Page last updated: 2024-12-11

1-(4-(6-bromobenzo(1,3)dioxol-5-yl)-3a,4,5,9b-tetrahydro-3h-cyclopenta(c)quinolin-8-yl)ethanone

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

Description

The compound you've described, **1-(4-(6-bromobenzo(1,3)dioxol-5-yl)-3a,4,5,9b-tetrahydro-3h-cyclopenta(c)quinolin-8-yl)ethanone**, is a complex organic molecule with a unique structure.

Here's a breakdown of its significance:

* **Structure:** The compound is a substituted quinoline derivative with a fused cyclopentane ring and a benzodioxole moiety. This specific arrangement of atoms and functional groups is key to its potential biological activity.
* **Potential for Research:** Due to its structure and the presence of a bromine atom and a carbonyl group, this compound likely possesses characteristics that make it interesting for research in various fields. Here's why:

* **Pharmacological Activity:** The presence of the quinoline scaffold and the benzodioxole group are known to be associated with a variety of pharmacological activities. These could include:
* **Anti-inflammatory Properties:** Quinoline derivatives have been shown to exhibit anti-inflammatory effects.
* **Anti-cancer Properties:** Certain quinoline derivatives have anticancer activity.
* **Antimicrobial Properties:** Some quinolines show antibacterial or antifungal properties.
* **Other Potential Applications:** Depending on the specific structural modifications, the compound could have activity in other areas such as neurological disorders, cardiovascular diseases, or even as a dye or pigment.

* **Importance for Research:** To understand the full potential of this compound, researchers would need to:

* **Synthesize and Characterize:** The compound needs to be synthesized in a lab, purified, and its structure confirmed.
* **Biological Activity Testing:** Experiments are needed to assess its potential therapeutic properties (e.g., in vitro cell cultures, animal models).
* **Mechanism of Action:** Research would aim to understand how the compound interacts with biological systems and what cellular pathways it targets.
* **Safety and Toxicity:** Extensive studies are required to assess the compound's safety profile in order to determine its potential for human use.

**In summary, while the compound is complex and has a unique structure, its specific importance for research hinges on its potential pharmacological activity, which remains to be investigated through rigorous experimentation.**

1-(4-(6-bromobenzo(1,3)dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta(c)quinolin-8-yl)ethanone: G-1 was able to induce both c-fos expression and proliferation in the ERalpha-negative/GPR30-positive SKBR3 breast cancer cells, the requirement for ERalpha expression in GPR30/EGFR signaling may depend on the specific cellular context of different tumor types [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5322399
CHEMBL ID569766
CHEBI ID156296
SCHEMBL ID12700948
MeSH IDM0507645

Synonyms (43)

Synonym
lns-8801
lns8801
gtpl1014
1-[4-(6-bromo-benzo[1,3]dioxol-5-yl)-3-alpha-4,5,9-beta-tetrahydro-3h-cyclopenta[c]quinolin-8-yl]-ethanone
ml051
UNM000011063001
UNM000000675701
1-(4-(6-bromobenzo[1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3h-cyclopenta[c]quinolin-8-yl)-ethanone
gpr30 agonist, g-1
STK330808
1-[(3as,4r,9br)-4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3h-cyclopenta[c]quinolin-8-yl]ethanone
CHEBI:156296
gper agonist
CHEMBL569766 ,
cid_3136849
cid_5322399
bdbm50303803
1-((3as,4r,9br)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3h-cyclopenta[c]quinolin-8-yl)ethanone
1-(4-(6-bromobenzo(1,3)dioxol-5-yl)-3a,4,5,9b-tetrahydro-3h-cyclopenta(c)quinolin-8-yl)ethanone
g-1 cpd
AKOS015969580
SCHEMBL12700948
(+/-)-1-[(3ar*,4s*,9bs*)-4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3h-cyclopenta[c]quinolin-8-yl]- ethanone
925419-53-0
HMS3650I22
sr-01000506928
SR-01000506928-1
unii-y3v5bv7okm
y3v5bv7okm ,
g 1 (anti-tumor agent)
EX-A3642
HY-107216
CS-0027669
HMS3678A07
Q27077759
SR-01000506928-3
HMS3414A07
ethanone, 1-((3ar,4s,9bs)-4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3h-cyclopenta(c)quinolin-8-yl)-, rel-
g 1 (g protein-coupled estrogen receptor agonist)
g 1 (gper agonist)
ethanone, 1-((3as,4r,9br)-4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3h-cyclopenta(c)quinolin-8-yl)-
TFS4QE36ZG ,
unii-tfs4qe36zg

Research Excerpts

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
agonistSubstance which binds to cell receptors normally responding to naturally occurring substances and which produces a response of its own.
[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 (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Estrogen receptorHomo sapiens (human)Ki10.00000.00000.42297.9070AID498758; AID503066
Orexin receptor type 2Rattus norvegicus (Norway rat)Ki0.01100.00010.00550.0110AID769552
G-protein coupled estrogen receptor 1Homo sapiens (human)IC50 (µMol)0.01100.01100.01100.0110AID443558
G-protein coupled estrogen receptor 1Homo sapiens (human)Ki0.00970.00700.00970.0110AID498757; AID503065; AID769552
[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)
estrogen receptor alpha, partialHomo sapiens (human)EC50 (µMol)0.04870.03660.03660.0366AID1223
GPER proteinHomo sapiens (human)EC50 (µMol)0.01110.01110.01110.0111AID1224
Orexin receptor type 2Rattus norvegicus (Norway rat)EC50 (µMol)0.00200.00200.00200.0020AID769553
Estrogen receptor betaHomo sapiens (human)EC50 (µMol)0.18380.00000.47954.8900AID1221
G-protein coupled estrogen receptor 1Homo sapiens (human)EC50 (µMol)0.48470.00200.48471.4500AID1387592; AID503076; AID769553
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (92)

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)
vasodilationG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of protein phosphorylationG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of neurotransmitter secretionG-protein coupled estrogen receptor 1Homo sapiens (human)
negative regulation of leukocyte activationG-protein coupled estrogen receptor 1Homo sapiens (human)
inflammatory responseG-protein coupled estrogen receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayG-protein coupled estrogen receptor 1Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationG-protein coupled estrogen receptor 1Homo sapiens (human)
nervous system developmentG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of cell population proliferationG-protein coupled estrogen receptor 1Homo sapiens (human)
negative regulation of cell population proliferationG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of gene expressionG-protein coupled estrogen receptor 1Homo sapiens (human)
negative regulation of gene expressionG-protein coupled estrogen receptor 1Homo sapiens (human)
negative regulation of cell cycle processG-protein coupled estrogen receptor 1Homo sapiens (human)
neuronal action potentialG-protein coupled estrogen receptor 1Homo sapiens (human)
cell differentiationG-protein coupled estrogen receptor 1Homo sapiens (human)
apoptotic chromosome condensationG-protein coupled estrogen receptor 1Homo sapiens (human)
nuclear fragmentation involved in apoptotic nuclear changeG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of cell migrationG-protein coupled estrogen receptor 1Homo sapiens (human)
intracellular steroid hormone receptor signaling pathwayG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of insulin secretionG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of inositol trisphosphate biosynthetic processG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of apoptotic processG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic processG-protein coupled estrogen receptor 1Homo sapiens (human)
steroid hormone mediated signaling pathwayG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of MAPK cascadeG-protein coupled estrogen receptor 1Homo sapiens (human)
innate immune responseG-protein coupled estrogen receptor 1Homo sapiens (human)
negative regulation of fat cell differentiationG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIG-protein coupled estrogen receptor 1Homo sapiens (human)
negative regulation of inflammatory responseG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of neurogenesisG-protein coupled estrogen receptor 1Homo sapiens (human)
negative regulation of lipid biosynthetic processG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolG-protein coupled estrogen receptor 1Homo sapiens (human)
regulation of cytosolic calcium ion concentrationG-protein coupled estrogen receptor 1Homo sapiens (human)
regulation of cell cycleG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionG-protein coupled estrogen receptor 1Homo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionG-protein coupled estrogen receptor 1Homo sapiens (human)
negative regulation of ERK1 and ERK2 cascadeG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of uterine smooth muscle contractionG-protein coupled estrogen receptor 1Homo sapiens (human)
cellular response to glucose stimulusG-protein coupled estrogen receptor 1Homo sapiens (human)
cellular response to tumor necrosis factorG-protein coupled estrogen receptor 1Homo sapiens (human)
cellular response to peptide hormone stimulusG-protein coupled estrogen receptor 1Homo sapiens (human)
cellular response to mineralocorticoid stimulusG-protein coupled estrogen receptor 1Homo sapiens (human)
cellular response to estradiol stimulusG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of protein localization to plasma membraneG-protein coupled estrogen receptor 1Homo sapiens (human)
negative regulation of vascular associated smooth muscle cell proliferationG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of endothelial cell apoptotic processG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of cardiac vascular smooth muscle cell differentiationG-protein coupled estrogen receptor 1Homo sapiens (human)
positive regulation of extrinsic apoptotic signaling pathwayG-protein coupled estrogen receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (32)

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)
chromatin bindingG-protein coupled estrogen receptor 1Homo sapiens (human)
G protein-coupled receptor activityG-protein coupled estrogen receptor 1Homo sapiens (human)
steroid bindingG-protein coupled estrogen receptor 1Homo sapiens (human)
protein bindingG-protein coupled estrogen receptor 1Homo sapiens (human)
nuclear estrogen receptor activityG-protein coupled estrogen receptor 1Homo sapiens (human)
G protein-coupled estrogen receptor activityG-protein coupled estrogen receptor 1Homo sapiens (human)
steroid hormone bindingG-protein coupled estrogen receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (35)

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)
plasma membraneG-protein coupled estrogen receptor 1Homo sapiens (human)
Golgi membraneG-protein coupled estrogen receptor 1Homo sapiens (human)
nucleusG-protein coupled estrogen receptor 1Homo sapiens (human)
nuclear envelopeG-protein coupled estrogen receptor 1Homo sapiens (human)
nucleoplasmG-protein coupled estrogen receptor 1Homo sapiens (human)
nucleolusG-protein coupled estrogen receptor 1Homo sapiens (human)
cytoplasmG-protein coupled estrogen receptor 1Homo sapiens (human)
early endosomeG-protein coupled estrogen receptor 1Homo sapiens (human)
endoplasmic reticulumG-protein coupled estrogen receptor 1Homo sapiens (human)
endoplasmic reticulum membraneG-protein coupled estrogen receptor 1Homo sapiens (human)
Golgi apparatusG-protein coupled estrogen receptor 1Homo sapiens (human)
trans-Golgi networkG-protein coupled estrogen receptor 1Homo sapiens (human)
cytosolG-protein coupled estrogen receptor 1Homo sapiens (human)
plasma membraneG-protein coupled estrogen receptor 1Homo sapiens (human)
postsynaptic densityG-protein coupled estrogen receptor 1Homo sapiens (human)
axonG-protein coupled estrogen receptor 1Homo sapiens (human)
dendriteG-protein coupled estrogen receptor 1Homo sapiens (human)
cytoplasmic vesicle membraneG-protein coupled estrogen receptor 1Homo sapiens (human)
mitochondrial membraneG-protein coupled estrogen receptor 1Homo sapiens (human)
dendritic spine membraneG-protein coupled estrogen receptor 1Homo sapiens (human)
presynaptic membraneG-protein coupled estrogen receptor 1Homo sapiens (human)
dendritic shaftG-protein coupled estrogen receptor 1Homo sapiens (human)
intracellular membrane-bounded organelleG-protein coupled estrogen receptor 1Homo sapiens (human)
axon terminusG-protein coupled estrogen receptor 1Homo sapiens (human)
dendritic spine headG-protein coupled estrogen receptor 1Homo sapiens (human)
keratin filamentG-protein coupled estrogen receptor 1Homo sapiens (human)
perinuclear region of cytoplasmG-protein coupled estrogen receptor 1Homo sapiens (human)
presynaptic active zoneG-protein coupled estrogen receptor 1Homo sapiens (human)
recycling endosomeG-protein coupled estrogen receptor 1Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseG-protein coupled estrogen receptor 1Homo sapiens (human)
Golgi apparatusG-protein coupled estrogen receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (47)

Assay IDTitleYearJournalArticle
AID446626Antagonist activity at GFP-tagged GPR30 expressed in COS7 cells assessed as inhibition of estradiol-induced PI3K activation at 10 uM by PIP3 localization based PH-RFP reporter gene assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and characterization of iodinated tetrahydroquinolines targeting the G protein-coupled estrogen receptor GPR30.
AID446624Antagonist activity at GFP-tagged ERalpha expressed in COS7 cells assessed as inhibition of estradiol-induced PI3K activation at 10 uM by PIP3 localization based PH-RFP reporter gene assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and characterization of iodinated tetrahydroquinolines targeting the G protein-coupled estrogen receptor GPR30.
AID498757Binding affinity to GPR30 in human Hec50 cells by competitive binding assay2009Nature chemical biology, Jun, Volume: 5, Issue:6
In vivo effects of a GPR30 antagonist.
AID503166Inhibition of chemoattractant-induced cell migration of human SK-BR-3 cells after 48 hrs by transwell migration assay2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID769553Agonist activity at GPR30 (unknown origin) by calcium mobilization assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Contributions of academic laboratories to the discovery and development of chemical biology tools.
AID503072Agonist activity at GFP-tagged ERalpha expressed in COS7 cells assessed as increase in intracellular calcium level at 1 nM by spectrofluorimetry2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID503161Agonist activity at GFP-tagged GPR30 expressed in COS7 cells assessed as PI3K activation at 10 nM by PIP3 nuclear accumulation assay2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID1387595Cytotoxicity against human SKBR3 cells assessed as decrease in cell viability at 1 uM after 72 hrs in presence of GPER agonist E2 by MTS assay2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
A Series of Indole-Thiazole Derivatives Act as GPER Agonists and Inhibit Breast Cancer Cell Growth.
AID1387597Displacement of fluoromone from recombinant human full length untagged estrogen receptor beta expressed in insect cells after 2 hrs by fluorescence polarization assay2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
A Series of Indole-Thiazole Derivatives Act as GPER Agonists and Inhibit Breast Cancer Cell Growth.
AID498758Binding affinity to ERalpha receptor in COS7 cells by competitive binding assay2009Nature chemical biology, Jun, Volume: 5, Issue:6
In vivo effects of a GPR30 antagonist.
AID503159Agonist activity at GFP-tagged ERalpha expressed in COS7 cells assessed as PI3K activation at 10 nM by PIP3 nuclear accumulation assay2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID503164Agonist activity at GPR30 in human SK-BR-3 cells endogenously expressing only GPR30 assessed as PI3K activation at 10 nM by PIP3 nuclear accumulation assay2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID503165Agonist activity at GPR30 in human MCF7 cells endogenously expressing both GPR30 and ER assessed as PI3K activation at 10 nM by PIP3 nuclear accumulation assay2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID503068Displacement of E2-Alexa633 from GFP-tagged ERalpha expressed in COS7 cells at 1 uM by FACS2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID503162Binding affinity to mRFP1-tagged GPR30 expressed in COS7 cells coexpressing GFP-tagged ERalpha assessed as inhibition of E2-Alexa633 binding in nucleus at 1 uM by FACS2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID503069Displacement of E2-Alexa633 from GFP-tagged ERbeta expressed in COS7 cells at 1 uM by FACS2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID443558Binding affinity to GPR302010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and characterization of iodinated tetrahydroquinolines targeting the G protein-coupled estrogen receptor GPR30.
AID1387605Cytotoxicity against human SKBR3 cells assessed as decrease in cell viability at 1 uM after 72 hrs in absence of GPER agonist E2 by MTS assay2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
A Series of Indole-Thiazole Derivatives Act as GPER Agonists and Inhibit Breast Cancer Cell Growth.
AID1387596Displacement of fluoromone from recombinant human full length untagged estrogen receptor alpha expressed in insect cells after 2 hrs by fluorescence polarization assay2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
A Series of Indole-Thiazole Derivatives Act as GPER Agonists and Inhibit Breast Cancer Cell Growth.
AID1387601Agonist activity at GPER (unknown origin) expressed in human HL60 cells assessed as increase in cAMP accumulation at 1 uM after 20 mins by HTRF assay2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
A Series of Indole-Thiazole Derivatives Act as GPER Agonists and Inhibit Breast Cancer Cell Growth.
AID446625Agonist activity at GFP-tagged GPR30 expressed in COS7 cells assessed as PI3K activation at 10 uM by PIP3 localization based PH-RFP reporter gene assay relative to 10 nM estradiol2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and characterization of iodinated tetrahydroquinolines targeting the G protein-coupled estrogen receptor GPR30.
AID1387608Cytotoxicity against human MCF7 cells assessed as decrease in cell viability at 1 uM after 72 hrs in presence of GPER agonist E2 by MTS assay2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
A Series of Indole-Thiazole Derivatives Act as GPER Agonists and Inhibit Breast Cancer Cell Growth.
AID769552Inhibition of estrogen binding to GPR30 (unknown origin)2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Contributions of academic laboratories to the discovery and development of chemical biology tools.
AID503073Agonist activity at GFP-tagged ERbeta expressed in COS7 cells assessed as increase in intracellular calcium level at 1 nM by spectrofluorimetry2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID503065Displacement of E2-Alexa633 from GFP-tagged GPR30 expressed in COS7 cells by FACS2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID446619Displacement of estradiol-Alexa 633 from GFP-tagged ERbeta expressed in COS7 cells at 10 uM2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and characterization of iodinated tetrahydroquinolines targeting the G protein-coupled estrogen receptor GPR30.
AID446623Agonist activity at GFP-tagged ERalpha expressed in COS7 cells assessed as PI3K activation at 10 uM by PIP3 localization based PH-RFP reporter gene assay relative to 10 nM estradiol2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and characterization of iodinated tetrahydroquinolines targeting the G protein-coupled estrogen receptor GPR30.
AID446618Displacement of estradiol-Alexa 633 from GFP-tagged ERalpha expressed in COS7 cells at 10 uM2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and characterization of iodinated tetrahydroquinolines targeting the G protein-coupled estrogen receptor GPR30.
AID503070Agonist activity at GFP-tagged GPR30 expressed in COS7 cells assessed as half life for increase in intracellular calcium level at 1 nM by spectrofluorimetry2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID446621Agonist activity at GPR30 in human SKBr3 cells assessed as stimulation of calcium mobilization at 10 uM relative to 200 nM estradiol2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and characterization of iodinated tetrahydroquinolines targeting the G protein-coupled estrogen receptor GPR30.
AID503076Agonist activity at GFP-tagged GPR30 expressed in COS7 cells assessed as half life for increase in intracellular calcium level by spectrofluorimetry2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID503163Binding affinity to GFP-tagged ERalpha expressed in COS7 cells coexpressing mRFP1-tagged GPR30 assessed as inhibition of E2-Alexa633 binding in nucleus at 1 uM by FACS2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID503167Inhibition of chemoattractant-induced cell migration of human MCF7 cells after 48 hrs by transwell migration assay2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID503160Agonist activity at GFP-tagged ERbeta expressed in COS7 cells assessed as PI3K activation at 10 nM by PIP3 nuclear accumulation assay2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID446622Antagonist activity at GPR30 in human SKBr3 cells assessed as inhibition of estradiol-induced calcium mobilization at 10 uM2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and characterization of iodinated tetrahydroquinolines targeting the G protein-coupled estrogen receptor GPR30.
AID503064Displacement of E2-Alexa633 from GFP-tagged GPR30 expressed in COS7 cells at 10 uM by FACS2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID1387602Agonist activity at GPER (unknown origin) expressed in human HL60 cells assessed as increase in cAMP accumulation at 1 uM incubated for 20 mins followed by GPER antagonist G15 addition measured after 10 mins by HTRF assay2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
A Series of Indole-Thiazole Derivatives Act as GPER Agonists and Inhibit Breast Cancer Cell Growth.
AID498771Effect on uterine weight in ovariectomized C57B16 mouse at 0.1 to 2.4 nM, sc2009Nature chemical biology, Jun, Volume: 5, Issue:6
In vivo effects of a GPR30 antagonist.
AID503066Displacement of E2-Alexa633 from GFP-tagged ERalpha expressed in COS7 cells by FACS2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
AID498764Stimulation of GPR30-mediated epithelial uterine cell proliferation in ovariectomized C57B16 mouse at 0.1 to 2.4 nM, sc relative to control2009Nature chemical biology, Jun, Volume: 5, Issue:6
In vivo effects of a GPR30 antagonist.
AID1387600Agonist activity at GPER (unknown origin) expressed in human HL60 cells assessed as increase in cAMP accumulation at 10 uM after 20 mins by HTRF assay2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
A Series of Indole-Thiazole Derivatives Act as GPER Agonists and Inhibit Breast Cancer Cell Growth.
AID1387594Decrease in cAMP accumulation in human HL60 cells harboring GPER siRNA at 100 nM after 48 hrs by HTRF assay2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
A Series of Indole-Thiazole Derivatives Act as GPER Agonists and Inhibit Breast Cancer Cell Growth.
AID1387606Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability at 1 uM after 72 hrs in presence of GPER agonist E2 by MTS assay2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
A Series of Indole-Thiazole Derivatives Act as GPER Agonists and Inhibit Breast Cancer Cell Growth.
AID1387607Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability at 1 uM after 72 hrs in absence of GPER agonist E2 by MTS assay2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
A Series of Indole-Thiazole Derivatives Act as GPER Agonists and Inhibit Breast Cancer Cell Growth.
AID1387592Agonist activity at GPER (unknown origin) expressed in human HL60 cells assessed as increase in cAMP accumulation in presence of IBMX after 15 mins by HTRF assay2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
A Series of Indole-Thiazole Derivatives Act as GPER Agonists and Inhibit Breast Cancer Cell Growth.
AID446620Displacement of 1-{2-[4-(6-bromobenzo[1,3]dioxol-5- yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]ethyl}- 3-(3-iodo(125)-phenyl)urea from GPR30 in human Hec50 cells2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and characterization of iodinated tetrahydroquinolines targeting the G protein-coupled estrogen receptor GPR30.
AID1345880Human GPER (G protein-coupled estrogen receptor)2006Nature chemical biology, Apr, Volume: 2, Issue:4
Virtual and biomolecular screening converge on a selective agonist for GPR30.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (131)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's13 (9.92)29.6817
2010's106 (80.92)24.3611
2020's12 (9.16)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.26

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 Index10.26 (24.57)
Research Supply Index4.89 (2.92)
Research Growth Index5.15 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.26)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (1.52%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other130 (98.48%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]