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cp 544326

Description

CP 544326: structure in first source [MeSH]

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

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Prostaglandin E2 receptor EP1 subtypeHomo sapiens (human)Ki3.2000AID1151360
Prostaglandin E2 receptor EP4 subtypeHomo sapiens (human)Ki3.2000AID1151362
Prostaglandin E2 receptor EP3 subtypeHomo sapiens (human)Ki3.2000AID1151361
Prostaglandin E2 receptor EP2 subtypeHomo sapiens (human)Ki0.0100AID1151359

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Prostaglandin E2 receptor EP2 subtypeHomo sapiens (human)EC500.0028AID1151368

Bioassays (12)

Assay IDTitleYearJournalArticle
AID1151362Binding affinity to EP4 receptor (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
ISSN: 1520-4804
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
ISSN: 1520-4804
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
ISSN: 1520-4804
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
ISSN: 1520-4804
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
ISSN: 1520-4804
Prostanoid receptor EP2 as a therapeutic target.
AID1151361Binding affinity to EP3 receptor (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
ISSN: 1520-4804
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
ISSN: 1520-4804
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
ISSN: 1520-4804
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
ISSN: 1520-4804
Prostanoid receptor EP2 as a therapeutic target.
AID1151360Binding affinity to EP1 receptor (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
ISSN: 1520-4804
Prostanoid receptor EP2 as a therapeutic target.
AID1346318Rat EP2 receptor (Prostanoid receptors)2011Experimental eye research, Sep, Volume: 93, Issue:3
ISSN: 1096-0007
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
ISSN: 1096-0007
Effect of PF-04217329 a prodrug of a selective prostaglandin EP(2) agonist on intraocular pressure in preclinical models of glaucoma.

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

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%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
ah 6809xanthones2014201410.0low000010
2-[[2-furanyl(oxo)methyl]amino]-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylic acid ethyl esterorganosulfur heterocyclic compound2014201410.0high000010
dinoprostoneprostaglandins Ehuman metabolite;
mouse metabolite;
oxytocic
2014201410.0low000010
butaprost2014201410.0high000010
tg4-1552014201410.0medium000010
cp533536monocarboxylic acid2014201410.0medium000010
pf-044189482014201410.0medium000010
tg6-10-12014201410.0medium000010
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
phenyl acetatebenzenes;
phenyl acetates
2011201910.4high200050
dinoprostoneprostaglandins Ehuman metabolite;
mouse metabolite;
oxytocic
201920195.0low000010
latanoprostisopropyl ester;
prostaglandins Falpha;
triol
antiglaucoma drug;
antihypertensive agent;
EC 4.2.1.1 (carbonic anhydrase) inhibitor;
prodrug
2011201312.0medium200020
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Apoplexy02014201410.0low000010
Chronic Primary Open Angle Glaucoma02011201312.3medium200030
Corneal Diseases02013201311.0low100010
Degenerative Diseases, Central Nervous System02014201410.0low000010
Disease Models, Animal02011201113.0low000010
Eye Diseases02014201410.0low000010
Eye Disorders02014201410.0low000010
Glaucoma02011201411.5low000020
Glaucoma, Open-Angle02011201312.3medium200030
Glaucoma, Suspect02011201312.0low200020
Intraocular Pressure02011201113.0low100020
Neurodegenerative Diseases02014201410.0low000010
Ocular Hypertension02011201312.0low200020
Stroke02014201410.0low000010

Bioavailability (1)

ArticleYear
Effect of PF-04217329 a prodrug of a selective prostaglandin EP(2) agonist on intraocular pressure in preclinical models of glaucoma.
Experimental eye research, , Volume: 93, Issue:3
2011

Dosage (3)

ArticleYear
Investigation of ocular events associated with taprenepag isopropyl, a topical EP2 agonist in development for treatment of glaucoma.
Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics, , Volume: 30, Issue:5
2014
A phase 2, randomized, dose-response trial of taprenepag isopropyl (PF-04217329) versus latanoprost 0.005% in open-angle glaucoma and ocular hypertension.
Current eye research, , Volume: 36, Issue:9
2011
Effect of PF-04217329 a prodrug of a selective prostaglandin EP(2) agonist on intraocular pressure in preclinical models of glaucoma.
Experimental eye research, , Volume: 93, Issue:3
2011