Page last updated: 2024-11-12

cp 544326

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

Description

CP 544326: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID18376177
CHEMBL ID2107783
SCHEMBL ID3318549
MeSH IDM0569393

Synonyms (48)

Synonym
bdbm50016953
taprenepag
752187-80-7
taprenepag (usan/inn)
D09968
2-(3-((((4-(1h-pyrazol-1-yl)phenyl)methyl)(pyridin-3-ylsulfonyl)amino) methyl)phenoxy)acetic acid
cp 544326
acetic acid, 2-(3-((((4-(1h-pyrazol-1-yl)phenyl)methyl)(3-pyridinylsulfonyl)amino) methyl)phenoxy)-
9cd894kumj ,
cp-544326
unii-9cd894kumj
pf 04217329
taprenepag [usan:inn]
CHEMBL2107783
gtpl5816
2-[3-[[(4-pyrazol-1-ylphenyl)methyl-pyridin-3-ylsulfonylamino]methyl]phenoxy]acetic acid
SCHEMBL3318549
pf04217329
taprenepag [usan]
taprenepag [who-dd]
2-(3-((n-((4-(1h-pyrazol-1-yl)phenyl)methyl)pyridine-3-sulfonamido)methyl)phenoxy)acetic acid
taprenepag [inn]
cp544326
acetic acid, (3-((((4-(1h-pyrazol-1-yl)phenyl)methyl)(3-pyridinylsulfonyl)amino)methyl)phenoxy)-
acetic acid, 2-(3-((((4-(1h-pyrazol-1-yl)phenyl)methyl)(3-pyridinylsulfonyl)amino)methyl)phenoxy)-
2-(3-{[{[4-(1h-pyrazol-1-yl)phenyl]methyl}(pyridin-3-ylsulfonyl)amino]methyl}phenoxy)acetic acid
DTXSID00226187
CS-5590
HY-14899
J-690347
EX-A941
acetic acid, [3-[[[[4-(1h-pyrazol-1-yl)phenyl]methyl](3-pyridinylsulfonyl)amino]methyl]phenoxy]-
mfcd18633300
AKOS030632799
taprenepag(cp-544326)
DB12623
A858259
BCP17228
BCP24232
Q27088938
2-(3-((n-(4-(1h-pyrazol-1-yl)benzyl)pyridine-3-sulfonamido)methyl)phenoxy)acetic acid
2-[3-[[[[4-(1h-pyrazol-1-yl)phenyl]methyl](3-pyridinylsulfonyl)amino]methyl]phenoxy]acetic acid; cp 544326
AS-76944
2-[3-[[(4-pyrazol-1-ylphenyl)methyl-pyridin-3-ylsulfonyl-amino]methyl]phenoxy]ethanoic acid
GNO ,
CFB18780
2-(3-((n-(4-(1h-pyrazol-1-yl)benzyl)pyridine-3-sulfonamido)methyl)phenoxy)aceticacid
AC-36845

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"8 nM) whose corneal permeability and ocular bioavailability were significantly increased when the compound was dosed as the isopropyl ester prodrug, PF-04217329."( Effect of PF-04217329 a prodrug of a selective prostaglandin EP(2) agonist on intraocular pressure in preclinical models of glaucoma.
Almaden, C; Anderson, S; Carreiro, S; Dinh, D; Fortner, J; Gale, D; Gukasyan, H; Krauss, A; Lafontaine, J; Niesman, M; Prasanna, G; Sartnurak, S; Toris, C; Wells, P; Xiang, C; Younis, H, 2011
)
0.37

Dosage Studied

ExcerptRelevanceReference
"8 nM) whose corneal permeability and ocular bioavailability were significantly increased when the compound was dosed as the isopropyl ester prodrug, PF-04217329."( Effect of PF-04217329 a prodrug of a selective prostaglandin EP(2) agonist on intraocular pressure in preclinical models of glaucoma.
Almaden, C; Anderson, S; Carreiro, S; Dinh, D; Fortner, J; Gale, D; Gukasyan, H; Krauss, A; Lafontaine, J; Niesman, M; Prasanna, G; Sartnurak, S; Toris, C; Wells, P; Xiang, C; Younis, H, 2011
)
0.37
"Monkeys were dosed daily for 28 days in 1 eye with taprenepag and in the other with vehicle control."( Investigation of ocular events associated with taprenepag isopropyl, a topical EP2 agonist in development for treatment of glaucoma.
Affolter, T; Eighmy, JJ; Evans, MG; Jessen, BA; Khoh-Reiter, S; Lee, D; Miller, PE; Shiue, MH; Trajkovic, D; Yanochko, GM, 2014
)
0.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Prostaglandin E2 receptor EP1 subtypeHomo sapiens (human)Ki3.20000.00910.66351.5849AID1151360
Prostaglandin E2 receptor EP4 subtypeHomo sapiens (human)Ki3.20000.00010.47443.1623AID1151362
Prostaglandin E2 receptor EP3 subtypeHomo sapiens (human)Ki3.20000.00031.70816.8000AID1151361
Prostaglandin E2 receptor EP2 subtypeHomo sapiens (human)Ki0.01000.00100.54483.0000AID1151359
[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)
Prostaglandin E2 receptor EP2 subtypeHomo sapiens (human)EC50 (µMol)0.00280.00190.96657.8000AID1151368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (31)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
response to lipopolysaccharideProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
inflammatory responseProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
negative regulation of cytokine productionProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
positive regulation of cytokine productionProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
immune responseProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
JNK cascadeProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
response to mechanical stimulusProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
response to nematodeProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
regulation of ossificationProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
response to lipopolysaccharideProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
negative regulation of integrin activationProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
T-helper cell differentiationProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
negative regulation of inflammatory responseProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
positive regulation of inflammatory responseProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
regulation of stress fiber assemblyProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
bone developmentProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
ERK1 and ERK2 cascadeProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
cellular response to mechanical stimulusProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
negative regulation of eosinophil extravasationProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
cellular response to prostaglandin E stimulusProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
inflammatory responseProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
cell deathProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
positive regulation of fever generationProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
intestine smooth muscle contractionProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
inflammatory responseProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
negative regulation of gastric acid secretionProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
response to nematodeProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
response to lipopolysaccharideProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
response to progesteroneProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
regulation of cell population proliferationProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
cellular response to prostaglandin E stimulusProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
inflammatory responseProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
D1 dopamine receptor bindingProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
prostaglandin E receptor activityProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
prostaglandin E receptor activityProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
protein bindingProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
prostaglandin E receptor activityProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
prostaglandin E receptor activityProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
plasma membraneProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
membraneProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
nuclear envelopeProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
membraneProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (12)

Assay IDTitleYearJournalArticle
AID1151362Binding affinity to EP4 receptor (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151373Selectivity ratio of Ki for EP4 receptor (unknown origin) to Ki for EP2 receptor (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151369Agonist activity at prostanoid IP receptor (unknown origin) by functional assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151372Selectivity ratio of Ki for EP3 receptor (unknown origin) to Ki for EP2 receptor (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151359Binding affinity to EP2 receptor (unknown origin) by competitive binding assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151361Binding affinity to EP3 receptor (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151368Agonist activity at EP2 receptor (unknown origin) by functional assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151363Binding affinity to prostanoid IP receptor (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151371Selectivity ratio of Ki for EP1 receptor (unknown origin) to Ki for EP2 receptor (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151360Binding affinity to EP1 receptor (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1346318Rat EP2 receptor (Prostanoid receptors)2011Experimental eye research, Sep, Volume: 93, Issue:3
Effect of PF-04217329 a prodrug of a selective prostaglandin EP(2) agonist on intraocular pressure in preclinical models of glaucoma.
AID1346308Human EP2 receptor (Prostanoid receptors)2011Experimental eye research, Sep, Volume: 93, Issue:3
Effect of PF-04217329 a prodrug of a selective prostaglandin EP(2) agonist on intraocular pressure in preclinical models of glaucoma.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's6 (100.00)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: 12.31

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 Index12.31 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.31)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (33.33%)5.53%
Reviews1 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other3 (50.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]