Page last updated: 2024-11-12

lgd 2226

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Cross-References

ID SourceID
PubMed CID11560224
CHEMBL ID436784
SCHEMBL ID1771552
MeSH IDM0504310

Synonyms (25)

Synonym
6-[bis(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)quinolin-2(1h)-one
lgd ,
bdbm18524
6-[bis(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one
lgd2226
chembl436784 ,
DB08089
lgd-2226
6-(bis-(2,2,2-trifluoroethyl)amino)-4-trifluoromethyl-1h-quinolin-2-one
6-[bis(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1h-quinolin-2-one
328947-93-9
unii-ri376rm5mt
ri376rm5mt ,
2HVC
SCHEMBL1771552
DTXSID10186546
6-[bis(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-2(1h)-quinolinone, analytical standard
ulbpqwigzugphu-uhfffaoysa-n
'1,2-dihydro-6-n,n-bis(2,2,2-trifluoroethyl)amino-4-trifluoromethyl-2-quinolinone'
HY-105318
Q6458310
CS-0025720
6-(bis(2,2,2-trifluoroethyl)amino)-4-(trifluoromethyl)quinolin-2(1h)-one
A937582
AKOS040741949
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (8)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Estrogen receptorHomo sapiens (human)Ki1.00000.00000.42297.9070AID272954
Glucocorticoid receptorHomo sapiens (human)Ki1.00000.00010.38637.0010AID272952
Progesterone receptorHomo sapiens (human)Ki1.00000.00030.03160.3997AID272951
Mineralocorticoid receptor Homo sapiens (human)Ki1.00000.00030.17380.8510AID272953
Androgen receptorHomo sapiens (human)IC50 (µMol)10.00000.00000.875310.0000AID272948; AID293943; AID298547
Androgen receptorHomo sapiens (human)Ki0.00260.00020.42407.2000AID1797738; AID1872310; AID1885021; AID272949; AID290231; AID293945; AID298549; AID375617
Cannabinoid receptor 2Mus musculus (house mouse)Ki0.00150.00020.07970.7943AID272949
Muscarinic acetylcholine receptorCavia porcellus (domestic guinea pig)Ki0.00150.00010.61203.8019AID293945
ALK tyrosine kinase receptorHomo sapiens (human)Ki0.00460.00010.20143.7000AID1797738
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Androgen receptorHomo sapiens (human)EC50 (µMol)0.00020.00000.20794.3000AID1872308; AID1885023; AID272946; AID290227; AID293941; AID298545
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (139)

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 IIGlucocorticoid receptorHomo sapiens (human)
regulation of gluconeogenesisGlucocorticoid receptorHomo sapiens (human)
chromatin organizationGlucocorticoid receptorHomo sapiens (human)
regulation of DNA-templated transcriptionGlucocorticoid receptorHomo sapiens (human)
apoptotic processGlucocorticoid receptorHomo sapiens (human)
chromosome segregationGlucocorticoid receptorHomo sapiens (human)
signal transductionGlucocorticoid receptorHomo sapiens (human)
glucocorticoid metabolic processGlucocorticoid receptorHomo sapiens (human)
gene expressionGlucocorticoid receptorHomo sapiens (human)
microglia differentiationGlucocorticoid receptorHomo sapiens (human)
adrenal gland developmentGlucocorticoid receptorHomo sapiens (human)
regulation of glucocorticoid biosynthetic processGlucocorticoid receptorHomo sapiens (human)
synaptic transmission, glutamatergicGlucocorticoid receptorHomo sapiens (human)
maternal behaviorGlucocorticoid receptorHomo sapiens (human)
intracellular glucocorticoid receptor signaling pathwayGlucocorticoid receptorHomo sapiens (human)
glucocorticoid mediated signaling pathwayGlucocorticoid receptorHomo sapiens (human)
positive regulation of neuron apoptotic processGlucocorticoid receptorHomo sapiens (human)
negative regulation of DNA-templated transcriptionGlucocorticoid receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIGlucocorticoid receptorHomo sapiens (human)
astrocyte differentiationGlucocorticoid receptorHomo sapiens (human)
cell divisionGlucocorticoid receptorHomo sapiens (human)
mammary gland duct morphogenesisGlucocorticoid receptorHomo sapiens (human)
motor behaviorGlucocorticoid receptorHomo sapiens (human)
cellular response to steroid hormone stimulusGlucocorticoid receptorHomo sapiens (human)
cellular response to glucocorticoid stimulusGlucocorticoid receptorHomo sapiens (human)
cellular response to dexamethasone stimulusGlucocorticoid receptorHomo sapiens (human)
cellular response to transforming growth factor beta stimulusGlucocorticoid receptorHomo sapiens (human)
neuroinflammatory responseGlucocorticoid receptorHomo sapiens (human)
positive regulation of miRNA transcriptionGlucocorticoid receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayGlucocorticoid receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIGlucocorticoid receptorHomo sapiens (human)
ovulation from ovarian follicleProgesterone receptorHomo sapiens (human)
glandular epithelial cell maturationProgesterone receptorHomo sapiens (human)
regulation of DNA-templated transcriptionProgesterone receptorHomo sapiens (human)
signal transductionProgesterone receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayProgesterone receptorHomo sapiens (human)
cell-cell signalingProgesterone receptorHomo sapiens (human)
positive regulation of gene expressionProgesterone receptorHomo sapiens (human)
negative regulation of gene expressionProgesterone receptorHomo sapiens (human)
paracrine signalingProgesterone receptorHomo sapiens (human)
negative regulation of phosphorylationProgesterone receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIProgesterone receptorHomo sapiens (human)
lung alveolus developmentProgesterone receptorHomo sapiens (human)
regulation of epithelial cell proliferationProgesterone receptorHomo sapiens (human)
progesterone receptor signaling pathwayProgesterone receptorHomo sapiens (human)
maintenance of protein location in nucleusProgesterone receptorHomo sapiens (human)
tertiary branching involved in mammary gland duct morphogenesisProgesterone receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIProgesterone receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayProgesterone receptorHomo sapiens (human)
signal transductionMineralocorticoid receptor Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionMineralocorticoid receptor Homo sapiens (human)
regulation of transcription by RNA polymerase IIMineralocorticoid receptor Homo sapiens (human)
intracellular steroid hormone receptor signaling pathwayMineralocorticoid receptor Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIAndrogen receptorHomo sapiens (human)
MAPK cascadeAndrogen receptorHomo sapiens (human)
in utero embryonic developmentAndrogen receptorHomo sapiens (human)
regulation of systemic arterial blood pressureAndrogen receptorHomo sapiens (human)
epithelial cell morphogenesisAndrogen receptorHomo sapiens (human)
transcription by RNA polymerase IIAndrogen receptorHomo sapiens (human)
signal transductionAndrogen receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAndrogen receptorHomo sapiens (human)
cell-cell signalingAndrogen receptorHomo sapiens (human)
spermatogenesisAndrogen receptorHomo sapiens (human)
single fertilizationAndrogen receptorHomo sapiens (human)
positive regulation of cell population proliferationAndrogen receptorHomo sapiens (human)
negative regulation of cell population proliferationAndrogen receptorHomo sapiens (human)
positive regulation of gene expressionAndrogen receptorHomo sapiens (human)
male somatic sex determinationAndrogen receptorHomo sapiens (human)
intracellular estrogen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
androgen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
intracellular receptor signaling pathwayAndrogen receptorHomo sapiens (human)
positive regulation of intracellular estrogen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
Leydig cell differentiationAndrogen receptorHomo sapiens (human)
multicellular organism growthAndrogen receptorHomo sapiens (human)
positive regulation of phosphorylationAndrogen receptorHomo sapiens (human)
positive regulation of MAPK cascadeAndrogen receptorHomo sapiens (human)
positive regulation of insulin-like growth factor receptor signaling pathwayAndrogen receptorHomo sapiens (human)
positive regulation of cell differentiationAndrogen receptorHomo sapiens (human)
negative regulation of integrin biosynthetic processAndrogen receptorHomo sapiens (human)
positive regulation of integrin biosynthetic processAndrogen receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionAndrogen receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIAndrogen receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIIAndrogen receptorHomo sapiens (human)
insulin-like growth factor receptor signaling pathwayAndrogen receptorHomo sapiens (human)
regulation of developmental growthAndrogen receptorHomo sapiens (human)
animal organ formationAndrogen receptorHomo sapiens (human)
male genitalia morphogenesisAndrogen receptorHomo sapiens (human)
epithelial cell proliferationAndrogen receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationAndrogen receptorHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityAndrogen receptorHomo sapiens (human)
activation of prostate induction by androgen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
morphogenesis of an epithelial foldAndrogen receptorHomo sapiens (human)
lateral sprouting involved in mammary gland duct morphogenesisAndrogen receptorHomo sapiens (human)
prostate gland growthAndrogen receptorHomo sapiens (human)
prostate gland epithelium morphogenesisAndrogen receptorHomo sapiens (human)
epithelial cell differentiation involved in prostate gland developmentAndrogen receptorHomo sapiens (human)
tertiary branching involved in mammary gland duct morphogenesisAndrogen receptorHomo sapiens (human)
mammary gland alveolus developmentAndrogen receptorHomo sapiens (human)
positive regulation of epithelial cell proliferation involved in prostate gland developmentAndrogen receptorHomo sapiens (human)
cellular response to steroid hormone stimulusAndrogen receptorHomo sapiens (human)
cellular response to estrogen stimulusAndrogen receptorHomo sapiens (human)
cellular response to testosterone stimulusAndrogen receptorHomo sapiens (human)
seminiferous tubule developmentAndrogen receptorHomo sapiens (human)
non-membrane-bounded organelle assemblyAndrogen receptorHomo sapiens (human)
positive regulation of miRNA transcriptionAndrogen receptorHomo sapiens (human)
regulation of protein localization to plasma membraneAndrogen receptorHomo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathwayAndrogen receptorHomo sapiens (human)
male gonad developmentAndrogen receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayAndrogen receptorHomo sapiens (human)
protein autophosphorylationALK tyrosine kinase receptorHomo sapiens (human)
signal transductionALK tyrosine kinase receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayALK tyrosine kinase receptorHomo sapiens (human)
phosphorylationALK tyrosine kinase receptorHomo sapiens (human)
hippocampus developmentALK tyrosine kinase receptorHomo sapiens (human)
adult behaviorALK tyrosine kinase receptorHomo sapiens (human)
swimming behaviorALK tyrosine kinase receptorHomo sapiens (human)
peptidyl-tyrosine autophosphorylationALK tyrosine kinase receptorHomo sapiens (human)
regulation of apoptotic processALK tyrosine kinase receptorHomo sapiens (human)
protein autophosphorylationALK tyrosine kinase receptorHomo sapiens (human)
neuron developmentALK tyrosine kinase receptorHomo sapiens (human)
negative regulation of lipid catabolic processALK tyrosine kinase receptorHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityALK tyrosine kinase receptorHomo sapiens (human)
regulation of dopamine receptor signaling pathwayALK tyrosine kinase receptorHomo sapiens (human)
response to environmental enrichmentALK tyrosine kinase receptorHomo sapiens (human)
energy homeostasisALK tyrosine kinase receptorHomo sapiens (human)
positive regulation of dendrite developmentALK tyrosine kinase receptorHomo sapiens (human)
regulation of neuron differentiationALK tyrosine kinase receptorHomo sapiens (human)
regulation of cell population proliferationALK tyrosine kinase receptorHomo sapiens (human)
multicellular organism developmentALK tyrosine kinase receptorHomo sapiens (human)
positive regulation of kinase activityALK tyrosine kinase receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (49)

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 transcription regulatory region sequence-specific DNA bindingGlucocorticoid receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingGlucocorticoid receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificGlucocorticoid receptorHomo sapiens (human)
core promoter sequence-specific DNA bindingGlucocorticoid receptorHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificGlucocorticoid receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificGlucocorticoid receptorHomo sapiens (human)
DNA-binding transcription factor activityGlucocorticoid receptorHomo sapiens (human)
RNA bindingGlucocorticoid receptorHomo sapiens (human)
nuclear receptor activityGlucocorticoid receptorHomo sapiens (human)
nuclear glucocorticoid receptor activityGlucocorticoid receptorHomo sapiens (human)
steroid bindingGlucocorticoid receptorHomo sapiens (human)
protein bindingGlucocorticoid receptorHomo sapiens (human)
zinc ion bindingGlucocorticoid receptorHomo sapiens (human)
TBP-class protein bindingGlucocorticoid receptorHomo sapiens (human)
protein kinase bindingGlucocorticoid receptorHomo sapiens (human)
identical protein bindingGlucocorticoid receptorHomo sapiens (human)
Hsp90 protein bindingGlucocorticoid receptorHomo sapiens (human)
steroid hormone bindingGlucocorticoid receptorHomo sapiens (human)
sequence-specific double-stranded DNA bindingGlucocorticoid receptorHomo sapiens (human)
estrogen response element bindingGlucocorticoid receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingProgesterone receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificProgesterone receptorHomo sapiens (human)
transcription coactivator bindingProgesterone receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificProgesterone receptorHomo sapiens (human)
DNA bindingProgesterone receptorHomo sapiens (human)
nuclear steroid receptor activityProgesterone receptorHomo sapiens (human)
G protein-coupled receptor activityProgesterone receptorHomo sapiens (human)
steroid bindingProgesterone receptorHomo sapiens (human)
protein bindingProgesterone receptorHomo sapiens (human)
zinc ion bindingProgesterone receptorHomo sapiens (human)
enzyme bindingProgesterone receptorHomo sapiens (human)
identical protein bindingProgesterone receptorHomo sapiens (human)
ATPase bindingProgesterone receptorHomo sapiens (human)
estrogen response element bindingProgesterone receptorHomo sapiens (human)
nuclear receptor activityProgesterone receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificMineralocorticoid receptor Homo sapiens (human)
DNA-binding transcription factor activityMineralocorticoid receptor Homo sapiens (human)
nuclear steroid receptor activityMineralocorticoid receptor Homo sapiens (human)
steroid bindingMineralocorticoid receptor Homo sapiens (human)
protein bindingMineralocorticoid receptor Homo sapiens (human)
zinc ion bindingMineralocorticoid receptor Homo sapiens (human)
TBP-class protein bindingMineralocorticoid receptor Homo sapiens (human)
sequence-specific double-stranded DNA bindingMineralocorticoid receptor Homo sapiens (human)
nuclear receptor activityMineralocorticoid receptor Homo sapiens (human)
estrogen response element bindingMineralocorticoid receptor Homo sapiens (human)
transcription cis-regulatory region bindingAndrogen receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingAndrogen receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificAndrogen receptorHomo sapiens (human)
RNA polymerase II general transcription initiation factor bindingAndrogen receptorHomo sapiens (human)
transcription coactivator bindingAndrogen receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificAndrogen receptorHomo sapiens (human)
chromatin bindingAndrogen receptorHomo sapiens (human)
DNA-binding transcription factor activityAndrogen receptorHomo sapiens (human)
nuclear receptor activityAndrogen receptorHomo sapiens (human)
G protein-coupled receptor activityAndrogen receptorHomo sapiens (human)
signaling receptor bindingAndrogen receptorHomo sapiens (human)
steroid bindingAndrogen receptorHomo sapiens (human)
androgen bindingAndrogen receptorHomo sapiens (human)
protein bindingAndrogen receptorHomo sapiens (human)
beta-catenin bindingAndrogen receptorHomo sapiens (human)
zinc ion bindingAndrogen receptorHomo sapiens (human)
enzyme bindingAndrogen receptorHomo sapiens (human)
ATPase bindingAndrogen receptorHomo sapiens (human)
molecular adaptor activityAndrogen receptorHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingAndrogen receptorHomo sapiens (human)
POU domain bindingAndrogen receptorHomo sapiens (human)
molecular condensate scaffold activityAndrogen receptorHomo sapiens (human)
estrogen response element bindingAndrogen receptorHomo sapiens (human)
protein tyrosine kinase activityALK tyrosine kinase receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityALK tyrosine kinase receptorHomo sapiens (human)
protein bindingALK tyrosine kinase receptorHomo sapiens (human)
ATP bindingALK tyrosine kinase receptorHomo sapiens (human)
heparin bindingALK tyrosine kinase receptorHomo sapiens (human)
receptor signaling protein tyrosine kinase activator activityALK tyrosine kinase receptorHomo sapiens (human)
identical protein bindingALK tyrosine kinase receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (20)

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)
nucleusGlucocorticoid receptorHomo sapiens (human)
nucleusGlucocorticoid receptorHomo sapiens (human)
nucleoplasmGlucocorticoid receptorHomo sapiens (human)
cytoplasmGlucocorticoid receptorHomo sapiens (human)
mitochondrial matrixGlucocorticoid receptorHomo sapiens (human)
centrosomeGlucocorticoid receptorHomo sapiens (human)
spindleGlucocorticoid receptorHomo sapiens (human)
cytosolGlucocorticoid receptorHomo sapiens (human)
membraneGlucocorticoid receptorHomo sapiens (human)
nuclear speckGlucocorticoid receptorHomo sapiens (human)
synapseGlucocorticoid receptorHomo sapiens (human)
chromatinGlucocorticoid receptorHomo sapiens (human)
protein-containing complexGlucocorticoid receptorHomo sapiens (human)
plasma membraneProgesterone receptorHomo sapiens (human)
nucleoplasmProgesterone receptorHomo sapiens (human)
mitochondrial outer membraneProgesterone receptorHomo sapiens (human)
cytosolProgesterone receptorHomo sapiens (human)
chromatinProgesterone receptorHomo sapiens (human)
nucleusProgesterone receptorHomo sapiens (human)
nucleoplasmMineralocorticoid receptor Homo sapiens (human)
endoplasmic reticulum membraneMineralocorticoid receptor Homo sapiens (human)
cytosolMineralocorticoid receptor Homo sapiens (human)
chromatinMineralocorticoid receptor Homo sapiens (human)
receptor complexMineralocorticoid receptor Homo sapiens (human)
nucleusMineralocorticoid receptor Homo sapiens (human)
plasma membraneAndrogen receptorHomo sapiens (human)
nucleusAndrogen receptorHomo sapiens (human)
nucleoplasmAndrogen receptorHomo sapiens (human)
cytoplasmAndrogen receptorHomo sapiens (human)
cytosolAndrogen receptorHomo sapiens (human)
nuclear speckAndrogen receptorHomo sapiens (human)
chromatinAndrogen receptorHomo sapiens (human)
protein-containing complexAndrogen receptorHomo sapiens (human)
nucleusAndrogen receptorHomo sapiens (human)
plasma membraneALK tyrosine kinase receptorHomo sapiens (human)
plasma membraneALK tyrosine kinase receptorHomo sapiens (human)
extracellular exosomeALK tyrosine kinase receptorHomo sapiens (human)
protein-containing complexALK tyrosine kinase receptorHomo sapiens (human)
receptor complexALK tyrosine kinase receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (47)

Assay IDTitleYearJournalArticle
AID272963Anabolic activity in orchidectomized rat at 3.0 mg/kg, po measured as increase in levator ani muscle weight to eugonadal level2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID1872308Modulation of Androgen receptor (unknown origin)2022European journal of medicinal chemistry, Feb-15, Volume: 230Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021).
AID290227Agonist activity at human androgen receptor expressed in CV1 cells2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.
AID375617Agonist activity at androgen receptor2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit.
AID272962Antagonist activity against human ERalpha in CV1 cells measured as inhibition of DHT-stimulated luciferase reporter gene activity upto 10 uM by cotransfection assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID298545Agonist activity at human androgen receptor by luciferase reporter gene assay2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.
AID1872310Binding affinity to Androgen receptor (unknown origin) assessed as inhibition constant2022European journal of medicinal chemistry, Feb-15, Volume: 230Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021).
AID272967Anabolic activity in orchidectomized rat measured as increase in levator ani muscle weight relative to intact rat2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID293943Antagonist activity at human AR2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones.
AID272946Agonist activity at human androgen receptor in CV1 cells measured as stimulation of luciferase reporter gene activity by cotransfection assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID375642Myotropic activity in rat assessed as ventral prostate weight at 100 mg/kg by Hershberger assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit.
AID298558Bioavailability in Sprague-Dawley rat at 10 mg/kg, po2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.
AID375644Suppression of hyphalamic-pituitary-gonadal axis in rat at 3 mg/kg2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit.
AID272948Antagonist activity against human androgen receptor in CV1 cells measured as inhibition of DHT-stimulated luciferase reporter gene activity by cotransfection assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID272953Binding affinity to mineralocorticoid receptor2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID298549Binding affinity to human AR2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.
AID290231Binding affinity to human androgen receptor expressed in CV1 cells2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.
AID272961Agonist activity at human ERalpha in CV1 cells measured as stimulation of luciferase reporter gene activity upto 10 uM by cotransfection assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID272947Agonist activity at human androgen receptor in CV1 cells measured as stimulation of luciferase reporter gene activity with relative to DHT by cotransfection assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID298547Antagonist activity at human androgen receptor by luciferase reporter gene assay2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.
AID272956Antagonist activity against human progesterone receptor in CV1 cells measured as inhibition of DHT-stimulated luciferase reporter gene activity upto 10 uM by cotransfection assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID298546Agonist efficacy at human androgen receptor by luciferase reporter gene assay relative to DHT2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.
AID272951Binding affinity to progesterone receptor2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID293941Agonist activity at human AR2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones.
AID290228Agonist activity at human androgen receptor expressed in CV1 cells relative to DHT2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.
AID1885023Agonist activity at human Androgen receptor2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Therapeutic Strategies to Target the Androgen Receptor.
AID272958Antagonist activity against human glucocorticoid receptor in CV1 cells measured as inhibition of DHT-stimulated luciferase reporter gene activity upto 10 uM by cotransfection assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID375626Myotropic activity in rat assessed as levator ani muscle weight by Hershberger assay relative to intact tissue2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit.
AID272950Antagonist activity against human androgen receptor in CV1 cells measured as percent of maximal inhibition of DHT-stimulated luciferase reporter gene activity by cotransfection assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID293942Agonist activity at human AR relative to DHT2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones.
AID272966Androgenic activity in orchidectomized rat at 100 mg/kg, po measured as increase in ventral prostate weight to intact level2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID298548Antagonist efficacy at human androgen receptor assessed as inhibition of DHT activity by luciferase reporter gene assay2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.
AID272952Binding affinity to glucocorticoid receptor2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID272954Binding affinity to estrogen receptor2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID272955Agonist activity at human progesterone receptor in CV1 cells measured as stimulation of luciferase reporter gene activity upto 10 uM by cotransfection assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID1885021Binding affinity to human Androgen receptor2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Therapeutic Strategies to Target the Androgen Receptor.
AID272957Agonist activity at human glucocorticoid receptor in CV1 cells measured as stimulation of luciferase reporter gene activity upto 10 uM by cotransfection assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID298557AUC (0 to infinity) in Sprague-Dawley rat at 10 mg/kg, po2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.
AID272949Displacement of [3H]DHT from human androgen receptor expressed in MDA-MB-453 cells by whole cell receptor binding assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID272959Agonist activity at human mineralocorticoid receptor in CV1 cells measured as stimulation of luciferase reporter gene activity upto 10 uM by cotransfection assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID298554Half life in Sprague-Dawley rat at 2.5 mg/kg, iv2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.
AID1885024Agonist activity at human Androgen receptor relative to control2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Therapeutic Strategies to Target the Androgen Receptor.
AID293944Antagonist activity at human AR assessed as inhibition of DHT-induced response2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones.
AID272960Antagonist activity against human mineralocorticoid receptor in CV1 cells measured as inhibition of DHT-stimulated luciferase reporter gene activity upto 10 uM by cotransfection assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID293945Binding affinity to human AR2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
AID1797738AR Transcriptional Activation Assay and MDA Whole-Cell Binding Assay from Article 10.1021/jm070231h: \\Substituted 6-(1-Pyrrolidine)quinolin-2(1H)-ones as Novel Selective Androgen Receptor Modulators.\\2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (71.43)29.6817
2010's0 (0.00)24.3611
2020's2 (28.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (42.86%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (57.14%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]