Page last updated: 2024-11-11

asoprisnil

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

Description

asoprisnil: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9577221
CHEMBL ID267431
SCHEMBL ID58611
MeSH IDM0470817

Synonyms (35)

Synonym
(8s,11r,13s,14s,17s)-11-[4-[(e)-hydroxyiminomethyl]phenyl]-17-methoxy-17-(methoxymethyl)-13-methyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one
j-867
asoprisnil
D02996
asoprisnil (usan/inn)
199396-76-4
4-[(11beta,17beta)-17-methoxy-17-(methoxymethyl)-3-oxoestra-4,9-dien-11-yl]benzaldehyde oxime
CHEMBL267431
j867
bay86-5294
j867 cpd
unii-72w09924wp
asoprisnil [usan:inn:ban]
72w09924wp ,
benzaldehyde, 4-((11beta,17beta)-17-methoxy-17-(methoxymethyl)-3-oxoestra-4,9-dien-11-yl)-, 1-oxime, (c(e))-
11beta-(4-((e)-(hydroxyimino)methyl)phenyl)-17beta-methoxy-17-(methoxymethyl)estra-4,9-dien-3-one
asoprisnil [mi]
benzaldehyde, 4-((11.beta.,17.beta.)-17-methoxy-17-(methoxymethyl)-3-oxoestra-4,9-dien-11-yl)-, 1-oxime, (c(e))-
benzaldehyde, 4-((11.beta.,17.beta.)-17-methoxy-17-(methoxymethyl)-3-oxoestra-4,9-dien-11-yl), 1-oxime, (c(e))
11beta-[4-[(e)-(hydroxyimino)methyl]phenyl]-17beta-methoxy-17-(methoxymethyl)estra-4,9-dien-3-one
asoprisnil [mart.]
asoprisnil [inn]
asoprisnil [who-dd]
asoprisnil [usan]
SCHEMBL58611
4-((8s,11r,13s,14s,17s)-17-methoxy-17-(methoxymethyl)-13-methyl-3-oxo-2,3,6,7,8,11,12,13,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthren-11-yl)benzaldehyde oxime
4-[(11alpha,13alpha,17beta)-17-methoxy-17-(methoxymethyl)-3-oxoestra-4,9-dien-11-yl]benzaldehyde oxime
AKOS032946286
DTXSID40904033
HY-119433
DB06680
benzaldehyde, 4-[(11beta,17beta)-17-methoxy-17-(methoxymethyl)-3-oxoestra-4,9-dien-11-yl]-, 1-oxime, [c(e)]-
CS-0068353
MS-28149
ZHA39676

Research Excerpts

Overview

Asoprisnil is a novel selective progesterone receptor modulator that exhibits partial agonist and antagonist activities in animals and humans. It controls uterine bleeding via an endometrial effect.

ExcerptReferenceRelevance
"Asoprisnil is a novel selective steroid receptor modulator that shows unique pharmacodynamic effects in animal models and humans. "( Asoprisnil (J867): a selective progesterone receptor modulator for gynecological therapy.
Chwalisz, K; DeManno, D; Elger, W; Garg, R; Hess-Stumpp, H; Lee, R; Schneider, B; Schubert, G, 2003
)
3.2
"Asoprisnil is a novel selective progesterone receptor modulator that exhibits partial agonist and antagonist activities in animals and humans. "( Therapeutic potential for the selective progesterone receptor modulator asoprisnil in the treatment of leiomyomata.
Chwalisz, K; DeManno, D; Garg, R; Larsen, L; Mattia-Goldberg, C; Stickler, T, 2004
)
2
"Asoprisnil (J867) is a novel selective progesterone receptor modulator (SPRM) that exhibits partial agonist and antagonist activities and tissue selective effects. "( The effects of 1-month administration of asoprisnil (J867), a selective progesterone receptor modulator, in healthy premenopausal women.
Chwalisz, K; Elger, W; Larsen, L; Mattia-Goldberg, C; Stickler, T, 2005
)
2.04
"Asoprisnil is a selective progesterone receptor modulator with mixed progesterone agonist/antagonist activity which controls uterine bleeding via an endometrial effect. "( The effects of the selective progesterone receptor modulator asoprisnil on the morphology of uterine tissues after 3 months treatment in patients with symptomatic uterine leiomyomata.
Cameron, IT; Chwalisz, K; Critchley, HO; Han, C; Ingamells, S; Osei, J; Williams, AR, 2007
)
2.02

Treatment

Asoprisnil treatment significantly (P < 0.05) increased TRAIL, DR4, and DR5 contents in cultured leiomyoma cells. Treatment decreased the proliferating cell nuclear antigen-positive rate and the number of viable cells.

ExcerptReferenceRelevance
"In asoprisnil-treated endometrium, there is a marked downregulation of stromal PR expression and virtual absence of uNK."( Uterine NK cells regulate endometrial bleeding in women and are suppressed by the progesterone receptor modulator asoprisnil.
Brito-Mutunayagam, SL; Cameron, IT; Chwalisz, K; Craigon, M; Critchley, HO; Forster, T; Ghazal, P; Gibson, DA; Lourenco, P; Male, V; Moffett, A; Wilkens, J; Williams, AR, 2013
)
1.11
"Each asoprisnil treatment was compared with placebo."( Effects of the selective progesterone receptor modulator asoprisnil on uterine artery blood flow, ovarian activity, and clinical symptoms in patients with uterine leiomyomata scheduled for hysterectomy.
Cameron, IT; Chwalisz, K; Critchley, HO; Han, C; Hapangama, D; Ingamells, S; Lawrence, AC; Lumsden, MA; Walker, J; Wilkens, J; Williams, AR, 2008
)
1.05
"Asoprisnil treatment was well tolerated when administered daily for a 12-wk period, and no serious adverse events occurred."( Effects of the selective progesterone receptor modulator asoprisnil on uterine artery blood flow, ovarian activity, and clinical symptoms in patients with uterine leiomyomata scheduled for hysterectomy.
Cameron, IT; Chwalisz, K; Critchley, HO; Han, C; Hapangama, D; Ingamells, S; Lawrence, AC; Lumsden, MA; Walker, J; Wilkens, J; Williams, AR, 2008
)
1.31
"Asoprisnil treatment significantly (P < 0.05) increased TRAIL, DR4, and DR5 contents in cultured leiomyoma cells in a dose-dependent manner with a cleavage of caspase-8, -7, and -3, and decreased X-linked chromosome-linked inhibitor of apoptosis protein contents."( A novel selective progesterone receptor modulator asoprisnil activates tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-mediated signaling pathway in cultured human uterine leiomyoma cells in the absence of comparable effects on myometrial
Chwalisz, K; DeManno, DA; Maruo, T; Ohara, N; Sasaki, H; Wang, J; Xu, Q; Yoshida, S, 2007
)
1.31
"Treatment with asoprisnil decreased the proliferating cell nuclear antigen-positive rate and the number of viable cells and increased the terminal deoxynucleotidyl transferase-mediated 2'-deoxyuridine 5'-triphosphate nick end labeling- positive rate in cultured leiomyoma cells in a dose-dependent manner ( P < .05)."( Comparative effects of SPRM asoprisnil (J867) on proliferation, apoptosis, and the expression of growth factors in cultured uterine leiomyoma cells and normal myometrial cells.
Chen, W; Chwalisz, K; DeManno, DA; Maruo, T; Morikawa, A; Ohara, N; Wang, J, 2007
)
0.97
"Treatment with asoprisnil at concentrations > or =10(-7) M for 48 h significantly (P < 0.05) increased EMMPRIN, MMP-1 and MT1-MMP protein contents, and decreased TIMP-1 (P < 0.05), TIMP-2 (P < 0.01), type I (P < 0.01) and type III (P < 0.05 at 10(-7) M; P < 0.01 at 10(-6) M) collagen protein contents in cultured leiomyoma cells compared with control cultures."( Selective progesterone receptor modulator asoprisnil down-regulates collagen synthesis in cultured human uterine leiomyoma cells through up-regulating extracellular matrix metalloproteinase inducer.
Chwalisz, K; DeManno, DA; Maruo, T; Morikawa, A; Nakabayashi, K; Ohara, N; Xu, Q; Yoshida, S, 2008
)
0.95

Toxicity

ExcerptReferenceRelevance
"Uninterrupted treatment with asoprisnil for 12 months effectively controlled HMB and reduced fibroid and uterine volume with few adverse events."( Safety and efficacy of the selective progesterone receptor modulator asoprisnil for heavy menstrual bleeding with uterine fibroids: pooled analysis of two 12-month, placebo-controlled, randomized trials.
Carr, BR; Chwalisz, K; Diamond, MP; Elger, W; Feldman, RA; Mattia-Goldberg, C; Myers, ER; Schwefel, BM; Stewart, EA; Williams, ARW, 2019
)
1.04

Dosage Studied

ExcerptRelevanceReference
" In low dosage and high dosage asoprisnil groups, the tight junction was longer and more curve than in the vehicle control group; microvilli were uneven and asymmetrically distributed in luminal epithelia; the stromal cells were small and the decidual change was not significant; there were karyopyknosis and karyolysis in stromal cells; there were abnormal thick-wall vessels in the endometrium."( Postcoital administration of asoprisnil inhibited embryo implantation and disturbed ultrastructure of endometrium in implantation window in mice.
Qiu, J; Shen, XL; Su, P; Wu, XL; Yang, YH; Yu, ZH, 2013
)
0.97
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Estrogen receptorHomo sapiens (human)IC50 (µMol)1.95000.00000.723732.7000AID326408; AID719371
Glucocorticoid receptorHomo sapiens (human)IC50 (µMol)0.10250.00000.495310.0000AID326404; AID719373
Progesterone receptorHomo sapiens (human)IC50 (µMol)0.00030.00000.580710.0000AID323989; AID719375; AID719529
Mineralocorticoid receptor Homo sapiens (human)IC50 (µMol)1.60000.00030.748410.0000AID326406; AID719372
Androgen receptorHomo sapiens (human)IC50 (µMol)0.00750.00000.875310.0000AID326402; AID719374
[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)
Progesterone receptorHomo sapiens (human)EC50 (µMol)0.10000.00010.40478.2000AID323987
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (121)

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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (44)

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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (19)

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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (25)

Assay IDTitleYearJournalArticle
AID323987Agonist activity at human PRB expressed in CHO cells2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
11-(pyridinylphenyl)steroids--a new class of mixed-profile progesterone agonists/antagonists.
AID323989Antagonist activity at human PRB expressed in CHO cells assessed as inhibition of Org 2058 induced-transactivation2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
11-(pyridinylphenyl)steroids--a new class of mixed-profile progesterone agonists/antagonists.
AID719377Agonist activity at estrogen receptor by cellular reporter gene assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.
AID326404Antagonist activity at human GR ligand binding domain expressed in african green monkey COS7 cells in presence of Dexamethasone by Gal4 hybrid assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID719375Antagonist activity at progesterone receptor by cellular reporter gene assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.
AID326408Antagonist activity at human ER ligand binding domain expressed in african green monkey COS7 cells in presence of 17-beta-estradiol by Gal4 hybrid assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID326401Agonist activity at human AR ligand binding domain expressed in african green monkey COS7 cells by Gal4 hybrid assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID719371Antagonist activity at estrogen receptor by cellular reporter gene assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.
AID719521Agonist activity at progesterone receptor by cellular reporter gene assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.
AID326407Agonist activity at human ER ligand binding domain expressed in african green monkey COS7 cells by Gal4 hybrid assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID570060Antagonist activity at progesterone receptor in orally dosed ovariectomized Sprague-Dawley rat assessed as reversal of R5020-induced down-regulation of estradiol-induced increase in complement 3 mRNA expression by C3 rat uterine assay2011ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
Novel 3-aryl indoles as progesterone receptor antagonists for uterine fibroids.
AID326405Agonist activity at human MR ligand binding domain receptor expressed in african green monkey COS7 cells by Gal4 hybrid assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID719373Antagonist activity at glucocorticoid receptor by cellular reporter gene assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.
AID719519Agonist activity at glucocorticoid receptor by cellular reporter gene assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.
AID326403Agonist activity at human GR ligand binding domain expressed in african green monkey COS7 cells by Gal4 hybrid assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID719374Antagonist activity at androgen receptor by cellular reporter gene assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.
AID326406Antagonist activity at human MR ligand binding domain expressed in african green monkey COS7 cells in presence of aldosterone by Gal4 hybrid assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
AID719378Agonist activity at mineralocorticoid receptor by cellular reporter gene assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.
AID323990Antagonist activity at human PRB expressed in CHO cells assessed as inhibition of Org 2058 induced-transactivation relative to Org 317102008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
11-(pyridinylphenyl)steroids--a new class of mixed-profile progesterone agonists/antagonists.
AID570063Agonist activity at progesterone receptor in estrogen-primed immature New Zealand White rabbit assessed as stimulation of progesterone-induced endometrial transformation at 30 mg/kg, sc by McPhail assay2011ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
Novel 3-aryl indoles as progesterone receptor antagonists for uterine fibroids.
AID719520Agonist activity at androgen receptor by cellular reporter gene assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.
AID719529Antagonist activity against progesterone receptor in human T47D cells by alkaline phosphatase assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.
AID570061Antagonist activity at progesterone receptor in estrogen-primed immature New Zealand White rabbit assessed as inhibition of progesterone-induced endometrial transformation at 1 mg/kg, sc by McPhail assay2011ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
Novel 3-aryl indoles as progesterone receptor antagonists for uterine fibroids.
AID719372Antagonist activity at mineralocorticoid receptor by cellular reporter gene assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.
AID326402Antagonist activity at human AR ligand binding domain expressed in african green monkey COS7 cells in presence of 5-alpha-dihydrotestosterone by Gal4 hybrid assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (44)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's25 (56.82)29.6817
2010's18 (40.91)24.3611
2020's1 (2.27)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 34.03

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index34.03 (24.57)
Research Supply Index4.04 (2.92)
Research Growth Index4.41 (4.65)
Search Engine Demand Index43.69 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (34.03)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials8 (16.67%)5.53%
Reviews18 (37.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other22 (45.83%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]