Page last updated: 2024-11-12

ly3201

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Description

LY3201: estrogen receptor beta agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11197931
CHEMBL ID236718
SCHEMBL ID3594257
MeSH IDM0572240

Synonyms (24)

Synonym
DC8 ,
(3as,4r,9br)-2,2-difluoro-4-(4-hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta[c]chromen-8-ol
2Z4B
2Q70
bmcl175563 compound 3a
(2r,6s,7r)-4,4-difluoro-7-(4-hydroxyphenyl)-8-oxatricyclo[7.4.0.0;{2,6}]trideca-1(9),10,12-trien-12-ol
bdbm19982
CHEMBL236718
DB07638
(3as,4r,9br)-2,2-difluoro-4-(4-hydroxy-phenyl)1,2,3,3a,4,9b-hexahydro-cyclopenta[c]chromen-8-ol
(3as, 4r, 9br)-2,2-difluoro-4-(4-hydroxy-phenyl)-1,2,3,3a,4,9b-hexahydro-cyclopenta[c]chromen-8-ol
(3as,4r,9br)-2,2-difluoro-4-(4-hydroxy-phenyl)-1,2,3,3a,4,9b-hexahydro-cyclopenta[c]chromen-8-ol
SCHEMBL3594257
787621-78-7
ly3201
ly 3201
(3as,4r,9br)-2,2-difluoro-4-(4-hydroxyphenyl)-3,3a,4,9b-tetrahydro-1h-cyclopenta(c)chromen-8-ol
(3as,4r,9br)-2,2-difluoro-4-(4-hydroxyphenyl)-3,3a,4,9b-tetrahydro-1h-cyclopenta[c]chromen-8-ol
Q27096857
CS-0166695
PD005600
HY-138690
estrogen receptor modulator 6
AKOS040758349
[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)
Chain A, Estrogen receptorHomo sapiens (human)Ki0.00440.00040.00440.0083AID977610
Chain A, Estrogen receptor betaHomo sapiens (human)Ki0.00440.00040.00440.0083AID977610
Estrogen receptorHomo sapiens (human)Ki0.00570.00000.42297.9070AID1797929; AID1797931; AID300596; AID301350
Estrogen receptor betaHomo sapiens (human)Ki0.00310.00000.12512.8760AID1797929; AID1797931; AID300595; AID301349
[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 (10)

Assay IDTitleYearJournalArticle
AID1811Experimentally measured binding affinity data derived from PDB2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification.
AID1797929Estrogen Receptor Binding Assay. from Article 10.1016/j.bmcl.2007.06.052: \\Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification.\\2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification.
AID1797931Estrogen Receptor Binding Assay. from Article 10.1016/j.bmcl.2007.08.009: \\Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies.\\2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies.
AID301350Binding affinity at ERalpha2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies.
AID300596Binding affinity to human ERalpha2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification.
AID301349Binding affinity at ERbeta2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies.
AID300595Binding affinity to human ERbeta2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification.
AID300597Selectivity for human ERbeta over human ERalpha2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification.
AID301351Selectivity ratio of Ki for ERbeta over Ki for ERalpha2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (25.00)29.6817
2010's5 (62.50)24.3611
2020's1 (12.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.72

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 Index12.72 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.92 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.72)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]