Page last updated: 2024-11-04

fluoxymesterone

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

Fluoxymesterone: An anabolic steroid that has been used in the treatment of male HYPOGONADISM, delayed puberty in males, and in the treatment of breast neoplasms in women. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6446
CHEMBL ID1445
CHEBI ID5120
SCHEMBL ID5096
MeSH IDM0008638

Synonyms (130)

Synonym
testosterone, 9-fluoro-11beta-hydroxy-17-methyl-
brn 2008796
fluoximesteron
fluoxymesteronum [inn-latin]
nsc 10704
ai3-52940
9-alpha-fluoro-11-beta,17-beta-dihydroxy-17-alpha-methyl-4-androstene-3-one
9-fluoro-11-beta,17-beta-dihydroxy-17-methylandrost-4-en-3-one
9alpha-fluoro-17alpha-methyl-11beta,17-dihydroxy-4-androsten-3-one
11beta,17beta-dihydroxy-9alpha-fluoro-17alpha-methyl-4-androsten-3-one
androst-4-en-3-one, 9-fluoro-11beta,17beta-dihydroxy-17-methyl-
9alpha-fluoro-11beta,17beta-dihydroxy-17alpha-methyl-4-androstene-3-one
9-alpha-fluoro-17-alpha-methyl-11-beta,17-dihydroxy-4-androsten-3-one
fluoximesteronum
fluoximesterona [inn-spanish]
androst-4-en-3-one, 9-fluoro-11,17-dihydroxy-17-methyl-, (11beta,17beta)-
anadroid-f
11-beta,17-beta-dihydroxy-9-alpha-fluoro-17-alpha-methyl-4-androster-3-one
ccris 9036
fluossimesterone [dcit]
einecs 200-961-8
hsdb 3333
9-alpha-fluoro-11-beta-hydroxy-17-methyltestosterone
17-alpha-methyl-9-alpha-fluoro-11-beta-hydroxytesterone
android-f
fluoro-9-alpha dihydroxy-11-beta,17-beta methyl-17-alpha androstene-4 one-3 [french]
androst-4-en-3-one, 9-fluoro-11beta,17beta-dihydroxy-17-methyl- (van)
MLS001055414
smr000686158
gtpl2861
9alpha-fluoro-11beta,17beta-dihydroxy-17-methylandrost-4-en-3-one
LMST02020025
nsc12165
nsc10704
fluoxymesterone
flusteron
oralsterone
fluosterone
u 6040
testoral
ora-testryl
fluoximesterone
oratestin
fluotestin
nsc-10704
76-43-7
androfluorone
neo-ormonal
9.alpha.-fluoro-11.beta.-hydroxy-17-methyltestosterone
androsterolo
FXM ,
component of halodrin
nsc-12165
androfluorene
testosterone, 9-fluoro-11.beta.-hydroxy-17-methyl-
9.alpha.-fluoro-11.beta.,17.beta.-dihydroxy-17.alpha.-methyl-4-androstene-3-one
ora testryl
halotestin
ultandren
ultandrene
flutestos
9-fluoro-11beta,17beta-dihydroxy-17alpha-methylandrost-4-en-3-one
CHEBI:5120 ,
fluoximesterona
fluoxymesteronum
NCGC00091037-01
halodrin
fluoxymesterone, solid (photosensitive)
DB01185
9alpha-fluoro-11beta-hydroxy-17-methyltestosterone
17alpha-methyl-9alpha-fluoro-11beta-hydroxytesterone
9-fluoro-11beta,17beta-dihydroxy-17-methylandrost-4-en-3-one
11beta,17beta-dihydroxy-9alpha-fluoro-17alpha-methyl-4-androster-3-one
D00327
androxy (tn)
fluoxymesterone (jan/usp/inn)
halotestin (tn)
(11beta,17beta)-9-fluoro-11,17-dihydroxy-17-methylandrost-4-en-3-one
fluoxymestrone
bdbm18189
(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
CHEMBL1445
fluoxymesterone ciii
(8s,9r,10s,11s,13s,14s,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
A838701
(8s,9r,10s,11s,13s,14s,17s)-9-fluoranyl-10,13,17-trimethyl-11,17-bis(oxidanyl)-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one
NCGC00091037-02
NCGC00258408-01
cas-76-43-7
dtxcid6013512
tox21_113158
tox21_200854
dtxsid8033512 ,
HMS2272B06
unii-9ju12s4yfy
fluoxymesterone [usp:inn:ban:jan]
fluossimesterone
fluoro-9-alpha dihydroxy-11-beta,17-beta methyl-17-alpha androstene-4 one-3
4-08-00-02057 (beilstein handbook reference)
9ju12s4yfy ,
androxy
fluoxymesterone [mart.]
fluoxymesterone ciii [usp-rs]
fluoxymesterone [orange book]
fluoxymesterone [mi]
fluoxymesterone [inn]
fluoxymesterone [vandf]
fluoxymesterone [jan]
fluoxymesterone [who-dd]
fluoxymesterone [hsdb]
fluoxymesterone [usp monograph]
AKOS015895109
SCHEMBL5096
W-104363
AC-29744
fluoxymesterone 1.0 mg/ml in acetonitrile
fluoxymesteron
9alpha-fluoro-11beta-hydroxy-17alpha-methyltestosterone
androst-4-en-3-one, 9-fluoro-11beta,17beta-dihydroxy-17-methyl-(van)
Q410663
BCP10776
(8s,9r,10s,11s,13s,14s,17s)-9-fluoro-11,17-dihydroxy-10,13,17-trimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthren-3(2h)-one
fluoxymesterone (usp monograph)
fluoxymesterone ciii (usp-rs)
fluoxymesterone (usp:inn:ban:jan)
fluoxymesteronum (inn-latin)
g03ba01
fluoximesterona (inn-spanish)
fluoxymesterone (mart.)
fluoxymesterone, 1mg/ml in acetonitrile

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The purpose of this study was to determine and compare the direct toxic effects of commonly abused AAS (both 17 alpha-alkylated and nonalkylated) in primary hepatic cell cultures."( Toxic effects of anabolic-androgenic steroids in primary rat hepatic cell cultures.
Melchert, RB; Robertson, JW; Welder, AA, 1995
)
0.29

Compound-Compound Interactions

ExcerptReferenceRelevance
"Postmenopausal women with early stage breast cancer that was known to be estrogen receptor (ER) positive were randomized to treatment with Tam (20 mg per day orally for 5 years) alone or combined with Flu (10 mg orally twice per day for 1 year)."( Randomized trial of tamoxifen alone or combined with fluoxymesterone as adjuvant therapy in postmenopausal women with resected estrogen receptor positive breast cancer. North Central Cancer Treatment Group Trial 89-30-52.
Donohue, JH; Goetz, MP; Ingle, JN; Krook, JE; Kugler, JW; Mailliard, JA; Michalak, JC; Perez, EA; Pisansky, TM; Suman, VJ; Wold, LE, 2006
)
0.33

Bioavailability

ExcerptReferenceRelevance
" Assay suitability was assessed in a bioavailability study in which six subjects each received two treatments of 10-mg fluoxymesterone tablets in a Latin-square crossover study."( Liquid chromatographic assay for fluoxymesterone in human serum with application to a preliminary bioavailability study.
Albert, KS; Antal, EJ; Capponi, VJ; Cox, SR; Harrington, EL; Wright, CE, 1985
)
0.27
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
"Megestrol acetate (Megace), an antiandrogen, was administered in a dosage of 80 mg daily to 6 patients with benign prostatic hypertrophy (BPH) for 4 to 25 days prior to transurethral resection of the prostate (TURP)."( Effect of megestrol acetate (Megace) on steroid metabolism and steroid-protein binding in the human prostate.
Albert, J; Cantor, T; Geller, J; Geller, S; Lopez, D; Yen, S, 1976
)
0.26
" The mean height velocity attained at the optimal dosage (0."( Medical Research Council of Canada therapeutic trial of human growth hormone: first 5 years of therapy.
Bailey, JD; Beck, JC; Friesen, H; Guyda, H; Leboeuf, G, 1975
)
0.25
" The preliminary results of a cooperative protocol using very low dosage of cytosine arabinoside (3mg/m2/twice daily) with or without androgens are given."( Present results of the treatment of myelodysplastic syndromes with low-dose cytosine arabinoside. Preliminary results of a cooperative protocol (38 patients) and review of the literature.
Baumelou, E; Calvo, F; Casassus, P; Chomienne, C; Ciccone, F; Degos, L; Fenaux, P; Gris, JC; Najean, Y; Thomas, G, 1987
)
0.27
" It was found that LH was suppressed to intact levels by testosterone or its active metabolites at doses within the "physiologic dosage range" (equivalent in biological activity to endogenously secreted androgens)."( Pituitary-gonadal axis before puberty: evaluation of testicular steroids in the male rat.
Eldrige, JC; Mahesh, VB, 1974
)
0.25
" No significant dose-response relationships emerged."( Evaluation of tamoxifen doses with and without fluoxymesterone in advanced breast cancer.
Cassidy, JG; Edwards, BK; Lippman, ME; Tormey, DC, 1983
)
0.27
" Patients receiving CMFH tended to maintain higher hemoglobin, leukocyte, and platelet levels, and receive a higher dosage of each of the cytotoxic drugs."( A prospective evaluation of chemohormonal therapy remission maintenance in advanced breast cancer.
Arseneau, JC; Band, PR; Bauer, M; Falkson, G; Gelman, R; Sears, M; Tormey, DC, 1981
)
0.26
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
anabolic agentA compound which stimulates anabolism and inhibits catabolism. Anabolic agents stimulate the development of muscle mass, strength, and power.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (5)

ClassDescription
anabolic androgenic steroidA steroid hormone related to the hormone testosterone. It increases protein synthesis within cells, which results in the buildup of cellular tissue (anabolism), especially in muscles. It also has androgenic and virilizing properties.
17beta-hydroxy steroidA 17-hydroxy steroid in which the hydroxy group at position 17 has a beta-configuration.
11beta-hydroxy steroidAny 11-hydroxy steroid in which the hydroxy group at position 11 has beta- configuration.
fluorinated steroidA steroid which is substituted with one or more fluorine atoms in any position.
3-oxo-Delta(4) steroidA 3-oxo steroid conjugated to a C=C double bond at the alpha,beta position.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (21)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency7.94330.003245.467312,589.2998AID2517
Chain A, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID886
Chain B, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID886
pregnane X receptorRattus norvegicus (Norway rat)Potency22.38720.025127.9203501.1870AID651751
GLI family zinc finger 3Homo sapiens (human)Potency29.89560.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency3.62190.000221.22318,912.5098AID1259243; AID1259247; AID1259381; AID588515; AID743035; AID743036; AID743040; AID743042; AID743053; AID743054
Smad3Homo sapiens (human)Potency3.98110.00527.809829.0929AID588855
progesterone receptorHomo sapiens (human)Potency1.23710.000417.946075.1148AID1346784; AID1347036
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency4.04310.000214.376460.0339AID588533; AID720692
retinoid X nuclear receptor alphaHomo sapiens (human)Potency27.70760.000817.505159.3239AID1159527
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency54.81530.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
pregnane X nuclear receptorHomo sapiens (human)Potency59.82440.005428.02631,258.9301AID1346982; AID720659
estrogen nuclear receptor alphaHomo sapiens (human)Potency37.82350.000229.305416,493.5996AID743069; AID743075; AID743077; AID743079
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency12.37650.001019.414170.9645AID743094
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency19.40990.023723.228263.5986AID588543; AID743223
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency0.00270.001723.839378.1014AID743083
chromobox protein homolog 1Homo sapiens (human)Potency79.43280.006026.168889.1251AID540317
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency2.51190.794321.275750.1187AID624246
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency62.69560.000627.21521,122.0200AID651741; AID743202; AID743219
Nuclear receptor ROR-gammaHomo sapiens (human)Potency29.84930.026622.448266.8242AID651802
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Androgen receptorHomo sapiens (human)IC50 (µMol)10.00000.00000.875310.0000AID286657
Androgen receptorHomo sapiens (human)Ki0.00570.00020.42407.2000AID1797703; AID286658
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Androgen receptorHomo sapiens (human)EC50 (µMol)0.00030.00000.20794.3000AID286656
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (66)

Processvia Protein(s)Taxonomy
negative regulation of transcription by RNA polymerase IIAndrogen receptorHomo sapiens (human)
MAPK cascadeAndrogen receptorHomo sapiens (human)
in utero embryonic developmentAndrogen receptorHomo sapiens (human)
regulation of systemic arterial blood pressureAndrogen receptorHomo sapiens (human)
epithelial cell morphogenesisAndrogen receptorHomo sapiens (human)
transcription by RNA polymerase IIAndrogen receptorHomo sapiens (human)
signal transductionAndrogen receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAndrogen receptorHomo sapiens (human)
cell-cell signalingAndrogen receptorHomo sapiens (human)
spermatogenesisAndrogen receptorHomo sapiens (human)
single fertilizationAndrogen receptorHomo sapiens (human)
positive regulation of cell population proliferationAndrogen receptorHomo sapiens (human)
negative regulation of cell population proliferationAndrogen receptorHomo sapiens (human)
positive regulation of gene expressionAndrogen receptorHomo sapiens (human)
male somatic sex determinationAndrogen receptorHomo sapiens (human)
intracellular estrogen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
androgen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
intracellular receptor signaling pathwayAndrogen receptorHomo sapiens (human)
positive regulation of intracellular estrogen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
Leydig cell differentiationAndrogen receptorHomo sapiens (human)
multicellular organism growthAndrogen receptorHomo sapiens (human)
positive regulation of phosphorylationAndrogen receptorHomo sapiens (human)
positive regulation of MAPK cascadeAndrogen receptorHomo sapiens (human)
positive regulation of insulin-like growth factor receptor signaling pathwayAndrogen receptorHomo sapiens (human)
positive regulation of cell differentiationAndrogen receptorHomo sapiens (human)
negative regulation of integrin biosynthetic processAndrogen receptorHomo sapiens (human)
positive regulation of integrin biosynthetic processAndrogen receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionAndrogen receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIAndrogen receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIIAndrogen receptorHomo sapiens (human)
insulin-like growth factor receptor signaling pathwayAndrogen receptorHomo sapiens (human)
regulation of developmental growthAndrogen receptorHomo sapiens (human)
animal organ formationAndrogen receptorHomo sapiens (human)
male genitalia morphogenesisAndrogen receptorHomo sapiens (human)
epithelial cell proliferationAndrogen receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationAndrogen receptorHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityAndrogen receptorHomo sapiens (human)
activation of prostate induction by androgen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
morphogenesis of an epithelial foldAndrogen receptorHomo sapiens (human)
lateral sprouting involved in mammary gland duct morphogenesisAndrogen receptorHomo sapiens (human)
prostate gland growthAndrogen receptorHomo sapiens (human)
prostate gland epithelium morphogenesisAndrogen receptorHomo sapiens (human)
epithelial cell differentiation involved in prostate gland developmentAndrogen receptorHomo sapiens (human)
tertiary branching involved in mammary gland duct morphogenesisAndrogen receptorHomo sapiens (human)
mammary gland alveolus developmentAndrogen receptorHomo sapiens (human)
positive regulation of epithelial cell proliferation involved in prostate gland developmentAndrogen receptorHomo sapiens (human)
cellular response to steroid hormone stimulusAndrogen receptorHomo sapiens (human)
cellular response to estrogen stimulusAndrogen receptorHomo sapiens (human)
cellular response to testosterone stimulusAndrogen receptorHomo sapiens (human)
seminiferous tubule developmentAndrogen receptorHomo sapiens (human)
non-membrane-bounded organelle assemblyAndrogen receptorHomo sapiens (human)
positive regulation of miRNA transcriptionAndrogen receptorHomo sapiens (human)
regulation of protein localization to plasma membraneAndrogen receptorHomo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathwayAndrogen receptorHomo sapiens (human)
male gonad developmentAndrogen receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayAndrogen receptorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
xenobiotic metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of glucose metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of steroid metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor ROR-gammaHomo sapiens (human)
circadian regulation of gene expressionNuclear receptor ROR-gammaHomo sapiens (human)
cellular response to sterolNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of circadian rhythmNuclear receptor ROR-gammaHomo sapiens (human)
regulation of fat cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor ROR-gammaHomo sapiens (human)
adipose tissue developmentNuclear receptor ROR-gammaHomo sapiens (human)
T-helper 17 cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
regulation of transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (27)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingAndrogen receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingAndrogen receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificAndrogen receptorHomo sapiens (human)
RNA polymerase II general transcription initiation factor bindingAndrogen receptorHomo sapiens (human)
transcription coactivator bindingAndrogen receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificAndrogen receptorHomo sapiens (human)
chromatin bindingAndrogen receptorHomo sapiens (human)
DNA-binding transcription factor activityAndrogen receptorHomo sapiens (human)
nuclear receptor activityAndrogen receptorHomo sapiens (human)
G protein-coupled receptor activityAndrogen receptorHomo sapiens (human)
signaling receptor bindingAndrogen receptorHomo sapiens (human)
steroid bindingAndrogen receptorHomo sapiens (human)
androgen bindingAndrogen receptorHomo sapiens (human)
protein bindingAndrogen receptorHomo sapiens (human)
beta-catenin bindingAndrogen receptorHomo sapiens (human)
zinc ion bindingAndrogen receptorHomo sapiens (human)
enzyme bindingAndrogen receptorHomo sapiens (human)
ATPase bindingAndrogen receptorHomo sapiens (human)
molecular adaptor activityAndrogen receptorHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingAndrogen receptorHomo sapiens (human)
POU domain bindingAndrogen receptorHomo sapiens (human)
molecular condensate scaffold activityAndrogen receptorHomo sapiens (human)
estrogen response element bindingAndrogen receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
protein bindingNuclear receptor ROR-gammaHomo sapiens (human)
oxysterol bindingNuclear receptor ROR-gammaHomo sapiens (human)
zinc ion bindingNuclear receptor ROR-gammaHomo sapiens (human)
ligand-activated transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
nuclear receptor activityNuclear receptor ROR-gammaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
plasma membraneAndrogen receptorHomo sapiens (human)
nucleusAndrogen receptorHomo sapiens (human)
nucleoplasmAndrogen receptorHomo sapiens (human)
cytoplasmAndrogen receptorHomo sapiens (human)
cytosolAndrogen receptorHomo sapiens (human)
nuclear speckAndrogen receptorHomo sapiens (human)
chromatinAndrogen receptorHomo sapiens (human)
protein-containing complexAndrogen receptorHomo sapiens (human)
nucleusAndrogen receptorHomo sapiens (human)
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
nucleoplasmNuclear receptor ROR-gammaHomo sapiens (human)
nuclear bodyNuclear receptor ROR-gammaHomo sapiens (human)
chromatinNuclear receptor ROR-gammaHomo sapiens (human)
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (56)

Assay IDTitleYearJournalArticle
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346888Human Androgen receptor (3C. 3-Ketosteroid receptors)2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID286656Agonist activity at human androgen receptor expressed in CV1 cells by transcriptional activation assay2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
AID286657Antagonist activity at human androgen receptor expressed in CV1 cells by transcriptional activation assay2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID286663Effect on ventral prostate weight in castrated male Sprague-Dawley rat at 100 mg/kg for 28 days, po relative to intact control2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID286662Effect on Levator ani muscle weight in castrated male Sprague-Dawley rat at 100 mg/kg for 28 days, po relative to intact control2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID286658Displacement of [3H]DHT from human AR expressed in MDA-MB-453 cells2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
AID1797703AR Transcriptional Activation Assay and MDA Whole-Cell Binding Assay from Article 10.1021/jm061329j: \\Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.\\2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (416)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990347 (83.41)18.7374
1990's43 (10.34)18.2507
2000's13 (3.13)29.6817
2010's11 (2.64)24.3611
2020's2 (0.48)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials61 (14.02%)5.53%
Reviews12 (2.76%)6.00%
Case Studies34 (7.82%)4.05%
Observational0 (0.00%)0.25%
Other328 (75.40%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Androgen Therapy for Management of Estrogen/Progesterone Receptor Negative ER(-)PR(-) Metastatic Breast Cancer, Phase II Study [NCT00303615]Phase 25 participants (Actual)Interventional2005-06-30Terminated(stopped due to Low accrural)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]