Compounds > 4-hydroxytoremifene
Page last updated: 2024-11-10

4-hydroxytoremifene

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Description

4-hydroxytoremifene: metabolite of toremifene; RN refers to (Z)-isomer; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3035198
CHEMBL ID1402
SCHEMBL ID9099337
MeSH IDM0172401

Synonyms (27)

Synonym
4-[(1z)-4-chloro-1-{4-[2-(dimethylamino)ethoxy]phenyl}-2-phenylbut-1-en-1-yl]phenol
bdbm22423
4-hydroxytoremifene
phenol, 4-((1z)-4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenyl-1-buten-1-yl)-
4-hydroxytormifene
CHEMBL1402
(z)-4-hydroxytoremifene
SCHEMBL9099337
wtw99894i6 ,
phenol, 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenyl-1-butenyl)-, (z)-
(z)-4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenyl-1-butenyl)phenol
unii-wtw99894i6
110503-62-3
z-4-chloro-1-(4-hydroxyphenyl) -1-[4-[2-(n,n-dimethylamino)ethoxy]phenyl]-2-phenyl-1-butene
OIUCUUXSMIJSEB-QPLCGJKRSA-N
tore ii
Q27292838
4-[(z)-4-chloro-1-[4-[2-(dimethylamino)ethoxy] phenyl]-2-phenylbut-1-enyl]phenol
4-hydroxy tor
4 hydroxytoremifene
4hydroxytoremifene
4oh-tor
4-[(z)-4-chloro-1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol
PD015530
(z)-4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-en-1-yl)phenol
DTXSID301043030
AKOS040749970

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
"A multicenter phase I pharmacokinetic study of a new triphenylethylene antiestrogen, toremifene, was examined in 70 patients with advanced breast cancer."( Pharmacokinetics of toremifene and its metabolites in patients with advanced breast cancer.
Benz, CC; Cadman, TB; DeGregorio, MW; Shemano, I; Wiebe, VJ, 1990)		0.28

Dosage Studied

ExcerptRelevanceReference
" The plasma concentrations of TOR and its N-desmethyl (NDM) and 4-hydroxy (4-OH) metabolites during steady-state dosing with TOR were also determined."( Role and pharmacologic significance of cytochrome P-450 2D6 in oxidative metabolism of toremifene and tamoxifen.
Barrett, CM; Bohl, CE; Coss, CC; Dalton, JT; He, Y; Kim, J; Li, CM; Mohler, ML; Veverka, KA, 2013)		0.39
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Estrogen receptorHomo sapiens (human)IC50 (µMol)0.00700.00000.723732.7000AID1798194; AID260520
Estrogen-related receptor gammaHomo sapiens (human)IC50 (µMol)0.01000.00200.22732.0000AID1798194; AID260519
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sulfotransferase 1E1Homo sapiens (human)Km6.40001.60004.63676.4000AID1222648
Sulfotransferase 1A1Homo sapiens (human)Km2.60000.17001.83436.6200AID1222647
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (55)

Processvia Protein(s)Taxonomy
positive regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
antral ovarian follicle growthEstrogen receptorHomo sapiens (human)
epithelial cell developmentEstrogen receptorHomo sapiens (human)
chromatin remodelingEstrogen receptorHomo sapiens (human)
regulation of DNA-templated transcriptionEstrogen receptorHomo sapiens (human)
signal transductionEstrogen receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayEstrogen receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationEstrogen receptorHomo sapiens (human)
androgen metabolic processEstrogen receptorHomo sapiens (human)
male gonad developmentEstrogen receptorHomo sapiens (human)
negative regulation of gene expressionEstrogen receptorHomo sapiens (human)
positive regulation of phospholipase C activityEstrogen receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayEstrogen receptorHomo sapiens (human)
intracellular estrogen receptor signaling pathwayEstrogen receptorHomo sapiens (human)
response to estradiolEstrogen receptorHomo sapiens (human)
regulation of toll-like receptor signaling pathwayEstrogen receptorHomo sapiens (human)
negative regulation of smooth muscle cell apoptotic processEstrogen receptorHomo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionEstrogen receptorHomo sapiens (human)
negative regulation of DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
response to estrogenEstrogen receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionEstrogen receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
fibroblast proliferationEstrogen receptorHomo sapiens (human)
positive regulation of fibroblast proliferationEstrogen receptorHomo sapiens (human)
stem cell differentiationEstrogen receptorHomo sapiens (human)
regulation of inflammatory responseEstrogen receptorHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
RNA polymerase II preinitiation complex assemblyEstrogen receptorHomo sapiens (human)
uterus developmentEstrogen receptorHomo sapiens (human)
vagina developmentEstrogen receptorHomo sapiens (human)
prostate epithelial cord elongationEstrogen receptorHomo sapiens (human)
prostate epithelial cord arborization involved in prostate glandular acinus morphogenesisEstrogen receptorHomo sapiens (human)
regulation of branching involved in prostate gland morphogenesisEstrogen receptorHomo sapiens (human)
mammary gland branching involved in pregnancyEstrogen receptorHomo sapiens (human)
mammary gland alveolus developmentEstrogen receptorHomo sapiens (human)
epithelial cell proliferation involved in mammary gland duct elongationEstrogen receptorHomo sapiens (human)
protein localization to chromatinEstrogen receptorHomo sapiens (human)
cellular response to estradiol stimulusEstrogen receptorHomo sapiens (human)
negative regulation of miRNA transcriptionEstrogen receptorHomo sapiens (human)
regulation of epithelial cell apoptotic processEstrogen receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
cellular response to estrogen stimulusEstrogen receptorHomo sapiens (human)
sulfationSulfotransferase 1E1Homo sapiens (human)
ethanol catabolic processSulfotransferase 1E1Homo sapiens (human)
estrogen catabolic processSulfotransferase 1E1Homo sapiens (human)
steroid metabolic processSulfotransferase 1E1Homo sapiens (human)
estrogen metabolic processSulfotransferase 1E1Homo sapiens (human)
positive regulation of fat cell differentiationSulfotransferase 1E1Homo sapiens (human)
3'-phosphoadenosine 5'-phosphosulfate metabolic processSulfotransferase 1E1Homo sapiens (human)
sulfationSulfotransferase 1E1Homo sapiens (human)
sulfationSulfotransferase 1A1Homo sapiens (human)
ethanol catabolic processSulfotransferase 1A1Homo sapiens (human)
catecholamine metabolic processSulfotransferase 1A1Homo sapiens (human)
xenobiotic metabolic processSulfotransferase 1A1Homo sapiens (human)
estrogen metabolic processSulfotransferase 1A1Homo sapiens (human)
amine metabolic processSulfotransferase 1A1Homo sapiens (human)
flavonoid metabolic processSulfotransferase 1A1Homo sapiens (human)
3'-phosphoadenosine 5'-phosphosulfate metabolic processSulfotransferase 1A1Homo sapiens (human)
sulfationSulfotransferase 1A1Homo sapiens (human)
regulation of DNA-templated transcriptionEstrogen-related receptor gammaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEstrogen-related receptor gammaHomo sapiens (human)
retinoic acid receptor signaling pathwayEstrogen-related receptor gammaHomo sapiens (human)
positive regulation of cold-induced thermogenesisEstrogen-related receptor gammaHomo sapiens (human)
regulation of transcription by RNA polymerase IIEstrogen-related receptor gammaHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayEstrogen-related receptor gammaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (34)

Processvia Protein(s)Taxonomy
RNA polymerase II cis-regulatory region sequence-specific DNA bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificEstrogen receptorHomo sapiens (human)
TFIIB-class transcription factor bindingEstrogen receptorHomo sapiens (human)
transcription coregulator bindingEstrogen receptorHomo sapiens (human)
transcription corepressor bindingEstrogen receptorHomo sapiens (human)
transcription coactivator bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificEstrogen receptorHomo sapiens (human)
chromatin bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
nuclear receptor activityEstrogen receptorHomo sapiens (human)
steroid bindingEstrogen receptorHomo sapiens (human)
protein bindingEstrogen receptorHomo sapiens (human)
calmodulin bindingEstrogen receptorHomo sapiens (human)
beta-catenin bindingEstrogen receptorHomo sapiens (human)
zinc ion bindingEstrogen receptorHomo sapiens (human)
TBP-class protein bindingEstrogen receptorHomo sapiens (human)
enzyme bindingEstrogen receptorHomo sapiens (human)
protein kinase bindingEstrogen receptorHomo sapiens (human)
nitric-oxide synthase regulator activityEstrogen receptorHomo sapiens (human)
nuclear estrogen receptor activityEstrogen receptorHomo sapiens (human)
nuclear estrogen receptor bindingEstrogen receptorHomo sapiens (human)
estrogen response element bindingEstrogen receptorHomo sapiens (human)
identical protein bindingEstrogen receptorHomo sapiens (human)
ATPase bindingEstrogen receptorHomo sapiens (human)
14-3-3 protein bindingEstrogen receptorHomo sapiens (human)
sequence-specific double-stranded DNA bindingEstrogen receptorHomo sapiens (human)
estrone sulfotransferase activitySulfotransferase 1E1Homo sapiens (human)
steroid bindingSulfotransferase 1E1Homo sapiens (human)
protein bindingSulfotransferase 1E1Homo sapiens (human)
sulfotransferase activitySulfotransferase 1E1Homo sapiens (human)
flavonol 3-sulfotransferase activitySulfotransferase 1E1Homo sapiens (human)
steroid sulfotransferase activitySulfotransferase 1E1Homo sapiens (human)
aryl sulfotransferase activitySulfotransferase 1E1Homo sapiens (human)
aryl sulfotransferase activitySulfotransferase 1A1Homo sapiens (human)
protein bindingSulfotransferase 1A1Homo sapiens (human)
sulfotransferase activitySulfotransferase 1A1Homo sapiens (human)
flavonol 3-sulfotransferase activitySulfotransferase 1A1Homo sapiens (human)
steroid sulfotransferase activitySulfotransferase 1A1Homo sapiens (human)
3'-phosphoadenosine 5'-phosphosulfate bindingSulfotransferase 1A1Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificEstrogen-related receptor gammaHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificEstrogen-related receptor gammaHomo sapiens (human)
nuclear steroid receptor activityEstrogen-related receptor gammaHomo sapiens (human)
steroid bindingEstrogen-related receptor gammaHomo sapiens (human)
protein bindingEstrogen-related receptor gammaHomo sapiens (human)
zinc ion bindingEstrogen-related receptor gammaHomo sapiens (human)
AF-2 domain bindingEstrogen-related receptor gammaHomo sapiens (human)
sequence-specific double-stranded DNA bindingEstrogen-related receptor gammaHomo sapiens (human)
estrogen response element bindingEstrogen-related receptor gammaHomo sapiens (human)
nuclear receptor activityEstrogen-related receptor gammaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
nucleusEstrogen receptorHomo sapiens (human)
nucleoplasmEstrogen receptorHomo sapiens (human)
transcription regulator complexEstrogen receptorHomo sapiens (human)
cytoplasmEstrogen receptorHomo sapiens (human)
Golgi apparatusEstrogen receptorHomo sapiens (human)
cytosolEstrogen receptorHomo sapiens (human)
plasma membraneEstrogen receptorHomo sapiens (human)
membraneEstrogen receptorHomo sapiens (human)
chromatinEstrogen receptorHomo sapiens (human)
euchromatinEstrogen receptorHomo sapiens (human)
protein-containing complexEstrogen receptorHomo sapiens (human)
nucleusEstrogen receptorHomo sapiens (human)
cytosolSulfotransferase 1E1Homo sapiens (human)
nuclear membraneSulfotransferase 1E1Homo sapiens (human)
cytoplasmSulfotransferase 1E1Homo sapiens (human)
cytosolSulfotransferase 1A1Homo sapiens (human)
cytoplasmSulfotransferase 1A1Homo sapiens (human)
nucleoplasmEstrogen-related receptor gammaHomo sapiens (human)
chromatinEstrogen-related receptor gammaHomo sapiens (human)
nucleusEstrogen-related receptor gammaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (22)

Assay IDTitleYearJournalArticle
AID1222667Drug metabolism in human liver cytosol assessed as SULT1A1 3'UTR ACG/GTA copy number-3-mediated 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenyl hydrogen sulfate formation by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID1222647Activity of human SULT1A1 expressed in escherichia coli assessed as enzyme-mediated 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenyl hydrogen sulfate formation after 15 mins by Michaelis-Menten equation in presence of 20 uM PAPS2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID1222648Activity of human SULT1E1 expressed in escherichia coli assessed as enzyme-mediated 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenyl hydrogen sulfate formation after 15 mins by Michaelis-Menten equation in presence of 20 uM PAPS2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID1222650Activity of human SULT1A1 expressed in escherichia coli assessed as enzyme-mediated 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenyl hydrogen sulfate formation measured per mg of protein after 15 mins by Michaelis-Menten equatio2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID1222657Drug metabolism in human liver cytosol assessed as SULT1A1 copy number-1-mediated 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenyl hydrogen sulfate formation by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID1222665Drug metabolism in human liver cytosol assessed as SULT1A1 3'UTR GTA/GTA copy number-2-mediated 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenyl hydrogen sulfate formation by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID260521Selectivity for ERRgamma over ERalpha relative to 4-hydroxytamoxifen2006Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
AID1222653Drug metabolism in human liver cytosol assessed as 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenyl hydrogen sulfate formation measured per mg of protein treated with 0.1 to 30 after 15 mins by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID1222651Activity of human SULT1E1 expressed in escherichia coli assessed as enzyme-mediated 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenyl hydrogen sulfate formation measured per mg of protein after 15 mins by Michaelis-Menten equatio2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID1222666Drug metabolism in human liver cytosol assessed as SULT1A1 3'UTR ACG/ACG copy number-3-mediated 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenyl hydrogen sulfate formation by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID1222655Drug metabolism in human liver cytosol assessed as SULT1A1*1/2 single nucleotide polymorphism-mediated 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenyl hydrogen sulfate formation by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID1222654Drug metabolism in human liver cytosol assessed as 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenyl hydrogen sulfate formation after 15 mins by HPLC analysis in presence of 20 uM PAPS and 0.1 to 10 uM SULT1A1 inhibitor DCNP2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID1222663Drug metabolism in human liver cytosol assessed as SULT1A1 3'UTR ACG/ACG copy number-2 -mediated 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenyl hydrogen sulfate formation by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID260519Displacement of [3H]4-OHT from ERRgamma2006Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
AID260520Displacement of [3H]estradiol from ERalpha2006Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
AID1222673Retention time of the compound2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID1222658Drug metabolism in human liver cytosol assessed as SULT1A1 copy number-2-mediated 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenyl hydrogen sulfate formation by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID1222652Drug metabolism in human liver cytosol assessed as 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenyl hydrogen sulfate formation measured per mg of protein after 15 mins by Michaelis-Menten equation in presence of 20 uM PAPS2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID1222659Drug metabolism in human liver cytosol assessed as SULT1A1 copy number-3-mediated 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenyl hydrogen sulfate formation by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID1222649Drug metabolism in human liver cytosol assessed as 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenyl hydrogen sulfate formation after 15 mins by Michaelis-Menten equation in presence of 20 uM PAPS2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID1222664Drug metabolism in human liver cytosol assessed as SULT1A1 3'UTR ACG/GTA copy number-2-mediated 4-(4-chloro-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenyl hydrogen sulfate formation by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Sulfation of 4-hydroxy toremifene: individual variability, isoform specificity, and contribution to toremifene pharmacogenomics.
AID1798194Radioligand Displacement Assay from Article 10.1016/j.bmcl.2005.11.030: \\Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.\\2006Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (45.45)18.2507
2000's3 (27.27)29.6817
2010's3 (27.27)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.88

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.88 (24.57)
Research Supply Index2.64 (2.92)
Research Growth Index4.52 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.88)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (8.33%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (91.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
quinone
benzoquinone : The simplest members of the class of benzoquinones, consisting of cyclohexadiene which is substituted by two oxo groups.. 1,4-benzoquinone : The simplest member of the class of 1,4-benzoquinones, obtained by the formal oxidation of hydroquinone to the corresponding diketone. It is a metabolite of benzene.. quinone : Compounds having a fully conjugated cyclic dione structure, such as that of benzoquinones, derived from aromatic compounds by conversion of an even number of -CH= groups into -C(=O)- groups with any necessary rearrangement of double bonds (polycyclic and heterocyclic analogues are included).		2101,4-benzoquinonescofactor;
human xenobiotic metabolite;
mouse metabolite
9,10-dimethyl-1,2-benzanthracene
9,10-Dimethyl-1,2-benzanthracene: Polycyclic aromatic hydrocarbon found in tobacco smoke that is a potent carcinogen.. 7,12-dimethyltetraphene : A tetraphene having methyl substituents at the 7- and 12-positions. It is a potent carcinogen and is present in tobacco smoke.		1.9710ortho-fused polycyclic arene;
tetraphenes		carcinogenic agent
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol
[no description available]		2.0310stilbenoid
quinone methide
quinone methide: intermediate in eumelanin biosynthesis; structure given in first source. quinomethane : A methylidenecyclohexadienone, formally derived from a benzoquinone by replacement of one of the quinone oxygens by a methylidene group.		2.4120quinomethane
afimoxifene
afimoxifene : A tertiary amino compound that is tamoxifen in which the phenyl group which is in a Z- relationship to the ethyl substituent is hydroxylated at the para- position. It is the active metabolite of tamoxifen.		3.5180phenols;
tertiary amino compound		antineoplastic agent;
estrogen receptor antagonist;
metabolite
enclomiphene
Enclomiphene: The trans or (E)-isomer of clomiphene.		1.9910
tamoxifen
[no description available]		5.09101stilbenoid;
tertiary amino compound		angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator
toremifene
Toremifene: A first generation selective estrogen receptor modulator (SERM). Like TAMOXIFEN, it is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on mammary and uterine tissue.		591aromatic ether;
organochlorine compound;
tertiary amine		antineoplastic agent;
bone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
droloxifene
[no description available]		2.420stilbenoid
n-desmethyltoremifene
N-desmethyltoremifene: metabolite of toremifene; structure given in first source; RN given refers to (Z)-isomer		3.3611stilbenoid
afimoxifene
[no description available]		2.0310
n-desmethyltamoxifen
N-desmethyltamoxifen: main metabolite of tamoxifen; RN given refers to (Z)-isomer		1.9810stilbenoid
gsk5182
GSK5182: an estrogen-related receptor gamma inverse agonist		2.0310
ConditionIndicatedRelationship StrengthStudiesTrials
Breast Cancer
[description not available]		04.2941
Cancer of Lung
[description not available]		01.9810
Breast Neoplasms
Tumors or cancer of the human BREAST.		04.2941
Lung Neoplasms
Tumors or cancer of the LUNG.		01.9810
Aneuploid
[description not available]		01.9910
Experimental Mammary Neoplasms
[description not available]		01.9710