Page last updated: 2024-12-07

ly 117018

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Description

LY 117018: from Eli Lilly; less estrogenic & more estrogen-antagonistic than tamoxifen & trioxifene in rats & mice; LY 139478 is the HCl salt of LY 117018; LY 139478 is an estrogen agonist; structure in first source; a raloxifene analog [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

LY 117018 : A member of the class of 1-benzothiophenes that is raloxifene in which the piperidin-1-yl group has been replaced by a pyrrolidin-1-yl group. [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]

Cross-References

ID SourceID
PubMed CID104946
CHEMBL ID10030
CHEBI ID90187
SCHEMBL ID4884822
MeSH IDM0084762

Synonyms (32)

Synonym
ly-117018
[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothien-3-yl][4-(2-pyrrolidin-1-ylethoxy)phenyl]methanone
LLC ,
ly 139478
ly 117018
6-hydroxy-2-(4-hydroxyphenyl)benzo(b)thien-3-yl 4-(2-(1-pyrrolidinyl)ethoxy) phenyl ketone
methanone, (6-hydroxy-2-(4-hydroxyphenyl)benzo(b)thien-3-yl)(4-(2-(1-pyrrolidinyl)ethoxy)phenyl)-
lilly 117018
ly-139478
ly117018
63676-25-5
chebi:90187 ,
CHEMBL10030
[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]{4-[2-(pyrrolidin-1-yl)ethoxy]phenyl}methanone
[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]methanone
unii-9fqt7vsr3v
9fqt7vsr3v ,
SCHEMBL4884822
6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-pyrrolidinoethoxy)benzoyl]benzo[b]thiophene
JLERVPBPJHKRBJ-UHFFFAOYSA-N
6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl 4-[2-(1-pyrrolidinyl)ethoxy] phenyl ketone
DTXSID80213055
phenethipylone
[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl][4-(2-pyrrolidin-1-ylethoxy)phenyl]methanone
Q27162388
HY-116896
bdbm50230557
2-(4-hydroxyphenyl)-3-(4-(2-(pyrrolidin-1-yl)ethoxy)benzoyl)-1-benzothiophen-6-ol
(6-hydroxy-2-(4-hydroxyphenyl)benzo(b)thien-3-yl)(4-(2-(1-pyrrolidinyl)ethoxy)phenyl)methanone
CS-0066774
(s)-(-)-3-(acetylthio)isobutyricacid
AKOS040741982

Research Excerpts

Overview

LY 117018 has been shown to antagonize more effectively than tamoxifen the effects of estradiol in rats and mice.

ExcerptReferenceRelevance
"LY 117018 is a nonsteroidal compound which has been shown to antagonize more effectively than tamoxifen the effects of estradiol in rats and mice. "( Antiestrogenic effects of LY 117018 in MCF-7 cells.
Huff, KK; Lippman, ME; Scholl, SM, 1983
)
2.01

Dosage Studied

ExcerptRelevanceReference
" Estrogens are approximately 10-fold more potent in stimulating cell number than in stimulating prolactin production, but the antiestrogens showed the same dose-response for both effects."( Characterization of antiestrogen stimulation of cell number and prolactin production.
Amara, JF; Dannies, PS, 1986
)
0.27
" The dose-response relationship was biphasic; 10(-10) M Ly-117018 and 10(-7) M tamoxifen caused maximal stimulation, but higher concentrations caused no stimulation and completely antagonized the 5-fold stimulation caused by estrogen."( Antiestrogens are partial estrogen agonists for prolactin production in primary pituitary cultures.
Amara, JF; Dannies, PS; Martinez-Campos, A, 1986
)
0.27
" The partial uterotrophic effect of monohydroxytamoxifen and full uterotrophic effects of estradiol were both inhibited by high doses of LY117018 at an approximate dosage ratio of 1:24, w/w."( Differential antiestrogen action in the immature rat uterus: a comparison of hydroxylated antiestrogens with high affinity for the estrogen receptor.
Gosden, B; Jordan, VC, 1983
)
0.27
" However, in the rat, LY117018 was more effective against the less potent compound tamoxifen, at a 6:1 dosage ratio compared with a 24:1 dosage ratio required for the potent compound monohydroxytamoxifen."( Inhibition of the uterotropic activity of estrogens and antiestrogens by the short acting antiestrogen LY117018.
Gosden, B; Jordan, VC, 1983
)
0.27
" In the present investigation, female MRL lpr/lpr mice have been dosed po daily for 7 months with the selective estrogen receptor modulator (SERM) LY139478 (4 mg/kg) or 17alpha-ethinylestradiol (EE2, 1 mg/kg) and compared to vehicle control animals."( The effect of a selective estrogen receptor modulator on the progression of spontaneous autoimmune disease in MRL lpr/lpr mice.
Apelgren, LD; Bailey, DL; Bryan, N; Bumol, TF; Evans, GF; Fouts, RL; Glasebrook, A; Sandusky, GE; Short, L; Zuckerman, SH, 1996
)
0.29
" Dilator responses to acetylcholine (ACh; 10[8] to 10[-5] M) were obtained in phenylephrine (PE; 2 microM)-contracted aorta, and constrictor dose-response curves to PE (10[-8] to 10[-5] M) were generated before and after pretreatment with N omega-nitro-L-arginine methyl ester (L-NAME; 200 microM), an inhibitor of nitric oxide synthase."( Estrogen and selective estrogen receptor modulator LY117018 enhance release of nitric oxide in rat aorta.
Dube, G; Laher, I; Rahimian, R; van Breemen, C, 1997
)
0.3
"To test the hypothesis that an antiresorptive agent might reduce the dosing requirement for an anabolic drug during reversal of osteopenia due to estrogen deficiency, the following experiment was conducted in 6-month-old female rats."( The addition of a raloxifene analog (LY117018) allows for reduced PTH(1-34) dosing during reversal of osteopenia in ovariectomized rats.
Bryant, H; Drost, D; Fraher, LJ; Hock, J; Hodsman, AB; Holdsworth, D; Thornton, M; Watson, PH, 1999
)
0.3
"This experiment was designed to evaluate the ability of a raloxifene analogue (RA), LY117018, with or without reduced dosing of human parathyroid hormone (hPTH)(1-34) to maintain gains in bone mass after a fully anabolic treatment regimen given to aging osteopenic rats."( Assessment of maintenance therapy with reduced doses of PTH(1-34) in combination with a raloxifene analogue (LY117018) following anabolic therapy in the ovariectomized rat.
Bryant, H; Drost, D; Fraher, LJ; Hock, J; Hodsman, AB; Holdsworth, D; Thornton, M; Watson, PH, 1999
)
0.3
" Similar dose-response curves were obtained with a combined treatment of IGF-I and E2 with a 2log shift."( Anti-growth factor activities of benzothiophenes in human breast cancer cells.
Aknin, C; Chalbos, D; Freiss, G; Galtier, F; Maudelonde, T; Puech, C; Vignon, F, 2005
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
estrogen receptor antagonistAn antagonist at the estrogen receptor.
estrogen receptor modulatorA substance that possess antiestrogenic actions but can also produce estrogenic effects as well. It acts as complete or partial agonist or as antagonist. It can be either steroidal or nonsteroidal in structure.
bone density conservation agentAn agent that inhibits bone resorption and/or favor bone mineralization and bone regeneration. Used to heal bone fractures and to treat bone diseases such as osteopenia and osteoporosis.
[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 (4)

ClassDescription
1-benzothiophenes
phenolsOrganic aromatic compounds having one or more hydroxy groups attached to a benzene or other arene ring.
aromatic ketoneA ketone in which the carbonyl group is attached to an aromatic ring.
N-alkylpyrrolidine
[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 (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Estrogen receptorHomo sapiens (human)IC50 (µMol)0.12000.00000.723732.7000AID68750
Estrogen receptor betaHomo sapiens (human)IC50 (µMol)0.12000.00010.529432.7000AID68750
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (44)

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)
negative regulation of transcription by RNA polymerase IIEstrogen receptor betaHomo sapiens (human)
regulation of DNA-templated transcriptionEstrogen receptor betaHomo sapiens (human)
signal transductionEstrogen receptor betaHomo sapiens (human)
cell-cell signalingEstrogen receptor betaHomo sapiens (human)
negative regulation of cell growthEstrogen receptor betaHomo sapiens (human)
intracellular estrogen receptor signaling pathwayEstrogen receptor betaHomo sapiens (human)
positive regulation of DNA-templated transcriptionEstrogen receptor betaHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityEstrogen receptor betaHomo sapiens (human)
cellular response to estradiol stimulusEstrogen receptor betaHomo sapiens (human)
regulation of transcription by RNA polymerase IIEstrogen receptor betaHomo sapiens (human)
cellular response to estrogen stimulusEstrogen receptor betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (29)

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)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingEstrogen receptor betaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificEstrogen receptor betaHomo sapiens (human)
DNA bindingEstrogen receptor betaHomo sapiens (human)
nuclear steroid receptor activityEstrogen receptor betaHomo sapiens (human)
nuclear receptor activityEstrogen receptor betaHomo sapiens (human)
steroid bindingEstrogen receptor betaHomo sapiens (human)
protein bindingEstrogen receptor betaHomo sapiens (human)
zinc ion bindingEstrogen receptor betaHomo sapiens (human)
enzyme bindingEstrogen receptor betaHomo sapiens (human)
nuclear estrogen receptor activityEstrogen receptor betaHomo sapiens (human)
estrogen response element bindingEstrogen receptor betaHomo sapiens (human)
receptor antagonist activityEstrogen receptor betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

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)
nucleusEstrogen receptor betaHomo sapiens (human)
nucleoplasmEstrogen receptor betaHomo sapiens (human)
mitochondrionEstrogen receptor betaHomo sapiens (human)
intracellular membrane-bounded organelleEstrogen receptor betaHomo sapiens (human)
chromatinEstrogen receptor betaHomo sapiens (human)
nucleusEstrogen receptor betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (20)

Assay IDTitleYearJournalArticle
AID187060Estrogenic activity as mean uterine weight in rats on 10 ug dose1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans.
AID68750Displacement of [3H]estradiol from Estrogen receptor in MCF-7 cells1992Journal of medicinal chemistry, Mar-06, Volume: 35, Issue:5
Antiestrogens. 3. Estrogen receptor affinities and antiproliferative effects in MCF-7 cells of phenolic analogues of trioxifene, [3,4-dihydro-2-(4- methoxyphenyl)-1-naphthalenyl][4-[2-(1-pyrrolidinyl)ethoxy]- phenyl]methanone.
AID69701Association constant for estrogen receptor1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Molecular structures, conformational analysis, and preferential modes of binding of 3-aroyl-2-arylbenzo[b]thiophene estrogen receptor ligands: LY117018 and aryl azide photoaffinity labeling analogs.
AID69839Relative binding affinity for lamb uterine estrogen receptor by displacement of [3H]estradiol1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Molecular structures, conformational analysis, and preferential modes of binding of 3-aroyl-2-arylbenzo[b]thiophene estrogen receptor ligands: LY117018 and aryl azide photoaffinity labeling analogs.
AID69531Relative binding affinity against estrogen receptor(ER)1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans.
AID38620Relative binding affinity(RBA) against AEBS (Antiestrogen binding site) in rat liver1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Synthesis of 2-(p-chlorobenzyl)-3-aryl-6-methoxybenzofurans as selective ligands for antiestrogen-binding sites. Effects on cell proliferation and cholesterol synthesis.
AID186921The compound was tested for uterotropic activity in immature rats(Dosage 1000 ug)1984Journal of medicinal chemistry, Aug, Volume: 27, Issue:8
Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec
AID186918The compound was tested for anti-uterotrophic activity in immature rats(Dosage 100 ug)1984Journal of medicinal chemistry, Aug, Volume: 27, Issue:8
Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec
AID185420Percent inhibition of estradiol stimulated uterine growth in rats1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans.
AID55209Inhibition of Calmodulin activation of cyclic nucleotide phosphodiesterase1992Journal of medicinal chemistry, Mar-06, Volume: 35, Issue:5
Antiestrogens. 3. Estrogen receptor affinities and antiproliferative effects in MCF-7 cells of phenolic analogues of trioxifene, [3,4-dihydro-2-(4- methoxyphenyl)-1-naphthalenyl][4-[2-(1-pyrrolidinyl)ethoxy]- phenyl]methanone.
AID187052The compound was tested for uterotropic activity in immature rats(Dosage 100 ug)1984Journal of medicinal chemistry, Aug, Volume: 27, Issue:8
Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec
AID69075Binding affinity for Estrogen receptor in MCF-Cells relative to estradiol1992Journal of medicinal chemistry, Mar-06, Volume: 35, Issue:5
Antiestrogens. 3. Estrogen receptor affinities and antiproliferative effects in MCF-7 cells of phenolic analogues of trioxifene, [3,4-dihydro-2-(4- methoxyphenyl)-1-naphthalenyl][4-[2-(1-pyrrolidinyl)ethoxy]- phenyl]methanone.
AID187054The compound was tested for uterotropic activity in immature rats(Dosage 1 ug)1984Journal of medicinal chemistry, Aug, Volume: 27, Issue:8
Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec
AID186916The compound was tested for anti-uterotrophic activity in immature rats(Dosage 10 microg)1984Journal of medicinal chemistry, Aug, Volume: 27, Issue:8
Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec
AID69054Relative binding affinity(RBA) against Estrogen receptor using MCF-7 cells1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Synthesis of 2-(p-chlorobenzyl)-3-aryl-6-methoxybenzofurans as selective ligands for antiestrogen-binding sites. Effects on cell proliferation and cholesterol synthesis.
AID38726Relative binding affinity against Antiestrogen binding site(AEBS)1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans.
AID186917The compound was tested for anti-uterotrophic activity in immature rats(Dosage 1000 ug)1984Journal of medicinal chemistry, Aug, Volume: 27, Issue:8
Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec
AID187053The compound was tested for uterotropic activity in immature rats(Dosage 10 ug)1984Journal of medicinal chemistry, Aug, Volume: 27, Issue:8
Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec
AID187059Antiestrogenic activity in presence of unlabeled estradiol as mean uterine weight in rats at 0.3 ug dose1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans.
AID186919The compound was tested for anti-uterotrophic activity in immature rats(Dosage 1 ug)1984Journal of medicinal chemistry, Aug, Volume: 27, Issue:8
Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (103)

TimeframeStudies, This Drug (%)All Drugs %
pre-199036 (34.95)18.7374
1990's34 (33.01)18.2507
2000's31 (30.10)29.6817
2010's2 (1.94)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: 9.65

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 Index9.65 (24.57)
Research Supply Index4.66 (2.92)
Research Growth Index4.31 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (9.65)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews4 (3.81%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other101 (96.19%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]