Page last updated: 2024-12-10

tanaproget

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

Description

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

Cross-References

ID SourceID
PubMed CID4369524
CHEMBL ID539163
SCHEMBL ID62188
MeSH IDM0490350

Synonyms (34)

Synonym
304853-42-7
D06003
tanaproget (usan/inn)
tanaproget
T98 ,
5-(4,4-dimethyl-2-thioxo-1,4-dihydro-2h-3,1-benzoxazin-6-yl)-1-methyl-1h-pyrrole-2-carbonitrile
DB04787
1ZUC
nsp-989
CHEMBL539163
5-(4,4-dimethyl-2-sulfanylidene-1h-3,1-benzoxazin-6-yl)-1-methylpyrrole-2-carbonitrile
w9f9h8gxwr ,
nsp 989
unii-w9f9h8gxwr
tanaproget [usan:inn]
1h-pyrrole-2-carbonitrile, 5-(1,4-dihydro-4,4-dimethyl-2-thioxo-2h-3,1-benzoxazin-6-yl)-1-methyl-
bdbm50375821
tanaproget [usan]
tanaproget [inn]
5-(4,4-dimethyl-2-sulfanylidene-2,4-dihydro-1h-3,1-benzoxazin-6-yl)-1-methyl-1h-pyrrole-2-carbonitrile
gtpl7416
CS-1550
HY-15606
SCHEMBL62188
DTXSID00184556
AKOS030526776
FT-0735521
5-(4,4-dimethyl-2-thioxo-1,4-dihydro-2h-benzo[d][1,3]oxazin-6-yl)-1-methyl-1h-pyrrole-2-carbonitrile
PYVFWTPEBMRKSR-UHFFFAOYSA-N
Q18211583
SB17247
A919251
F84964
MS-24272

Research Excerpts

Overview

Tanaproget is a nonsteroidal progestin agonist with very high PR binding affinity and excellent in vivo potency. It is being investigated for use in contraception.

ExcerptReferenceRelevance
"Tanaproget is a nonsteroidal progestin agonist with very high PR binding affinity and excellent in vivo potency."( Imaging progesterone receptor in breast tumors: synthesis and receptor binding affinity of fluoroalkyl-substituted analogues of tanaproget.
Carlson, KE; Katzenellenbogen, JA; Lee, JH; Mayne, CG; Zhou, HB, 2010
)
1.29
"Tanaproget is a first-in-class nonsteroidal progesterone receptor agonist that is being investigated for use in contraception. "( NMR characterization of an S-linked glucuronide metabolite of the potent, novel, nonsteroidal progesterone agonist tanaproget.
Chandrasekaran, A; Demaio, W; Elmarakby, S; Keating, KA; Mallis, L; McConnell, O; Shen, L; Zhang, Y, 2006
)
1.99
[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)
Chain A, Progesterone receptorHomo sapiens (human)IC50 (µMol)0.00170.00170.00170.0017AID977608
Progesterone receptorHomo sapiens (human)IC50 (µMol)0.00050.00000.580710.0000AID326397
[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)0.00020.00010.40478.2000AID326395
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (18)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (8)

Assay IDTitleYearJournalArticle
AID300889Inhibition of ovulation-induced progesterone levels in po dosed cynamologous monkey2007Bioorganic & medicinal chemistry, Oct-15, Volume: 15, Issue:20
5-(3-Cyclopentyl-2-thioxo-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile: A novel, highly potent, selective, and orally active non-steroidal progesterone receptor agonist.
AID326395Agonist activity at human PR expressed in human T47D cells assessed as stimulation of alkaline phosphatase2008Journal 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).
AID326397Displacement of [3H]R5020 from human PR in human T47D cells by whole cell 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).
AID478059Binding affinity to progesterone receptor relative to R50202010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Imaging progesterone receptor in breast tumors: synthesis and receptor binding affinity of fluoroalkyl-substituted analogues of tanaproget.
AID246369Effective concentration against alkaline phosphatase activity in human T47D breast carcinoma cell line2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading to the potent and selective nonsteroidal progesterone receptor agonist tanaproget.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2005The Journal of biological chemistry, Aug-05, Volume: 280, Issue:31
Molecular and pharmacological properties of a potent and selective novel nonsteroidal progesterone receptor agonist tanaproget.
AID1811Experimentally measured binding affinity data derived from PDB2005The Journal of biological chemistry, Aug-05, Volume: 280, Issue:31
Molecular and pharmacological properties of a potent and selective novel nonsteroidal progesterone receptor agonist tanaproget.
AID1346851Human Progesterone receptor (3C. 3-Ketosteroid receptors)2008Journal 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 (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's8 (72.73)29.6817
2010's3 (27.27)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: 22.35

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 Index22.35 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index4.25 (4.65)
Search Engine Demand Index21.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.35)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (9.09%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (90.91%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]