Page last updated: 2024-11-12

plomestane

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

Description

plomestane: selective inhibitor of aromatization in human breast tissue; may provide a mechanism for controlling estrogen responsive processes [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9904788
CHEMBL ID2105261
SCHEMBL ID3434
MeSH IDM0102773

Synonyms (24)

Synonym
D03749
plomestane (usan/inn)
77016-85-4
10-propargylestr-4-ene-3,17-dione
10-(2-propynyl)estr-4-ene-3,17-dione
mdl 18,962
estr-4-ene-3,17-dione, 10-(2-propynyl)-
plomestane
plomestane [usan:inn]
unii-fl3vs913tw
fl3vs913tw ,
mdl-18962
CHEMBL2105261
plomestane [inn]
plomestane [usan]
10-(2-propynl)-estr-4-ene-3,17-dione
bdbm50421840
SCHEMBL3434
10-(2-propynyl)-estr-4-ene-3,17-dione
10beta-propargyl-estra-4-ene-3,17-dione
JKPDEYAOCSQBSZ-OEUJLIAZSA-N
Q7205081
(8r,9s,10s,13s,14s)-13-methyl-10-prop-2-ynyl-2,6,7,8,9,11,12,14,15,16-decahydro-1h-cyclopenta[a]phenanthrene-3,17-dione
DTXSID601318490

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" This model of peripheral aromatization was utilized to evaluate in vivo pharmacological parameters of MDL 18,962 (10-(2-propynyl)estr-4-ene-3,17-dione) such as bioavailability of several formulations, time course and dose responses following different routes of drug administration, pharmacokinetics and tissue distribution of [14C]MDL 18,962."( Human trophoblast xenografts in athymic mice: a model for peripheral aromatization.
Johnston, JO; Shumaker, RC; Wright, CL, 1989
)
0.28
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AromataseHomo sapiens (human)IC50 (µMol)0.05620.00001.290410.0000AID53547
AromataseHomo sapiens (human)Ki0.00850.00000.60469.5010AID159833; AID53397; AID53875
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.01520.00010.601710.0000AID53397
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AromataseHomo sapiens (human)Ks0.21300.10500.21400.3240AID159831
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (15)

Processvia Protein(s)Taxonomy
negative regulation of chronic inflammatory responseAromataseHomo sapiens (human)
steroid biosynthetic processAromataseHomo sapiens (human)
estrogen biosynthetic processAromataseHomo sapiens (human)
androgen catabolic processAromataseHomo sapiens (human)
syncytium formationAromataseHomo sapiens (human)
negative regulation of macrophage chemotaxisAromataseHomo sapiens (human)
sterol metabolic processAromataseHomo sapiens (human)
female genitalia developmentAromataseHomo sapiens (human)
mammary gland developmentAromataseHomo sapiens (human)
uterus developmentAromataseHomo sapiens (human)
prostate gland growthAromataseHomo sapiens (human)
testosterone biosynthetic processAromataseHomo sapiens (human)
positive regulation of estradiol secretionAromataseHomo sapiens (human)
female gonad developmentAromataseHomo sapiens (human)
response to estradiolAromataseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
iron ion bindingAromataseHomo sapiens (human)
steroid hydroxylase activityAromataseHomo sapiens (human)
electron transfer activityAromataseHomo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenAromataseHomo sapiens (human)
oxygen bindingAromataseHomo sapiens (human)
heme bindingAromataseHomo sapiens (human)
aromatase activityAromataseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
endoplasmic reticulumAromataseHomo sapiens (human)
endoplasmic reticulum membraneAromataseHomo sapiens (human)
membraneAromataseHomo sapiens (human)
endoplasmic reticulumAromataseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (15)

Assay IDTitleYearJournalArticle
AID159833Binding affinity(KI) for formation of reversible enzyme-ligand complex with human placental aromatase (PL2)1989Journal of medicinal chemistry, Jan, Volume: 32, Issue:1
Interactions of thiol-containing androgens with human placental aromatase.
AID159831Binding affinity constant for formation of reversible enzyme-ligand complex with human placental aromatase (PL1)1989Journal of medicinal chemistry, Jan, Volume: 32, Issue:1
Interactions of thiol-containing androgens with human placental aromatase.
AID232769Selectivity index of Kcat/app Ki(inact)1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
6 beta-Propynyl-substituted steroids: mechanism-based enzyme-activated irreversible inhibitors of aromatase.
AID159829Dithiothreitol (10 nM) reactivation of human placental aromatase following 1.0 uM inactivation for 10 minutes1989Journal of medicinal chemistry, Jan, Volume: 32, Issue:1
Interactions of thiol-containing androgens with human placental aromatase.
AID53397Binding affinity for human placental microsome Cytochrome P450 19A1 by nonlinear regression analysis1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
6 beta-Propynyl-substituted steroids: mechanism-based enzyme-activated irreversible inhibitors of aromatase.
AID54051In vitro inactivation of human placental Cytochrome P450 19A11989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Is there a case for P-450 inhibitors in cancer treatment?
AID53875In vitro inhibition of Cytochrome P450 19A11989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Is there a case for P-450 inhibitors in cancer treatment?
AID17474Kcat calculated from 0.693/T1/21997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
6 beta-Propynyl-substituted steroids: mechanism-based enzyme-activated irreversible inhibitors of aromatase.
AID159828Maximum absorbance for formation of reversible-enzyme-ligand complexes with human placental aromatase (PL1)1989Journal of medicinal chemistry, Jan, Volume: 32, Issue:1
Interactions of thiol-containing androgens with human placental aromatase.
AID53547Inhibition of human placental microsome Cytochrome P450 19A11997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
6 beta-Propynyl-substituted steroids: mechanism-based enzyme-activated irreversible inhibitors of aromatase.
AID159834Ratio of Kcat and KI for human placental microsome aromatase1989Journal of medicinal chemistry, Jan, Volume: 32, Issue:1
Interactions of thiol-containing androgens with human placental aromatase.
AID40036Effective dose for inhibition of extragonadal estrogen production in baboons1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Is there a case for P-450 inhibitors in cancer treatment?
AID19549The T1/2 values were obtained from the time point at which each half-time reached 50% of its value at zero time1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
6 beta-Propynyl-substituted steroids: mechanism-based enzyme-activated irreversible inhibitors of aromatase.
AID159835Catalytic constant (Kcat) for reversible enzyme-ligand complex formation with human placental aromatase (PL2)1989Journal of medicinal chemistry, Jan, Volume: 32, Issue:1
Interactions of thiol-containing androgens with human placental aromatase.
AID15829Compound was tested for inactivation kinetic values1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
6 beta-Propynyl-substituted steroids: mechanism-based enzyme-activated irreversible inhibitors of aromatase.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (28)

TimeframeStudies, This Drug (%)All Drugs %
pre-199015 (53.57)18.7374
1990's13 (46.43)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.93

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 Index10.93 (24.57)
Research Supply Index3.50 (2.92)
Research Growth Index4.43 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.93)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (3.23%)5.53%
Reviews3 (9.68%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other27 (87.10%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]