. Isoform 3-specific target genes may be regulated independently of FOXA1 expression. Lacks the C-terminal ligand-binding domain and may therefore constitutively activate the transcription of a specific set of genes independently of steroid hormones.

Subunit / interactions. Binds DNA as a homodimer. Part of a ternary complex containing AR, EFCAB6/DJBP and PARK7. Interacts with HIPK3 and NR0B2 in the presence of androgen. The ligand binding domain interacts with KAT7/HBO1 in the presence of dihydrotestosterone. Interacts with EFCAB6/DJBP, PQBP1, RANBP9, RBAK, SPDEF, SRA1, TGFB1I1 and RREB1. Interacts with ZMIZ1/ZIMP10 and ZMIZ2/ZMIP7 which both enhance its transactivation activity. Interacts with SLC30A9 and RAD54L2/ARIP4. Interacts with MACROD1 (via macro domain). Interacts via the ligand-binding domain with LXXLL and FXXLF motifs from NCOA1, NCOA2, NCOA3 and MAGEA11. Interacts (via nuclear receptor DNA binding domain and nuclear receptor ligand binding domain) with NCOA4. The AR N-terminal poly-Gln region binds Ran resulting in enhancement of AR-mediated transactivation. Ran-binding decreases as the poly-Gln length increases. Interacts with HIP1 (via coiled coil domain). Interacts (via ligand-binding domain) with TRIM68. Interacts with TNK2. Interacts with USP26. Interacts with RNF6. Interacts (regulated by RNF6 probably through polyubiquitination) with RNF14; regulates AR transcriptional activity. Interacts with PRMT2 and TRIM24. Interacts with RACK1. Interacts with RANBP10; this interaction enhances dihydrotestosterone-induced AR transcriptional activity. Interacts with PRPF6 in a hormone-independent way; this interaction enhances dihydrotestosterone-induced AR transcriptional activity. Interacts with STK4/MST1. Interacts with ZIPK/DAPK3. Interacts with LPXN. Interacts with MAK. Part of a complex containing AR, MAK and NCOA3. Interacts with CRY1. Interacts with CCAR1 and GATA2. Interacts with ZNF318. Interacts with BUD31. Interacts with ARID4A. Interacts with ARID4B. Interacts (via NR LBD domain) with ZBTB7A; the interaction is direct and androgen-dependent. Interacts with NCOR1. Interacts with NCOR2. Interacts with CRY2 in a ligand-dependent manner. Interacts (via NR LBD domain) with RWDD1; the interaction is direct and may stimulate AR activity.

Subcellular location. Nucleus. Cytoplasm.

Tissue specificity. Mainly expressed in heart and skeletal muscle. Expressed in basal and stromal cells of the prostate (at protein level).

Post-translational modifications. Sumoylated on Lys-388 (major) and Lys-521. Ubiquitinated. Deubiquitinated by USP26. ‘Lys-6’ and ‘Lys-27’-linked polyubiquitination by RNF6 modulates AR transcriptional activity and specificity. Phosphorylated in prostate cancer cells in response to several growth factors including EGF. Phosphorylation is induced by c-Src kinase (CSK). Tyr-535 is one of the major phosphorylation sites and an increase in phosphorylation and Src kinase activity is associated with prostate cancer progression. Phosphorylation by TNK2 enhances the DNA-binding and transcriptional activity and may be responsible for androgen-independent progression of prostate cancer. Phosphorylation at Ser-83 by CDK9 regulates AR promoter selectivity and cell growth. Phosphorylation by PAK6 leads to AR-mediated transcription inhibition. Palmitoylated by ZDHHC7 and ZDHHC21. Palmitoylation is required for plasma membrane targeting and for rapid intracellular signaling via ERK and AKT kinases and cAMP generation.

Disease relevance. Androgen insensitivity syndrome (AIS) [MIM:300068] An X-linked recessive form of pseudohermaphroditism due end-organ resistance to androgen. Affected males have female external genitalia, female breast development, blind vagina, absent uterus and female adnexa, and abdominal or inguinal testes, despite a normal 46,XY karyotype. The disease is caused by variants affecting the gene represented in this entry. Spinal and bulbar muscular atrophy X-linked 1 (SMAX1) [MIM:313200] An X-linked recessive form of spinal muscular atrophy. Spinal muscular atrophy refers to a group of neuromuscular disorders characterized by degeneration of the anterior horn cells of the spinal cord, leading to symmetrical muscle weakness and atrophy. SMAX1 occurs only in men. Age at onset is usually in the third to fifth decade of life, but earlier involvement has been reported. It is characterized by slowly progressive limb and bulbar muscle weakness with fasciculations, muscle atrophy, and gynecomastia. The disorder is clinically similar to classic forms of autosomal spinal muscular atrophy. The disease is caused by variants affecting the gene represented in this entry. Caused by trinucleotide CAG repeat expansion. In SMAX1 patients the number of Gln ranges from 38 to 62. Longer expansions result in earlier onset and more severe clinical manifestations of the disease. Prostate cancer, hereditary, X-linked 3 (HPCX3) [MIM:301120] A condition associated with familial predisposition to cancer of the prostate. Most prostate cancers are adenocarcinomas that develop in the acini of the prostatic ducts. Other rare histopathologic types of prostate cancer that occur in approximately 5% of patients include small cell carcinoma, mucinous carcinoma, prostatic ductal carcinoma, transitional cell carcinoma, squamous cell carcinoma, basal cell carcinoma, adenoid cystic carcinoma (basaloid), signet-ring cell carcinoma and neuroendocrine carcinoma. Disease susceptibility is associated with variants affecting the gene represented in this entry. Defects in AR may play a role in metastatic prostate cancer. The mutated receptor stimulates prostate growth and metastases development despite of androgen ablation. This treatment can reduce primary and metastatic lesions probably by inducing apoptosis of tumor cells when they express the wild-type receptor. Androgen insensitivity, partial (PAIS) [MIM:312300] A disorder that is characterized by hypospadias, hypogonadism, gynecomastia, genital ambiguity, normal XY karyotype, and a pedigree pattern consistent with X-linked recessive inheritance. Some patients present azoospermia or severe oligospermia without other clinical manifestations. The disease is caused by variants affecting the gene represented in this entry. Hypospadias 1, X-linked (HYSP1) [MIM:300633] A common malformation in which the urethra opens on the ventral side of the penis, due to developmental arrest of urethral fusion. The opening can be located glandular, penile, or even more posterior in the scrotum or perineum. Hypospadias is a feature of several syndromic disorders, including the androgen insensitivity syndrome and Opitz syndrome. The disease is caused by variants affecting the gene represented in this entry.

Activity regulation. AIM-100 (4-amino-5,6-biaryl-furo[2,3-d]pyrimidine) suppresses TNK2-mediated phosphorylation at Tyr-269. Inhibits the binding of the Tyr-269 phosphorylated form to androgen-responsive enhancers (AREs) and its transcriptional activity.

Domain organisation. Composed of three domains: a modulating N-terminal domain, a DNA-binding domain and a C-terminal ligand-binding domain. In the presence of bound steroid the ligand-binding domain interacts with the N-terminal modulating domain, and thereby activates AR transcription factor activity. Agonist binding is required for dimerization and binding to target DNA. The transcription factor activity of the complex formed by ligand-activated AR and DNA is modulated by interactions with coactivator and corepressor proteins. Interaction with RANBP9 is mediated by both the N-terminal domain and the DNA-binding domain. Interaction with EFCAB6/DJBP is mediated by the DNA-binding domain.

Polymorphism. The poly-Gln region of AR is highly polymorphic and the number of Gln varies in the population (from 17 to 26). A smaller size of the poly-Gln region may be associated with the development of prostate cancer. Long poly-Gln alleles (>23) may be associated with higher testosterone levels and severe clinical outcome in COVID-19 disease. The poly-Gly region of AR is polymorphic and ranges from 24 to 31 Gly. A poly-Gly region shorter or equal to 23 may be associated with the development of androgenetic alopecia.

Miscellaneous. In the absence of ligand, steroid hormone receptors are thought to be weakly associated with nuclear components; hormone binding greatly increases receptor affinity. The hormone-receptor complex appears to recognize discrete DNA sequences upstream of transcriptional start sites. Transcriptional activity is enhanced by binding to RANBP9. The level of tyrosine phosphorylation may serve as a diagnostic tool to predict patient outcome in response to hormone-ablation therapy. Inhibition of tyrosine phosphorylation may be an effective intervention target for hormone-refractory prostate cancer. Minor isoform up-regulated in prostate cancer cells. Minor isoform identified in prostate cancer cells.

Similarity. Belongs to the nuclear hormone receptor family. NR3 subfamily.

Isoforms (4)

UniProt ID	Names	Canonical?
P10275-1	1, AR-B	yes
P10275-2	2, AR-A, Variant AR45
P10275-3	3, AR3, AR-V7
P10275-4	4, AR4

RefSeq proteins (4): NP_000035, NP_001011645, NP_001334990, NP_001334993 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000536	Nucl_hrmn_rcpt_lig-bd	Domain
IPR001103	Andrgn_rcpt	Family
IPR001628	Znf_hrmn_rcpt	Domain
IPR013088	Znf_NHR/GATA	Homologous_superfamily
IPR035500	NHR-like_dom_sf	Homologous_superfamily
IPR050200	Nuclear_hormone_rcpt_NR3	Family

Pfam: PF00104, PF00105, PF02166

UniProt features (310 total): sequence variant 219, mutagenesis site 19, modified residue 15, helix 13, region of interest 8, sequence conflict 7, strand 6, splice variant 6, cross-link 4, compositionally biased region 3, binding site 3, site 2, zinc finger region 2, chain 1, domain 1, DNA-binding region 1

Structure

Experimental structures (PDB)

95 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
8E1A	X-RAY DIFFRACTION	1.2
7ZTZ	X-RAY DIFFRACTION	1.4
4OHA	X-RAY DIFFRACTION	1.42
5V8Q	X-RAY DIFFRACTION	1.44
2AX6	X-RAY DIFFRACTION	1.5
3L3X	X-RAY DIFFRACTION	1.55
8FH0	X-RAY DIFFRACTION	1.59
8FH2	X-RAY DIFFRACTION	1.59
8FGZ	X-RAY DIFFRACTION	1.61
2AM9	X-RAY DIFFRACTION	1.64
2AX9	X-RAY DIFFRACTION	1.65
2PNU	X-RAY DIFFRACTION	1.65
3B66	X-RAY DIFFRACTION	1.65
1T65	X-RAY DIFFRACTION	1.66
7ZU1	X-RAY DIFFRACTION	1.68
8FH1	X-RAY DIFFRACTION	1.69
2AX8	X-RAY DIFFRACTION	1.7
3RLL	X-RAY DIFFRACTION	1.7
3V49	X-RAY DIFFRACTION	1.7
7ZU2	X-RAY DIFFRACTION	1.74
2AMB	X-RAY DIFFRACTION	1.75
2PIT	X-RAY DIFFRACTION	1.76
1XOW	X-RAY DIFFRACTION	1.8
1Z95	X-RAY DIFFRACTION	1.8
2AXA	X-RAY DIFFRACTION	1.8
2OZ7	X-RAY DIFFRACTION	1.8
2PIP	X-RAY DIFFRACTION	1.8
2Q7K	X-RAY DIFFRACTION	1.8
3B5R	X-RAY DIFFRACTION	1.8
3B65	X-RAY DIFFRACTION	1.8

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P10275-F1	58.85	0.29

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (2): 721 (interaction with coactivator lxxl and fxxfy motifs); 898 (interaction with coactivator fxxlf and fxxfy motifs)

Ligand- & substrate-binding residues (3): 706; 753; 878

Post-translational modifications (19): 83, 96, 225, 258, 269, 309, 348, 359, 364, 365, 395, 535, 552, 651, 916, 388, 521, 846, 848

Mutagenesis-validated functional residues (19):

Position	Phenotype
83	reduced cell growth.
225	decrease of csk-induced phosphorylation.
269	decrease of csk-induced phosphorylation and phosphorylation by tnk2. complete loss of tnk2-dependent phosphorylation; wh
309	decrease of csk-induced phosphorylation.
348	decrease of csk-induced phosphorylation.
359	decrease of csk-induced phosphorylation.
364	decrease of csk-induced phosphorylation.
365	decrease of csk-induced phosphorylation and phosphorylation by tnk2. complete loss of tnk2-dependent phosphorylation; wh
395	decrease of csk-induced phosphorylation.
535	greatest decrease of csk-induced phosphorylation and inhibition of transcriptional activity induced by egf.
552	decrease in csk-induced phosphorylation.
702	alters receptor specificity, so that transcription is activated by the antiandrogen cyproterone acetate.
721	loss of transcription activation in the presence of androgen and of interaction with ncoa2.
742	strongly decreased transcription activation in the presence of androgen.
846	prevents ubiquitination by rnf6. prevents ar transcriptional activation by rnf14 in absence of hormone.
848	partially prevents ubiquitination by rnf6.
898	reduced transcription activation in the presence of androgen.
898	loss of transcription activation in the presence of androgen.
916	decrease in csk-induced phosphorylation.

Function

Pathways and Gene Ontology

Reactome pathways

23 pathways

ID	Pathway
R-HSA-3371497	HSP90 chaperone cycle for steroid hormone receptors (SHR) in the presence of ligand
R-HSA-383280	Nuclear Receptor transcription pathway
R-HSA-4090294	SUMOylation of intracellular receptors
R-HSA-5625886	Activated PKN1 stimulates transcription of AR (androgen receptor) regulated genes KLK2 and KLK3
R-HSA-5689880	Ub-specific processing proteases
R-HSA-8940973	RUNX2 regulates osteoblast differentiation
R-HSA-162582	Signal Transduction
R-HSA-194315	Signaling by Rho GTPases
R-HSA-195258	RHO GTPase Effectors
R-HSA-212436	Generic Transcription Pathway
R-HSA-2262752	Cellular responses to stress
R-HSA-2990846	SUMOylation
R-HSA-3108232	SUMO E3 ligases SUMOylate target proteins
R-HSA-392499	Metabolism of proteins
R-HSA-5625740	RHO GTPases activate PKNs
R-HSA-5688426	Deubiquitination
R-HSA-597592	Post-translational protein modification
R-HSA-73857	RNA Polymerase II Transcription
R-HSA-74160	Gene expression (Transcription)
R-HSA-8878166	Transcriptional regulation by RUNX2
R-HSA-8941326	RUNX2 regulates bone development
R-HSA-8953897	Cellular responses to stimuli
R-HSA-9716542	Signaling by Rho GTPases, Miro GTPases and RHOBTB3

MSigDB gene sets: 613 (showing top): GSE45365_CTRL_VS_MCMV_INFECTION_NK_CELL_UP, GSE45365_NK_CELL_VS_CD8A_DC_UP, GOBP_NEGATIVE_REGULATION_OF_EPITHELIAL_CELL_PROLIFERATION, GOBP_MORPHOGENESIS_OF_AN_EPITHELIUM, GOBP_SINGLE_FERTILIZATION, MODULE_92, GOBP_POSITIVE_REGULATION_OF_REPRODUCTIVE_PROCESS, GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, GOBP_EPITHELIUM_DEVELOPMENT, GOBP_MAMMARY_GLAND_MORPHOGENESIS, FARMER_BREAST_CANCER_CLUSTER_7, GOBP_GLAND_MORPHOGENESIS, GOBP_REGULATION_OF_BLOOD_PRESSURE, YAGI_AML_WITH_INV_16_TRANSLOCATION, GOBP_REGULATION_OF_MORPHOGENESIS_OF_A_BRANCHING_STRUCTURE

GO Biological Process (62): negative regulation of transcription by RNA polymerase II (GO:0000122), MAPK cascade (GO:0000165), in utero embryonic development (GO:0001701), regulation of systemic arterial blood pressure (GO:0003073), epithelial cell morphogenesis (GO:0003382), transcription by RNA polymerase II (GO:0006366), signal transduction (GO:0007165), cell-cell signaling (GO:0007267), spermatogenesis (GO:0007283), single fertilization (GO:0007338), positive regulation of cell population proliferation (GO:0008284), negative regulation of cell population proliferation (GO:0008285), male gonad development (GO:0008584), positive regulation of gene expression (GO:0010628), male somatic sex determination (GO:0019102), estrogen receptor signaling pathway (GO:0030520), androgen receptor signaling pathway (GO:0030521), intracellular receptor signaling pathway (GO:0030522), positive regulation of intracellular estrogen receptor signaling pathway (GO:0033148), Leydig cell differentiation (GO:0033327), multicellular organism growth (GO:0035264), positive regulation of MAPK cascade (GO:0043410), positive regulation of insulin-like growth factor receptor signaling pathway (GO:0043568), positive regulation of cell differentiation (GO:0045597), positive regulation of integrin biosynthetic process (GO:0045726), positive regulation of DNA-templated transcription (GO:0045893), positive regulation of transcription by RNA polymerase II (GO:0045944), positive regulation of transcription by RNA polymerase III (GO:0045945), insulin-like growth factor receptor signaling pathway (GO:0048009), regulation of developmental growth (GO:0048638), animal organ formation (GO:0048645), male genitalia morphogenesis (GO:0048808), epithelial cell proliferation (GO:0050673), negative regulation of epithelial cell proliferation (GO:0050680), prostate induction (GO:0060514), morphogenesis of an epithelial fold (GO:0060571), lateral sprouting involved in mammary gland duct morphogenesis (GO:0060599), prostate gland growth (GO:0060736), prostate gland epithelium morphogenesis (GO:0060740), epithelial cell differentiation involved in prostate gland development (GO:0060742)

GO Molecular Function (30): transcription cis-regulatory region binding (GO:0000976), RNA polymerase II transcription regulatory region sequence-specific DNA binding (GO:0000977), RNA polymerase II cis-regulatory region sequence-specific DNA binding (GO:0000978), RNA polymerase II core promoter sequence-specific DNA binding (GO:0000979), DNA-binding transcription factor activity, RNA polymerase II-specific (GO:0000981), RNA polymerase II general transcription initiation factor binding (GO:0001091), transcription coactivator binding (GO:0001223), DNA-binding transcription activator activity, RNA polymerase II-specific (GO:0001228), chromatin binding (GO:0003682), DNA-binding transcription factor activity (GO:0003700), nuclear steroid receptor activity (GO:0003707), nuclear receptor activity (GO:0004879), signaling receptor binding (GO:0005102), steroid binding (GO:0005496), androgen binding (GO:0005497), beta-catenin binding (GO:0008013), zinc ion binding (GO:0008270), enzyme binding (GO:0019899), estrogen response element binding (GO:0034056), ATPase binding (GO:0051117), molecular adaptor activity (GO:0060090), RNA polymerase II-specific DNA-binding transcription factor binding (GO:0061629), POU domain binding (GO:0070974), molecular condensate scaffold activity (GO:0140693), DNA binding (GO:0003677), protein binding (GO:0005515), lipid binding (GO:0008289), sequence-specific DNA binding (GO:0043565), metal ion binding (GO:0046872), sequence-specific double-stranded DNA binding (GO:1990837)

GO Cellular Component (8): chromatin (GO:0000785), nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), cytosol (GO:0005829), plasma membrane (GO:0005886), nuclear speck (GO:0016607), protein-containing complex (GO:0032991)

Reactome top-level categories

Rollup of top-15 pathways:

Category	Pathways
Generic Transcription Pathway	2
Post-translational protein modification	2
Cellular responses to stress	1
SUMO E3 ligases SUMOylate target proteins	1
RHO GTPases activate PKNs	1
Deubiquitination	1
RUNX2 regulates bone development	1
Signaling by Rho GTPases, Miro GTPases and RHOBTB3	1
Signaling by Rho GTPases	1
RNA Polymerase II Transcription	1
Cellular responses to stimuli	1
SUMOylation	1
RHO GTPase Effectors	1
Metabolism of proteins	1
Gene expression (Transcription)	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
RNA polymerase II transcription regulatory region sequence-specific DNA binding	4
cellular anatomical structure	4
nuclear receptor-mediated steroid hormone signaling pathway	3
protein binding	3
regulation of transcription by RNA polymerase II	2
cell communication	2
signaling	2
developmental process involved in reproduction	2
cell population proliferation	2
regulation of cell population proliferation	2
transcription cis-regulatory region binding	2
DNA-binding transcription factor activity, RNA polymerase II-specific	2
transcription by RNA polymerase II	1
negative regulation of DNA-templated transcription	1
intracellular signaling cassette	1
chordate embryonic development	1
regulation of blood pressure	1
cell morphogenesis	1
epithelial cell development	1
DNA-templated transcription	1
cellular process	1
regulation of cellular process	1
cellular response to stimulus	1
male gamete generation	1
fertilization	1
positive regulation of cellular process	1
negative regulation of cellular process	1
gonad development	1
development of primary male sexual characteristics	1
gene expression	1
regulation of gene expression	1
positive regulation of macromolecule biosynthetic process	1
somatic sex determination	1
male sex determination	1
intracellular signal transduction	1
estrogen receptor signaling pathway	1
positive regulation of intracellular steroid hormone receptor signaling pathway	1
regulation of intracellular estrogen receptor signaling pathway	1
male gonad development	1
cell differentiation	1

Protein interactions and networks

STRING

5158 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
AR	HSP90AA1	P07900	990
AR	HSP90AB1	P08238	990
AR	FOXA1	P55317	987
AR	KDM1A	O60341	982
AR	MDM2	Q00987	980
AR	ESR1	P03372	979
AR	CTNNB1	P35222	968
AR	NCOA4	Q13772	964
AR	SRC	P12931	944
AR	EZH2	Q15910	942
AR	KLK3	P07288	935
AR	BRD4	O60885	929
AR	NKX3-1	Q99801	917
AR	NCOA2	Q15596	906
AR	PAK6	Q9NQU5	903

IntAct

514 interactions, top by confidence:

A	B	Type	Score
AR		psi-mi:“MI:0914”(association)	0.920
	AR	psi-mi:“MI:0914”(association)	0.920
	AR	psi-mi:“MI:0915”(physical association)	0.920
AR		psi-mi:“MI:0915”(physical association)	0.920
AR		psi-mi:“MI:0914”(association)	0.890
AR	CTNNB1	psi-mi:“MI:0915”(physical association)	0.890
CTNNB1	AR	psi-mi:“MI:0407”(direct interaction)	0.890
AR		psi-mi:“MI:0915”(physical association)	0.890
	AR	psi-mi:“MI:0915”(physical association)	0.890
AR	CTNNB1	psi-mi:“MI:0403”(colocalization)	0.890
CTNNB1	AR	psi-mi:“MI:0914”(association)	0.890
AR	CTNNB1	psi-mi:“MI:0914”(association)	0.890
MYCN	AURKA	psi-mi:“MI:0914”(association)	0.830
FKBP4	HSP90AB1	psi-mi:“MI:0914”(association)	0.790

BioGRID (1728): RNF6 (Affinity Capture-Western), AR (Biochemical Activity), USP12 (Affinity Capture-Western), WHSC1 (Affinity Capture-Western), SPOP (Affinity Capture-Western), DAPK3 (Co-localization), TSG101 (Co-localization), AATF (Co-localization), AR (Co-localization), AR (Co-localization), AR (Co-localization), AR (Affinity Capture-Western), SPOP (Reconstituted Complex), TAF1 (Two-hybrid), TAF1 (Reconstituted Complex)

ESM2 similar proteins: A1L020, A1L3F4, A7X8B3, A7X8B5, A7X8B7, A7X8B9, A7X8C2, A7X8C4, A7X8C7, A7X8C9, A7X8D2, A7X8D4, A7XW25, O97775, O97776, O97952, O97960, P06401, P10275, P84550, P84551, P89463, Q01JD1, Q05A36, Q0VDT2, Q3UE17, Q5PQQ7, Q5U5Q3, Q69Z36, Q6QT55, Q6ZK57, Q6ZN04, Q71FD5, Q7RTV3, Q7TSJ6, Q7XQN1, Q7XT42, Q84SL2, Q86XN8, Q8BQ89

Diamond homologs: A7X8B3, A7X8B5, A7X8B7, A7X8B9, A7X8C2, A7X8C4, A7X8C7, A7X8C9, A7X8D2, A7X8D4, A7XW16, A7XW20, A7XW25, O08537, O08580, O13012, O13186, O46567, O73673, O95718, O97775, O97776, O97952, O97960, P03372, P04150, P06186, P06211, P06212, P06401, P06536, P06537, P07812, P08235, P10275, P11474, P11475, P15207, P16058, P19091

SIGNOR signaling

114 interactions.

A	Effect	B	Mechanism
NCOR2	down-regulates	AR	acetylation
AR	up-regulates	NR5A1	binding
NR0B2	down-regulates	AR	binding
AR	“down-regulates quantity by repression”	CTNNB1	“transcriptional regulation”
ERBB3	“up-regulates quantity by expression”	AR	“transcriptional regulation”
HIP1	“down-regulates quantity by repression”	AR	“transcriptional regulation”
PKN1	up-regulates	AR	phosphorylation
AKT1	down-regulates	AR	phosphorylation
CDK7	down-regulates	AR	phosphorylation
CDK1	up-regulates	AR	phosphorylation
CDK5	up-regulates	AR	phosphorylation
MAPK1	down-regulates	AR	phosphorylation
DDX5	up-regulates	AR	binding
NSD2	up-regulates	AR	binding
TRIM24	up-regulates	AR	binding
(2S)-3-(4-acetamidophenoxy)-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide	up-regulates	AR	“chemical activation”
N-[4-cyano-3-(trifluoromethyl)phenyl]-3-(4-fluorophenyl)sulfonyl-2-hydroxy-2-methylpropanamide	down-regulates	AR	“chemical inhibition”
“cyproterone acetate”	down-regulates	AR	“chemical inhibition”
enzalutamide	down-regulates	AR	“chemical inhibition”
nilutamide	down-regulates	AR	“chemical inhibition”
FER	up-regulates	AR	phosphorylation
ENOBOSARM	up-regulates	AR	“chemical activation”
TBL1XR1	up-regulates	AR	binding
AKT	down-regulates	AR	phosphorylation
ERK1/2	down-regulates	AR	phosphorylation
NCOA2	“up-regulates activity”	AR	binding
17beta-hydroxy-5alpha-androstan-3-one	up-regulates	AR	“chemical activation”
HSP90AB1	“up-regulates activity”	AR	binding
HSP90AA1	“up-regulates activity”	AR	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 68 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
R-HSA-1368082	5	58.5×	6e-07
Activation of HOX genes during differentiation	6	43.2×	2e-07
Epigenetic regulation of adipogenesis genes by MLL3 and MLL4 complexes	12	42.4×	1e-14
Epigenetic regulation of gene expression by MLL3 and MLL4 complexes	13	42.0×	1e-15
BMAL1:CLOCK,NPAS2 activates circadian expression	5	34.7×	7e-06
RORA,B,C and NR1D1 (REV-ERBA) regulate gene expression	5	33.4×	7e-06
Epigenetic regulation by WDR5-containing histone modifying complexes	13	32.9×	1e-14
Regulation of cholesterol biosynthesis by SREBP (SREBF)	6	31.2×	1e-06

GO biological processes:

GO term	Partners	Fold	FDR
regulation of androgen receptor signaling pathway	5	77.4×	1e-06
positive regulation of erythrocyte differentiation	5	39.9×	2e-05
positive regulation of double-strand break repair via homologous recombination	5	29.9×	6e-05
positive regulation of transcription elongation by RNA polymerase II	5	23.5×	2e-04
positive regulation of miRNA transcription	5	22.7×	2e-04
response to estradiol	6	18.6×	7e-05
cellular response to hydrogen peroxide	5	18.3×	4e-04
fat cell differentiation	5	14.2×	1e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

1090 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	251
Likely pathogenic	109
Uncertain significance	203
Likely benign	288
Benign	106

Top pathogenic / likely-pathogenic (30)

Variant ID	HGVS	Classification
1068775	NM_000044.6(AR):c.2225G>T (p.Trp742Leu)	Pathogenic
1071361	NC_000023.10:g.(?66905832)(66905988_?)del	Pathogenic
1071362	NC_000023.10:g.(?66863078)(66943703_?)del	Pathogenic
1072748	NM_000044.6(AR):c.1737del (p.Cys580fs)	Pathogenic
1076800	NM_000044.6(AR):c.1063G>T (p.Glu355Ter)	Pathogenic
1202584	NM_000044.6(AR):c.2607+2T>G	Pathogenic
1202585	NM_000044.6(AR):c.2657A>T (p.His886Leu)	Pathogenic
1244244	NM_000044.6(AR):c.2486A>T (p.Asp829Val)	Pathogenic
1298359	NM_000044.6(AR):c.2255G>A (p.Trp752Ter)	Pathogenic
1298364	NM_000044.6(AR):c.1567G>T (p.Glu523Ter)	Pathogenic
1298367	NM_000044.6(AR):c.175C>T (p.Gln59Ter)	Pathogenic
1338498	NM_000044.6(AR):c.675_678del (p.Asn224_Tyr225insTer)	Pathogenic
1341693	NM_000044.6(AR):c.2226G>A (p.Trp742Ter)	Pathogenic
1342730	NM_000044.6(AR):c.2494C>T (p.Arg832Ter)	Pathogenic
1344487	NM_000044.6(AR):c.2126G>A (p.Gly709Glu)	Pathogenic
1344505	NM_000044.6(AR):c.2407dup (p.Gln803fs)	Pathogenic
1394063	NM_000044.6(AR):c.2319_2321dup (p.Tyr774Ter)	Pathogenic
1410848	NM_000044.6(AR):c.1477C>T (p.Gln493Ter)	Pathogenic
1421027	NM_000044.6(AR):c.358C>T (p.Gln120Ter)	Pathogenic
1437090	NM_000044.6(AR):c.1885+2T>G	Pathogenic
1454388	NC_000023.10:g.(?66941655)(66943683_?)del	Pathogenic
1454419	NM_000044.6(AR):c.1707del (p.Cys570fs)	Pathogenic
1454671	NM_000044.6(AR):c.829_833dup (p.Val279fs)	Pathogenic
1455502	NM_000044.6(AR):c.2512G>T (p.Glu838Ter)	Pathogenic
1460010	NC_000023.10:g.(?66931224)(66931551_?)del	Pathogenic
1460367	NM_000044.6(AR):c.2515C>A (p.Leu839Ile)	Pathogenic
1470535	NM_000044.6(AR):c.1A>T (p.Met1Leu)	Pathogenic
151774	GRCh38/hg38 Xq12(chrX:67532311-68353901)x1	Pathogenic
1518028	NM_000044.6(AR):c.2750del (p.Phe917fs)	Pathogenic
1526808	GRCh37/hg19 Xq12-13.1(chrX:65734663-68081523)	Pathogenic

SpliceAI

0 predictions. Top by Δscore:

AlphaMissense

5978 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
X:67643317:T:A	C560S	1.000
X:67643317:T:C	C560R	1.000
X:67643317:T:G	C560G	1.000
X:67643318:G:A	C560Y	1.000
X:67643318:G:C	C560S	1.000
X:67643318:G:T	C560F	1.000
X:67643319:C:G	C560W	1.000
X:67643321:T:C	L561P	1.000
X:67643324:T:A	I562N	1.000
X:67643324:T:C	I562T	1.000
X:67643324:T:G	I562S	1.000
X:67643326:T:A	C563S	1.000
X:67643326:T:C	C563R	1.000
X:67643326:T:G	C563G	1.000
X:67643327:G:A	C563Y	1.000
X:67643327:G:C	C563S	1.000
X:67643327:G:T	C563F	1.000
X:67643328:T:G	C563W	1.000
X:67643332:G:C	D565H	1.000
X:67643333:A:C	D565A	1.000
X:67643333:A:T	D565V	1.000
X:67643339:C:A	A567D	1.000
X:67643342:C:A	S568Y	1.000
X:67643342:C:T	S568F	1.000
X:67643344:G:A	G569R	1.000
X:67643344:G:C	G569R	1.000
X:67643344:G:T	G569W	1.000
X:67643345:G:A	G569E	1.000
X:67643345:G:T	G569V	1.000
X:67643347:T:C	C570R	1.000

dbSNP variants (sampled 300 via entrez): RS1000005499 (X:67602006 T>C), RS1000060358 (X:67654094 A>G), RS1000064938 (X:67610971 C>G), RS1000076103 (X:67725605 G>A), RS1000083410 (X:67720370 T>A), RS1000120379 (X:67548815 C>A), RS1000141604 (X:67665017 C>A), RS1000150253 (X:67639265 T>C), RS1000206476 (X:67573398 T>A), RS1000274763 (X:67613057 C>G,T), RS1000284696 (X:67580632 A>C), RS1000309845 (X:67707931 G>A,T), RS1000336142 (X:67706198 T>C), RS1000399851 (X:67581237 A>G), RS1000405296 (X:67668474 T>C)

Disease associations

OMIM: gene MIM:313700 | disease phenotypes: MIM:313200, MIM:300068, MIM:167000, MIM:300633, MIM:307300, MIM:312100, MIM:312300, MIM:301120, MIM:176807, MIM:400044

GenCC curated gene-disease

Disease	Classification	Inheritance
androgen insensitivity syndrome	Definitive	X-linked
Kennedy disease	Definitive	X-linked
partial androgen insensitivity syndrome	Strong	X-linked
complete androgen insensitivity syndrome	Supportive	X-linked

ClinGen Gene-Disease Validity (1)

Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.

Disease	Classification	Inheritance
Kennedy disease	Definitive	XL

Mondo (15): Kennedy disease (MONDO:0010735), androgen insensitivity syndrome (MONDO:0019154), ovarian cancer (MONDO:0008170), male infertility (MONDO:0005372), prostate cancer (MONDO:0008315), hypospadias 1, X-linked (MONDO:0010384), partial androgen insensitivity syndrome (MONDO:0010720), prostate cancer, hereditary, X-linked 3 (MONDO:0971170), primary ovarian failure (MONDO:0005387), complete androgen insensitivity syndrome (MONDO:0021023), prostate cancer, hereditary (MONDO:0700275), disorder of sexual differentiation (MONDO:0002145), posterior hypospadias (MONDO:0019848), Castleman-Kojima disease (MONDO:0018702), 46,XY complete gonadal dysgenesis (MONDO:0010765)

Orphanet (13): Kennedy disease (Orphanet:481), Androgen insensitivity syndrome (Orphanet:754), Complete androgen insensitivity syndrome (Orphanet:99429), Rare ovarian cancer (Orphanet:213500), Familial prostate cancer (Orphanet:1331), OBSOLETE: Familial hypospadias (Orphanet:440), Partial androgen insensitivity syndrome (Orphanet:90797), Male infertility with azoospermia or oligozoospermia due to single gene mutation (Orphanet:399805), Difference of sex development (Orphanet:90771), Non-syndromic posterior hypospadias (Orphanet:95706), TAFRO syndrome (Orphanet:457077), 46,XY complete gonadal dysgenesis (Orphanet:242), NON RARE IN EUROPE: Primary ovarian failure (Orphanet:619)

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

0 associations (top):

MeSH disease descriptors (11)

Descriptor	Name	Tree numbers
D013734	Androgen-Insensitivity Syndrome	C12.050.351.875.253.096.500; C12.200.706.316.096.500; C12.800.316.096.500; C16.131.939.316.096.500; C16.320.322.061; C19.391.119.096.500
D055534	Bulbo-Spinal Atrophy, X-Linked	C10.228.854.468.399; C10.574.500.175; C10.574.562.500.374; C10.668.467.500.186; C16.320.322.076; C16.320.400.100
D012734	Disorders of Sex Development	C12.050.351.875.253; C12.200.706.316; C12.800.316; C16.131.939.316; C19.391.119
D006061	Gonadal Dysgenesis, 46,XY	C12.050.351.875.253.096.687; C12.050.351.875.253.309.388; C12.200.706.316.096.687; C12.200.706.316.309.388; C12.800.316.096.687; C12.800.316.309.388; C16.131.939.316.096.687; C16.131.939.316.309.388; C19.391.119.096.687; C19.391.119.309.388
D007248	Infertility, Male	C12.100.500.430; C12.100.750.700; C12.200.294.430
D010051	Ovarian Neoplasms	C04.588.322.455; C12.050.351.500.056.630.705; C12.050.351.937.418.685; C12.100.250.056.630.705; C12.900.418.685; C19.344.410; C19.391.630.705
D016649	Primary Ovarian Insufficiency	C12.050.351.500.056.630.750; C12.100.250.056.630.750; C19.391.630.750
D011471	Prostatic Neoplasms	C04.588.945.440.770; C12.100.500.260.750; C12.100.500.565.625; C12.200.294.260.750; C12.200.294.565.625; C12.200.758.409.750; C12.900.619.750
C567482	Hypospadias 1, X-Linked (supp.)
C538435	Lubs syndrome (supp.)
C537243	Prostate cancer, familial (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (7): CHEMBL1871 (SINGLE PROTEIN), CHEMBL4296118 (PROTEIN-PROTEIN INTERACTION), CHEMBL4523653 (PROTEIN-PROTEIN INTERACTION), CHEMBL4523684 (PROTEIN-PROTEIN INTERACTION), CHEMBL4523730 (PROTEIN-PROTEIN INTERACTION), CHEMBL5169084 (PROTEIN-PROTEIN INTERACTION), CHEMBL6193822 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

116 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 446,209 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL103	PROGESTERONE	4	162,141
CHEMBL1082407	ENZALUTAMIDE	4	9,652
CHEMBL1091	HYDROCORTISONE ACETATE	4	45,061
CHEMBL1095097	EPLERENONE	4	13,067
CHEMBL110691	CHLORMADINONE ACETATE	4	9,747
CHEMBL1112	ARIPIPRAZOLE	4	24,205
CHEMBL1161	MOMETASONE FUROATE	4	25,884
CHEMBL1170	TESTOSTERONE PROPIONATE	4	17,619
CHEMBL1200430	ESTRADIOL ACETATE	4	1,114
CHEMBL1200436	OXANDROLONE	4	5,232
CHEMBL1200500	BECLOMETHASONE DIPROPIONATE	4	29,239
CHEMBL1200545	DIFLORASONE DIACETATE	4	20,278
CHEMBL1200624	ETHYNODIOL DIACETATE	4	5,941
CHEMBL1200845	HALCINONIDE	4	22,539
CHEMBL1200853	DYDROGESTERONE	4	4,463
CHEMBL1200877	FLUMETHASONE PIVALATE	4	6,132
CHEMBL1200908	HALOBETASOL PROPIONATE	4	10,126
CHEMBL1200973	ESTRADIOL CYPIONATE	4	4,089
CHEMBL1200975	CLOCORTOLONE PIVALATE	4	11,614
CHEMBL1201012	FLURANDRENOLIDE	4	18,066
CHEMBL1201139	MEGESTROL ACETATE	4
CHEMBL1201146	NORETHINDRONE ACETATE	4
CHEMBL1201196	SERTACONAZOLE	4
CHEMBL1201303	PYRVINIUM	4
CHEMBL1201772	PRASUGREL	4
CHEMBL1262	OXICONAZOLE	4
CHEMBL1274	NILUTAMIDE	4
CHEMBL1276308	MIFEPRISTONE	4
CHEMBL131	PREDNISOLONE	4
CHEMBL135	ESTRADIOL	4

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: nhr — 3C. 3-Ketosteroid receptors

Most potent curated ligand interactions (30 total), top 25:

Ligand	Action	Affinity	Parameter
methyltestosterone	Full agonist	9.66	pEC50
testosterone propionate	Agonist	9.6	pKi
dihydrotestosterone	Agonist	9.3	pKd
mifepristone	Antagonist	9.19	pKi
mibolerone	Agonist	8.96	pIC50
androstenedione	Agonist	8.56	pIC50
GSK2881078	Agonist	8.4	pEC50
andarine	Agonist	8.4	pKi
fluoxymesterone	Agonist	8.24	pKi
danazol	Agonist	8.0	pKi
cyproterone acetate	Antagonist	7.85	pKi
testosterone	Agonist	7.8	pIC50
stanozolol	Agonist	7.66	pIC50
darolutamide	Antagonist	7.59	pIC50
PF0998425	Antagonist	7.5	pIC50
pruxelutamide	Antagonist	7.49	pIC50
clascoterone	Antagonist	7.4	pKi
deutenzalutamide	Antagonist	7.4	pIC50
JNJ-63576253	Antagonist	7.27	pIC50
ARD-69	Antagonist	7.23	pIC50
nilutamide	Antagonist	7.12	pIC50
apalutamide	Antagonist	6.7	pIC50
enzalutamide	Antagonist	6.66	pIC50
hydroxyflutamide	Antagonist	6.6	pEC50
galeterone	Antagonist	6.42	pIC50

Binding affinities (BindingDB)

539 measured of 577 human assays (579 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
6-[bis(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one	EC50	0.2 nM
6-[(2,2-difluoroethyl)(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one	EC50	0.2 nM
BMS-665139	EC50	0.2 nM
oxazolidin-2-imine, 6d	KI	0.2 nM
ACP-105	EC50	0.251 nM
(1R,2S,10S,11S,14S,15S,17S)-1-fluoro-14,17-dihydroxy-2,14,15-trimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-5-one	EC50	0.3 nM
oxazolidin-2-imine, 6b	KI	0.3 nM
oxazolidin-2-imine, 6f	KI	0.3 nM
6-[ethyl(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one	EC50	0.4 nM
6-[bis(2,2-difluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one	EC50	0.4 nM
6-[(2-chloro-2,2-difluoroethyl)(2,2-difluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one	EC50	0.4 nM
6-[bis(2,2,2-trifluoroethyl)amino]-4-(difluoromethyl)-1,2-dihydroquinolin-2-one	KI	0.4 nM
4-[(1S,7aR)-1-hydroxy-7-methyl-5-oxo-2,3,5,7a-tetrahydro-1H-pyrrolizin-6-yl]-2-chloro-3-methylbenzonitrile	KI	0.5 nM
6-[(2-chloroethyl)(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one	EC50	0.5 nM
6-[bis(2,2,2-trifluoroethyl)amino]-4-chloro-1,2-dihydroquinolin-2-one	KI	0.5 nM
6-[bis(2,2,2-trifluoroethyl)amino]-4-bromo-1,2-dihydroquinolin-2-one	KI	0.5 nM
4-[(7R,7aS)-7-hydroxy-1,3-dioxo-hexahydro-1H-pyrrolo[1,2-a]imidazolidin-2-yl]-2-chloro-3-methylbenzonitrile	EC50	0.7 nM
4-[(1S,7R,7aR)-1-ethyl-7-hydroxy-3-oxo-hexahydro-1H-pyrrolo[1,2-a]imidazolidin-2-yl]-2-chloro-3-methylbenzonitrile	KI	0.7 nM
oxazolidin-2-imine, 6g	KI	0.7 nM
6-[bis(2,2,2-trifluoroethyl)amino]-4-methyl-1,2-dihydroquinolin-2-one	EC50	0.8 nM
oxazolidin-2-imine, 6a	KI	0.8 nM
4-[(1S,7S,7aR)-1-ethyl-7-hydroxy-3-oxo-hexahydro-1H-pyrrolo[1,2-a]imidazolidin-2-yl]-2-chloro-3-methylbenzonitrile	KI	0.9 nM
4-[(1R,7S,7aR)-7-hydroxy-3-oxo-1-(trifluoromethyl)-hexahydro-1H-pyrrolo[1,2-a]imidazolidin-2-yl]-2-chloro-3-methylbenzonitrile	KI	0.9 nM
6-[propan-2-yl(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one	EC50	0.9 nM
(1R,6R,7S)-4-(4-nitronaphthalen-1-yl)-2,4-diazatricyclo[5.2.1.0^{2,6}]decane-3,5-dione	KI	1 nM
4-[(1R,7R,7aR)-7-hydroxy-3-oxo-1-(trifluoromethyl)-hexahydro-1H-pyrrolo[1,2-a]imidazolidin-2-yl]-2-chloro-3-methylbenzonitrile	KI	1 nM
6-[bis(2,2,2-trifluoroethyl)amino]-1,2-dihydroquinolin-2-one	IC50	1 nM
(2S,6R)-4-(4-Nitro-naphthalen-1-yl)-4-aza-tricyclo[5.2.1.02,6]dec-8-ene-3,5-dione	KI	1 nM
CHEMBL403668	KI	1 nM
(2R)-2-methyl-1-(2,2,2-trifluoroethyl)-9-(trifluoromethyl)-1H,2H,3H,6H,7H-quinolino[7,6-b][1,4]oxazin-7-one	EC50	1.1 nM
oxazolidin-2-imine, 6e	EC50	1.1 nM
1-ethyl-9-(trifluoromethyl)-1H,2H,3H,6H,7H-quinolino[7,6-b][1,4]oxazin-7-one	KI	1.2 nM
6-[propyl(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one	EC50	1.3 nM
1-(cyclopropylmethyl)-9-(trifluoromethyl)-1H,2H,3H,6H,7H-quinolino[7,6-b][1,4]oxazin-7-one	EC50	1.4 nM
(6R)-6-hydroxy-2-(4-nitronaphthalen-1-yl)-hexahydro-1H-pyrrolo[1,2-a]imidazolidine-1,3-dione	KI	1.5 nM
(7R,7aS)-7-hydroxy-2-(4-nitronaphthalen-1-yl)-hexahydro-1H-pyrrolo[1,2-a]imidazolidine-1,3-dione	EC50	1.5 nM
(7S,7aR)-7-hydroxy-2-(4-nitronaphthalen-1-yl)-hexahydro-1H-pyrrolo[1,2-a]imidazolidine-1,3-dione	KI	1.5 nM
JMC522794 Compound 16	KI	1.5 nM
6-[(2R,5R)-2-methyl-5-[(1R)-2,2,2-trifluoro-1-hydroxyethyl]pyrrolidin-1-yl]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one	KI	1.5 nM
6-(dipropylamino)-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one	EC50	1.5 nM
4-[(1R,7S,7aR)-1-ethyl-7-hydroxy-3-oxo-hexahydro-1H-pyrrolo[1,2-a]imidazolidin-2-yl]-2-chloro-3-methylbenzonitrile	KI	1.6 nM
6-[(2,2-dichloroethyl)(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one	EC50	1.6 nM
2-(4-nitronaphthalen-1-yl)-hexahydro-1H-pyrrolo[1,2-a]imidazolidine-1,3-dione	KI	1.7 nM
6-[(2,2-dimethylpropyl)(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one	EC50	1.8 nM
4-[(1S,7S,7aR)-7-hydroxy-3-oxo-1-(trifluoromethyl)-hexahydro-1H-pyrrolo[1,2-a]imidazolidin-2-yl]-2-chloro-3-methylbenzonitrile	KI	1.9 nM
1-(cyclopropylmethyl)-2-methyl-9-(trifluoromethyl)-1H,2H,3H,6H,7H-quinolino[7,6-b][1,4]oxazin-7-one	EC50	1.9 nM
6-[bis(cyclopropylmethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one	EC50	1.9 nM
guanidine derivative, 12	KI	1.9 nM
4-[(7R,7aR)-7-hydroxy-3-oxo-hexahydro-1H-pyrrolo[1,2-a]imidazolidin-2-yl]-2-chloro-3-methylbenzonitrile	KI	2 nM
6-[bis(2,2,2-trifluoroethyl)amino]-4-(propan-2-yl)-1,2-dihydroquinolin-2-one	IC50	2 nM

ChEMBL bioactivities

5359 potent at pChembl≥5 of 5556 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	Ki	0.01	nM	CHEMBL180681
10.89	EC50	0.013	nM	METRIBOLONE
10.70	IC50	0.02	nM	CHEMBL391548
10.50	EC50	0.03162	nM	CHEMBL3818706
10.41	EC50	0.039	nM	CHEMBL3238292
10.40	EC50	0.0398	nM	CHEMBL3765171
10.30	IC50	0.05	nM	STANOLONE
10.30	EC50	0.05	nM	STANOLONE
10.22	EC50	0.06	nM	CHEMBL3238291
10.13	EC50	0.074	nM	CHEMBL3238288
10.00	EC50	0.1	nM	CHEMBL2323490
10.00	IC50	0.1	nM	CHEMBL184313
10.00	EC50	0.1	nM	CHEMBL4879244
10.00	EC50	0.1	nM	STANOLONE
10.00	EC50	0.1	nM	RAD-140
9.96	EC50	0.11	nM	CHEMBL3233072
9.96	EC50	0.11	nM	METRIBOLONE
9.89	EC50	0.13	nM	STANOLONE
9.85	EC50	0.14	nM	INDOMETHACIN
9.85	EC50	0.14	nM	CHEMBL2323511
9.85	EC50	0.14	nM	CHEMBL3238292
9.85	EC50	0.14	nM	CHEMBL4095364
9.85	EC50	0.14	nM	STANOLONE
9.82	EC50	0.15	nM	CHEMBL2323507
9.82	EC50	0.15	nM	CHEMBL3238287
9.80	EC50	0.16	nM	CHEMBL3326461
9.80	EC50	0.1585	nM	CHEMBL3819048
9.77	EC50	0.17	nM	CHEMBL4074555
9.74	EC50	0.18	nM	STANOLONE
9.72	EC50	0.19	nM	CHEMBL3402221
9.72	IC50	0.19	nM	CHEMBL4090028
9.72	EC50	0.19	nM	CHEMBL4090028
9.70	IC50	0.2	nM	CHEMBL2311179
9.70	IC50	0.2	nM	CHEMBL189306
9.70	EC50	0.1995	nM	CHEMBL3818497
9.70	EC50	0.1995	nM	CHEMBL3818619
9.70	EC50	0.1995	nM	CHEMBL3819648
9.70	Ki	0.2	nM	STANOLONE
9.70	EC50	0.2	nM	CHEMBL436784
9.70	IC50	0.2	nM	CHEMBL4060271
9.70	EC50	0.2	nM	CHEMBL440980
9.70	IC50	0.2	nM	CHEMBL256769
9.70	IC50	0.2	nM	CHEMBL427898
9.70	EC50	0.2	nM	CHEMBL4747369
9.70	EC50	0.2	nM	CHEMBL484726
9.70	IC50	0.2	nM	CHEMBL391548
9.70	Ki	0.2	nM	CHEMBL484727
9.62	EC50	0.24	nM	CHEMBL3402224
9.60	EC50	0.25	nM	CHEMBL3233071
9.60	EC50	0.25	nM	CHEMBL3402228

PubChem BioAssay actives

1873 with measured affinity, of 6100 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
(11S,13S,17S)-17-hydroxy-13-methyl-11-pentyl-2,6,7,8,11,12,14,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-3-one	242094: Inhibition of AR-dimerization in CHO-K1 cells expressing human androgen receptor	ic50	<0.0001	uM
4-(1-cyclopropyl-2,2,2-trifluoro-1-hydroxyethyl)-3-methyl-2-(trifluoromethyl)benzonitrile	1307766: Modulation of human androgen receptor expressed in African green monkey CV1 cells after 24 hrs by luciferase reporter gene assay	ec50	<0.0001	uM
(5S,8R,9S,10S,13S,14S,17S)-17-hydroxy-10,13-dimethyl-1,2,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthren-3-one	1187582: Agonist activity at human androgen receptor expressed in mouse C2C12 cells by androgen-specific response element-driven luciferase reporter gene assay	ec50	0.0001	uM
5-(2,6-difluoro-4-hydroxyphenyl)-1-methylpyrrole-2-carbonitrile	1457899: Agonist activity at human androgen receptor expressed in African green monkey CV-1 cells after 17 hrs by ARE luciferase reporter gene assay	ec50	0.0001	uM
N-[3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]-4-[4-[4-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]piperazin-1-yl]piperidin-1-yl]benzamide	1784623: Protac activity at VHL/AR in human VCaP cells assessed as induction of AR degradation measured after 24 hrs by western blot analysis	ec50	0.0001	uM
4-[[(1R,7S,7aS)-7-hydroxy-1-(trifluoromethyl)-5,6,7,7a-tetrahydro-1H-pyrrolo[1,2-c][1,3]oxazol-3-ylidene]amino]-2-chloro-3-methylbenzonitrile	1885023: Agonist activity at human Androgen receptor	ec50	0.0002	uM
6-[bis(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1H-quinolin-2-one	1872308: Modulation of Androgen receptor (unknown origin)	ec50	0.0002	uM
(8S,13S,14S,17S)-17-hydroxy-13-methyl-2,6,7,8,11,12,14,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-3-one	242138: Inhibition of human androgen receptor expressed in Escherichia coli	ic50	0.0002	uM
4-(1-cyclopropyl-2,2,2-trifluoro-1-hydroxyethyl)-2-(trifluoromethyl)benzonitrile	1307766: Modulation of human androgen receptor expressed in African green monkey CV1 cells after 24 hrs by luciferase reporter gene assay	ec50	0.0002	uM
4-(1-cyclobutyl-2,2,2-trifluoro-1-hydroxyethyl)-3-methyl-2-(trifluoromethyl)benzonitrile	1307766: Modulation of human androgen receptor expressed in African green monkey CV1 cells after 24 hrs by luciferase reporter gene assay	ec50	0.0002	uM
2-chloro-4-(1-cyclopropyl-2,2,2-trifluoro-1-hydroxyethyl)-3-methylbenzonitrile	1307766: Modulation of human androgen receptor expressed in African green monkey CV1 cells after 24 hrs by luciferase reporter gene assay	ec50	0.0002	uM
2,3-dichloro-4-(1-cyclopropyl-2,2,2-trifluoro-1-hydroxyethyl)benzonitrile	1307766: Modulation of human androgen receptor expressed in African green monkey CV1 cells after 24 hrs by luciferase reporter gene assay	ec50	0.0002	uM
5-(2,6-dichloro-4-hydroxyphenyl)-1-methylpyrrole-2-carbonitrile	1457899: Agonist activity at human androgen receptor expressed in African green monkey CV-1 cells after 17 hrs by ARE luciferase reporter gene assay	ec50	0.0002	uM
N-[3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]-4-[4-[[1-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]azetidin-3-yl]methyl]piperazin-1-yl]benzamide	1784623: Protac activity at VHL/AR in human VCaP cells assessed as induction of AR degradation measured after 24 hrs by western blot analysis	ec50	0.0002	uM
(9R,10S,11S,13S,17S)-9-fluoro-11,17-dihydroxy-10,13,17-trimethyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one	38803: Agonist activity against Human Androgen receptor expressed in CV-1 cells	ec50	0.0003	uM
4-[[(1R,7R,7aS)-7-hydroxy-1-(trifluoromethyl)-5,6,7,7a-tetrahydro-1H-pyrrolo[1,2-c][1,3]oxazol-3-ylidene]amino]-2-chloro-3-methylbenzonitrile	1798994: Receptor Binding Assay (Ki) and Transactivation Assay (EC50) from Article 10.1021/jm801583j: “N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.”	ki	0.0003	uM
2-chloro-4-[(1R,5S)-3-hydroxy-3-methyl-8-azabicyclo[3.2.1]octan-8-yl]-3-methylbenzonitrile	445841: Agonist activity at androgen receptor in human MDA-KB2 cells transfected with MMTV linked luciferase assessed as transcriptional activation by luciferase reporter gene assay	ec50	0.0003	uM
3-methyl-4-(1,1,1-trifluoro-2-hydroxy-3-methylbutan-2-yl)-2-(trifluoromethyl)benzonitrile	1307766: Modulation of human androgen receptor expressed in African green monkey CV1 cells after 24 hrs by luciferase reporter gene assay	ec50	0.0003	uM
3-methyl-4-[2,2,2-trifluoro-1-(furan-2-yl)-1-hydroxyethyl]-2-(trifluoromethyl)benzonitrile	1307766: Modulation of human androgen receptor expressed in African green monkey CV1 cells after 24 hrs by luciferase reporter gene assay	ec50	0.0003	uM
5-(2-fluoro-4-hydroxyphenyl)-1-methylpyrrole-2-carbonitrile	1457899: Agonist activity at human androgen receptor expressed in African green monkey CV-1 cells after 17 hrs by ARE luciferase reporter gene assay	ec50	0.0003	uM
N-[3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]-4-[4-[[1-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]piperidin-4-yl]methyl]piperazin-1-yl]benzamide	1784623: Protac activity at VHL/AR in human VCaP cells assessed as induction of AR degradation measured after 24 hrs by western blot analysis	ec50	0.0003	uM
5-(2-fluoro-4-hydroxyphenyl)-1H-pyrrole-2-carbonitrile	1885054: Agonist activity at human Androgen receptor expressed in African green monkey CV-1 cells measured by ARE-luciferase assay	ec50	0.0003	uM
4-[(3aS,4R)-4-hydroxy-1,1,3-trioxo-3a,4,5,6-tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2-yl]-2-chloro-3-methylbenzonitrile	1885049: Displacement of [3H]DHT from Androgen receptor expressed in human MDA-MB-453 cells	ki	0.0004	uM
2-chloro-4-(1-cyclopropyl-2,2,2-trifluoro-1-hydroxyethyl)benzonitrile	1307766: Modulation of human androgen receptor expressed in African green monkey CV1 cells after 24 hrs by luciferase reporter gene assay	ec50	0.0004	uM
N-[3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]-4-[4-[[4-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]piperazin-1-yl]methyl]piperidin-1-yl]benzamide	1784623: Protac activity at VHL/AR in human VCaP cells assessed as induction of AR degradation measured after 24 hrs by western blot analysis	ec50	0.0004	uM
2-chloro-4-[(7S,8R)-7-hydroxy-1-methyl-3-oxo-5,6,7,8-tetrahydropyrrolizin-2-yl]-3-methylbenzonitrile	1797702: Receptor Binding and Transactivation Assay from Article 10.1021/jm070312d: “Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications.”	ki	0.0005	uM
3-methyl-4-[2,2,2-trifluoro-1-hydroxy-1-(1,3-oxazol-4-yl)ethyl]-2-(trifluoromethyl)benzonitrile	1307766: Modulation of human androgen receptor expressed in African green monkey CV1 cells after 24 hrs by luciferase reporter gene assay	ec50	0.0005	uM
(2S)-3-(4-cyanophenoxy)-N-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide	1885044: Displacement of [3H]mibolerone from Androgen receptor (unknown origin) measured by liquid scintillation counting method	ki	0.0006	uM
(1S,3aS,3bS,5aR,9aS,9bS,11aS)-8-fluoro-N-(1H-imidazo[4,5-b]pyridin-2-ylmethyl)-6,9a,11a-trimethyl-7-oxo-2,3,3a,3b,4,5,5a,9b,10,11-decahydro-1H-indeno[5,4-f]quinoline-1-carboxamide	1872309: Modulation of human Androgen receptor transfected in African green monkey COS cells	ec50	0.0006	uM
2,3-dichloro-4-(1-cyclobutyl-2,2,2-trifluoro-1-hydroxyethyl)benzonitrile	1307766: Modulation of human androgen receptor expressed in African green monkey CV1 cells after 24 hrs by luciferase reporter gene assay	ec50	0.0006	uM
2-chloro-4-[(3S)-8-[4-[4-[1-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]azetidin-3-yl]piperazine-1-carbonyl]phenyl]-3-methyl-2,8-diazaspiro[4.5]decan-2-yl]benzonitrile	1982086: Induction of androgen receptor degradation in human VCaP cells incubated for 24 hrs by Western blot analysis	ec50	0.0006	uM
4-[(1S,7R,7aR)-1-ethyl-7-hydroxy-3-oxo-5,6,7,7a-tetrahydro-1H-pyrrolo[1,2-c]imidazol-2-yl]-2-chloro-3-methylbenzonitrile	1797702: Receptor Binding and Transactivation Assay from Article 10.1021/jm070312d: “Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications.”	ki	0.0007	uM
6-[cyclopropylmethyl(propyl)amino]-4-(trifluoromethyl)pyridine-3-carbonitrile	309346: Displacement of [3H]dihydrotestosterone from human androgen receptor expressed in Sf9 cells	ic50	0.0008	uM
2-chloro-3-methyl-4-(1,1,1-trifluoro-2-hydroxy-3-methylbutan-2-yl)benzonitrile	1307766: Modulation of human androgen receptor expressed in African green monkey CV1 cells after 24 hrs by luciferase reporter gene assay	ec50	0.0008	uM
2,3-dichloro-4-(1,1,1-trifluoro-2-hydroxy-3-methylbutan-2-yl)benzonitrile	1307766: Modulation of human androgen receptor expressed in African green monkey CV1 cells after 24 hrs by luciferase reporter gene assay	ec50	0.0008	uM
(2S,4R)-N-[(1S)-3-[4-[4-[2-[4-[[3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]carbamoyl]phenyl]ethynyl]piperidin-1-yl]piperidin-1-yl]-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]-3-oxopropyl]-1-[(2S)-2-[(1-fluorocyclopropanecarbonyl)amino]-3,3-dimethylbutanoyl]-4-hydroxypyrrolidine-2-carboxamide	1960582: Protac activity at VHL/AR in human VCaP cells assessed as induction of protein degradation measured after 24 hrs by Western blot analysis	ec50	0.0008	uM
N-[3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]-4-[4-[1-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]piperidin-4-yl]piperazin-1-yl]benzamide	1784623: Protac activity at VHL/AR in human VCaP cells assessed as induction of AR degradation measured after 24 hrs by western blot analysis	ec50	0.0008	uM
4-[(1S,7S,7aR)-1-ethyl-7-hydroxy-3-oxo-5,6,7,7a-tetrahydro-1H-pyrrolo[1,2-c]imidazol-2-yl]-2-chloro-3-methylbenzonitrile	1797702: Receptor Binding and Transactivation Assay from Article 10.1021/jm070312d: “Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications.”	ki	0.0009	uM
4-[(1R,7S,7aR)-7-hydroxy-3-oxo-1-(trifluoromethyl)-5,6,7,7a-tetrahydro-1H-pyrrolo[1,2-c]imidazol-2-yl]-2-chloro-3-methylbenzonitrile	1797702: Receptor Binding and Transactivation Assay from Article 10.1021/jm070312d: “Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications.”	ki	0.0009	uM
4-[(4S)-4-(4-hydroxyphenyl)-4-methyl-2,5-dioxoimidazolidin-1-yl]-2-(trifluoromethyl)benzonitrile	1885053: Partial agonist activity at human Androgen receptor	ic50	0.0009	uM
4-(trifluoromethyl)-6,7,8,9-tetrahydropyrano[3,2-g]quinolin-2-one	38985: In vitro binding affinity at human androgen receptor transfected into COS cells.	ic50	0.0010	uM
2-chloro-4-(3-hydroxy-3-methyl-8-azabicyclo[3.2.1]octan-8-yl)-3-methylbenzonitrile	1885021: Binding affinity to human Androgen receptor	ic50	0.0010	uM
N-[(3aR,4R,5R,7S,7aS)-2-[4-cyano-3-(trifluoromethyl)phenyl]-4,7-dimethyl-1,3-dioxo-3a,5,6,7a-tetrahydro-4,7-epoxyisoindol-5-yl]benzenesulfonamide	1249995: Antagonist activity at androgen receptor in human MDA-MB-453 cells assessed as inhibition of DHT-induced PSA expression by alkaline phosphatase reporter gene assay	ic50	0.0010	uM
N-[(3aR,4R,5R,7S,7aS)-2-[4-cyano-3-(trifluoromethyl)phenyl]-4,7-dimethyl-1,3-dioxo-3a,5,6,7a-tetrahydro-4,7-epoxyisoindol-5-yl]-2-fluorobenzenesulfonamide	1249994: Displacement of [3H]-DHT from androgen receptor in human MDA-MB-453 cells after 90 mins by TopCount analysis	ki	0.0010	uM
N-[4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-[[4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxoisoindol-5-yl]piperazin-1-yl]methyl]piperidin-1-yl]pyridazine-3-carboxamide	1872331: Protac activity at CRBN/AR in human castration-resistant prostate cancer cells assessed as induction of androgen receptor degradation	ec50	0.0010	uM
4-[(1R,7R,7aR)-7-hydroxy-3-oxo-1-(trifluoromethyl)-5,6,7,7a-tetrahydro-1H-pyrrolo[1,2-c]imidazol-2-yl]-2-chloro-3-methylbenzonitrile	1797702: Receptor Binding and Transactivation Assay from Article 10.1021/jm070312d: “Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications.”	ki	0.0010	uM
tert-butyl 2,5-dioxo-4-(trifluoromethyl)-1H-chromeno[3,4-f]quinoline-10-carboxylate	1885023: Agonist activity at human Androgen receptor	ec50	0.0011	uM
4-[2,2,2-trifluoro-1-hydroxy-1-(1,3-oxazol-4-yl)ethyl]-2-(trifluoromethyl)benzonitrile	1307766: Modulation of human androgen receptor expressed in African green monkey CV1 cells after 24 hrs by luciferase reporter gene assay	ec50	0.0013	uM
4-[2,2,2-trifluoro-1-(furan-2-yl)-1-hydroxyethyl]-2-(trifluoromethyl)benzonitrile	1307766: Modulation of human androgen receptor expressed in African green monkey CV1 cells after 24 hrs by luciferase reporter gene assay	ec50	0.0013	uM
(4Z)-3-(2-fluorophenyl)-4-[(4-pyrrolidin-1-ylphenyl)methylidene]-1,2-oxazol-5-one	39000: Dissociation constant against GST-hARLBD was measured in SC-3 cell by using [3H]testosterone as radioligand	kd	0.0014	uM

CTD chemical–gene interactions

772 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Dihydrotestosterone	decreases reaction, increases activity, affects cotreatment, affects localization, increases phosphorylation (+12 more)	137
Metribolone	affects binding, affects localization, affects reaction, increases expression, increases stability (+11 more)	51
bicalutamide	affects reaction, decreases reaction, increases stability, increases activity, affects cotreatment (+13 more)	49
Flutamide	decreases reaction, increases expression, increases activity, affects binding, decreases activity (+3 more)	42
bisphenol A	decreases expression, increases activity, affects activity, affects folding, affects cotreatment (+9 more)	41
Testosterone	affects phosphorylation, increases phosphorylation, decreases expression, decreases reaction, increases activity (+10 more)	39
Estradiol	decreases reaction, increases activity, increases expression, decreases expression, decreases activity (+6 more)	31
vinclozolin	affects binding, decreases activity, affects cotreatment, affects localization, increases phosphorylation (+4 more)	30
hydroxyflutamide	affects binding, affects cotreatment, decreases expression, increases expression, increases phosphorylation (+7 more)	24
Dichlorodiphenyl Dichloroethylene	decreases expression, increases phosphorylation, affects cotreatment, decreases reaction, affects reaction (+6 more)	23
Cyproterone Acetate	decreases expression, increases expression, increases activity, affects binding, affects reaction (+7 more)	17
Methoxychlor	decreases reaction, increases activity, affects reaction, increases expression, affects binding (+2 more)	15
Benzo(a)pyrene	decreases expression, decreases reaction, increases reaction, decreases activity, increases activity (+4 more)	13
o,p’-DDT	increases expression, decreases reaction, increases activity, affects binding, decreases activity (+1 more)	12
mibolerone	increases localization, increases phosphorylation, affects cotreatment, affects localization, increases expression (+5 more)	11
enzalutamide	affects localization, increases activity, decreases response to substance, decreases activity, decreases localization (+7 more)	11
Linuron	affects activity, affects binding, decreases activity, affects cotreatment, increases expression (+2 more)	11
2,2-bis(4-hydroxyphenyl)-1,1,1-trichloroethane	decreases reaction, increases activity, affects binding, decreases activity, affects cotreatment	10
Progesterone	affects activity, affects binding, decreases activity, increases activity, decreases reaction (+1 more)	10
procymidone	affects cotreatment, affects binding, increases expression, decreases activity, decreases reaction (+1 more)	9
prochloraz	decreases reaction, increases activity, affects localization, affects binding, decreases activity (+3 more)	9
DDT	decreases activity, affects localization, decreases expression, affects cotreatment, affects binding (+4 more)	9
nilutamide	affects localization, affects cotreatment, decreases reaction, increases response to substance, increases activity (+3 more)	8
bisphenol AF	affects folding, affects reaction, increases reaction, decreases activity, decreases response to substance (+4 more)	8
Resveratrol	increases expression, decreases expression, affects binding, decreases phosphorylation, increases reaction (+4 more)	8
Fenitrothion	decreases reaction, increases activity, affects binding, decreases activity, affects cotreatment (+1 more)	8
Quercetin	affects localization, decreases methylation, affects binding, decreases activity, increases activity (+8 more)	8
4,4’-bisphenol F	increases expression, decreases activity, affects binding, decreases reaction, increases activity	7
pentabrominated diphenyl ether 100	decreases reaction, increases activity, increases reaction, affects binding, decreases activity	7
Dibutyl Phthalate	affects cotreatment, decreases reaction, increases activity, decreases activity, decreases expression (+2 more)	7

ChEMBL screening assays

2100 unique, capped per target: 1727 binding, 339 functional, 33 admet, 1 unclassified

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1013140	Binding	Displacement of [3H]testosterone from wild type human androgen receptor	4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor. — Bioorg Med Chem
CHEMBL1013144	Functional	Antagonist activity at wild type human recombinant androgen receptor assessed as inhibition of testosterone-induced growth of mouse androgen dependent SC3 cells by WST-1 method	4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor. — Bioorg Med Chem
CHEMBL3243253	ADMET	Binding affinity to human AR NTD (1 to 561 aa) expressed in CV1 cells coexpressing human AR-LBD (644-919 aa) assessed as N/C-termini interaction by androgenic assay	1-(2-Hydroxy-2-methyl-3-phenoxypropanoyl)indoline-4-carbonitrile derivatives as potent and tissue selective androgen receptor modulators. — J Med Chem

Cellosaurus cell lines

142 cell lines: 108 cancer cell line, 18 induced pluripotent stem cell, 7 transformed cell line, 6 embryonic stem cell, 3 spontaneously immortalized cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_0046	HTh83	Cancer cell line	Male
CVCL_0395	LNCaP	Cancer cell line	Male
CVCL_0418	MDA-MB-453	Cancer cell line	Female
CVCL_1379	LNCaP clone FGC	Cancer cell line	Male
CVCL_2821	4-11	Cancer cell line	Female
CVCL_3872	LNCaP-CL1	Cancer cell line	Male
CVCL_3967	CWR22	Cancer cell line	Male
CVCL_4782	LNCaP C4-2	Cancer cell line	Male
CVCL_4783	LNCaP C4	Cancer cell line	Male
CVCL_4784	LNCaP C4-2B	Cancer cell line	Male

Clinical trials (associated diseases)

301 trials via MONDO — disease-level, not drug-specific.

Trial	Phase	Status	Title
NCT00851461	PHASE4	COMPLETED	Effect of Goserelin (Zoladex®) in Spinal and Bulbar Muscular Atrophy
NCT00190697	PHASE4	COMPLETED	A Study of LY353381 (Arzoxifene) for Patients Who Benefitted From This Drug in Other Oncology Trials and Wished to Continue Treatment
NCT00277160	PHASE4	COMPLETED	A Study of Primary Prophylaxis With Neulasta (Pegfilgrastim) Versus Secondary Prophylaxis After Chemotherapy in Elderly Subjects (>/= 65 Years Old) With Cancer
NCT00727961	PHASE4	COMPLETED	A Study to Evaluate Efficacy and Tolerance of Caelyx in Patients With Epithelial Ovarian Cancer. (Study P04072)(COMPLETED)
NCT00740116	PHASE4	COMPLETED	Tranexamic Acid in Surgery of Advanced Ovarian Cancer
NCT00817479	PHASE4	COMPLETED	Tumor Gene Expression in Women With Ovarian Cancer
NCT01432015	PHASE4	COMPLETED	Fosaprepitant Versus Aprepitant in the Prevention of Chemotherapy Induced Nausea and Vomiting
NCT01706120	PHASE4	UNKNOWN	Study of Clinical and Biological Prognostic Factors in Patients With Ovarian Cancer Receiving Carboplatin +Paclitaxel With Bevacizumab
NCT01932125	PHASE4	COMPLETED	An Interventional Study of Avastin (Bevacizumab) in Patients With Advanced/Metastatic Epithelial Ovarian Cancer, Fallopian Tube Cancer or Primary Peritoneal Cancer
NCT01953107	PHASE4	COMPLETED	Oral Iron vs. Placebo in Newly Diagnosed Gynecologic Oncology Patients Who Are Surgical Candidates.
NCT02035345	PHASE4	TERMINATED	Slowed Carboplatin Infusion for Ovarian Cancer Patients Receiving Carboplatin Re-Treatment
NCT02243059	PHASE4	WITHDRAWN	Magnetic Resonance Imaging for Lymph Node Staging in Ovarian Cancer
NCT03164980	PHASE4	TERMINATED	QoL-Comparison Between Trabectedin/PLD and Pt-based Therapy in Patients With Pt-sensitive Recurrent Ovarian Cancer
NCT03384511	PHASE4	COMPLETED	The Use of 18F-ALF-NOTA-PRGD2 PET/CT Scan to Predict the Efficacy and Adverse Events of Apatinib in Malignancies.
NCT03543462	PHASE4	COMPLETED	Diaphragmatic Resection And Gynecological Ovarian Neoplasm
NCT03752216	PHASE4	COMPLETED	NIraparib and Quality of LifE is a Longitudinal Study Evaluating in Real Life the Tolerability of Niraparib.
NCT03858166	PHASE4	TERMINATED	Efficacy and Safety of PEG-rhG-CSF Secondary Prophylaxis vs. Therapeutic Administration in Patients With Ovarian Cancer
NCT04024254	PHASE4	COMPLETED	A Study of Serum Folate Levels in Patients Treated With Olaparib
NCT04330040	PHASE4	COMPLETED	Prospective Multicentre Phase-IV Clinical Trial of Olaparib in Indian Patients With Ovarian and Metastatic Breast Cancer
NCT04352439	PHASE4	COMPLETED	Aspirin for Prevention of Venous Thromboembolism Among Ovarian Cancer Patients Receiving Neoadjuvant Chemotherapy
NCT05187208	PHASE4	UNKNOWN	PARP Inhibitor Oral Maintenance in Low-Risk Ovarian Cancer
NCT05606692	PHASE4	RECRUITING	Influences of Propofol and Sevoflurane Anesthesia in Ovarian Cancer (Anesthetics)
NCT05926336	PHASE4	RECRUITING	The Effects of Using Different Anesthetics on the Prognosis of Primary Tumors and Its Mechanism of Action
NCT06412120	PHASE4	RECRUITING	Study Evaluating Safety, Tolerability, and Metabolism of Niraparib
NCT06871787	PHASE4	NOT_YET_RECRUITING	Near-Infrared Fluorescence Imaging With Indocyanine Green to Evaluate Bowel Anastomoses in Gynecologic Oncology Surgery
NCT06887933	PHASE4	NOT_YET_RECRUITING	A Trial to Evaluate the Safety of Niraparib Tablets in Adult Female Participants With Advanced or Relapsed Epithelial Ovarian Cancer
NCT07469202	PHASE4	NOT_YET_RECRUITING	CYTALUX Dose Extension Study
NCT04422366	PHASE3	RECRUITING	Evaluate the Efficacy, Immunogenicity and Safety of 9-valent HPV Recombinant Vaccine in Chinese Healthy Females
NCT04425291	PHASE3	COMPLETED	Evaluate the Immunogenicity and Safety of 4-valent and 9-valent HPV Recombinant Vaccine in Chinese Healthy Females
NCT04895020	PHASE3	RECRUITING	Immunobridging Study of 9-valent Human Papillomavirus Recombinant Vaccine in Chinese Females Aged 9 to 19 Years
NCT05372016	PHASE3	COMPLETED	Evaluate the Immunogenicity and Safety of 9-valent HPV Recombinant Vaccine in Chinese Healthy Females
NCT05584332	PHASE3	TERMINATED	A Phase Ⅲ Study to Evaluate the Efficacy, Immunogenicity, Safety of Quadrivalent HPV Recombinant Vaccine in Chinese Healthy Females
NCT07520565	PHASE3	RECRUITING	A Multicentre, Randomised, Double-blind, Placebo-parallel Controlled Phase Ⅲ Clinical Trial Evaluating the Efficacy and Safety of BXOS110 Injection in the Treatment of Acute Ischaemic Stroke Within 3 Hours of Onset.
NCT00001806	PHASE3	COMPLETED	Methods in Education for Breast Cancer Genetics
NCT00002477	PHASE3	UNKNOWN	Adjuvant Chemotherapy Compared With Observation in Treating Patients With Resected Early Stage Ovarian Epithelial Cancer
NCT00002568	PHASE3	COMPLETED	Combination Chemotherapy With or Without Surgery in Treating Patients With Stage III Ovarian Epithelial Cancer
NCT00002641	PHASE3	COMPLETED	Surgery With or Without Chemotherapy in Treating Patients With Soft Tissue Sarcoma
NCT00002717	PHASE3	COMPLETED	Paclitaxel and Cisplatin in Treating Patients With Stage III or Stage IV Ovarian Cancer or Primary Peritoneal Cancer
NCT00002764	PHASE3	COMPLETED	Surgery With or Without Combination Chemotherapy in Treating Patients With Lung Metastases From Soft Tissue Sarcoma
NCT00002819	PHASE3	TERMINATED	Chemotherapy With or Without Peripheral Stem Cell Transplantation in Treating Patients With Persistent Ovarian Epithelial Cancer