Page last updated: 2024-11-12

ema401

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

Cross-References

ID SourceID
PubMed CID9937291
CHEMBL ID34124
SCHEMBL ID421411
MeSH IDM000602433

Synonyms (40)

Synonym
(s)-5-benzyloxy-2-diphenylacetyl-6-methoxy-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid
bdbm50049182
ema-401
ema401
pd-126055
CHEMBL34124 ,
olodanrigan
SCHEMBL421411
[s]-enantiomer of ema400
gtpl8374
[s]-enantiomer of pd-126,055
(3s)-2-(2,2-diphenylacetyl)-6-methoxy-5-phenylmethoxy-3,4-dihydro-1h-isoquinoline-3-carboxylic acid
1316755-16-4
AKOS026676520
1316755-17-5
P0FN522VTO ,
3-isoquinolinecarboxylic acid, 2-(2,2-diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-, (3s)-
olodanrigan [who-dd]
olodanrigan [inn]
unii-p0fn522vto
CS-5781
HY-13106
P16290
(s)-5-(benzyloxy)-2-(2,2-diphenylacetyl)-6-methoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
pd-126055 free acid
olodanrigan,ema 401,ema-401,ema401,1418274-28-8
OLODANRIGAN(EMA401) ,
AS-53290
olodanrigan; pd-126055
mfcd28502251
ema401; olodanrigan
EX-A2623
ema-401; ema401; ema 401; pd-126055; pd 126055;pd 126055
BCP23998
Q18388936
(3s)-5-(benzyloxy)-2-(diphenylacetyl)-6-methoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
olodanrigan (ema401)
(s)-5-(benzyloxy)-2-(2,2-diphenylacetyl)-6-methoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylicacid
DTXSID101031601
AC-35554

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" The primary efficacy endpoint was change in mean pain intensity between baseline and the last week of dosing (days 22-28), measured on an 11-point numerical rating scale."( EMA401, an orally administered highly selective angiotensin II type 2 receptor antagonist, as a novel treatment for postherpetic neuralgia: a randomised, double-blind, placebo-controlled phase 2 clinical trial.
Anand, P; Bountra, C; Cutter, G; Desem, N; Dworkin, RH; Hill, J; Kitson, G; McCarthy, TD; McCloud, PI; Raff, M; Rice, ASC, 2014
)
1.85
[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)
Type-1A angiotensin II receptor Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00040.15553.8000AID37842
Type-1B angiotensin II receptorRattus norvegicus (Norway rat)IC50 (µMol)100.00000.00040.13343.8000AID37842
Type-1 angiotensin II receptorHomo sapiens (human)IC50 (µMol)0.03900.00020.09323.6000AID1560688
Type-2 angiotensin II receptorHomo sapiens (human)IC50 (µMol)5.00030.00010.02890.2000AID1560689; AID38150
Type-2 angiotensin II receptorHomo sapiens (human)Ki0.03950.00020.56507.7790AID1277889
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (50)

Processvia Protein(s)Taxonomy
regulation of cell growthType-1 angiotensin II receptorHomo sapiens (human)
kidney developmentType-1 angiotensin II receptorHomo sapiens (human)
renin-angiotensin regulation of aldosterone productionType-1 angiotensin II receptorHomo sapiens (human)
maintenance of blood vessel diameter homeostasis by renin-angiotensinType-1 angiotensin II receptorHomo sapiens (human)
regulation of systemic arterial blood pressure by renin-angiotensinType-1 angiotensin II receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationType-1 angiotensin II receptorHomo sapiens (human)
Rho protein signal transductionType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationType-1 angiotensin II receptorHomo sapiens (human)
regulation of vasoconstrictionType-1 angiotensin II receptorHomo sapiens (human)
calcium-mediated signalingType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of phospholipase A2 activityType-1 angiotensin II receptorHomo sapiens (human)
low-density lipoprotein particle remodelingType-1 angiotensin II receptorHomo sapiens (human)
regulation of renal sodium excretionType-1 angiotensin II receptorHomo sapiens (human)
angiotensin-activated signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
regulation of cell population proliferationType-1 angiotensin II receptorHomo sapiens (human)
symbiont entry into host cellType-1 angiotensin II receptorHomo sapiens (human)
regulation of inflammatory responseType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of inflammatory responseType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of protein metabolic processType-1 angiotensin II receptorHomo sapiens (human)
cell chemotaxisType-1 angiotensin II receptorHomo sapiens (human)
phospholipase C-activating angiotensin-activated signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
blood vessel diameter maintenanceType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of blood vessel endothelial cell proliferation involved in sprouting angiogenesisType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of CoA-transferase activityType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processType-1 angiotensin II receptorHomo sapiens (human)
inflammatory responseType-1 angiotensin II receptorHomo sapiens (human)
blood vessel remodelingType-2 angiotensin II receptorHomo sapiens (human)
regulation of systemic arterial blood pressure by circulatory renin-angiotensinType-2 angiotensin II receptorHomo sapiens (human)
angiotensin-mediated vasodilation involved in regulation of systemic arterial blood pressureType-2 angiotensin II receptorHomo sapiens (human)
brain renin-angiotensin systemType-2 angiotensin II receptorHomo sapiens (human)
cell surface receptor signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway coupled to cGMP nucleotide second messengerType-2 angiotensin II receptorHomo sapiens (human)
brain developmentType-2 angiotensin II receptorHomo sapiens (human)
regulation of blood pressureType-2 angiotensin II receptorHomo sapiens (human)
negative regulation of heart rateType-2 angiotensin II receptorHomo sapiens (human)
negative regulation of cell growthType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of phosphoprotein phosphatase activityType-2 angiotensin II receptorHomo sapiens (human)
regulation of metanephros sizeType-2 angiotensin II receptorHomo sapiens (human)
exploration behaviorType-2 angiotensin II receptorHomo sapiens (human)
nitric oxide-cGMP-mediated signalingType-2 angiotensin II receptorHomo sapiens (human)
angiotensin-activated signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
vasodilationType-2 angiotensin II receptorHomo sapiens (human)
negative regulation of blood vessel endothelial cell migrationType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionType-2 angiotensin II receptorHomo sapiens (human)
negative regulation of neurotrophin TRK receptor signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
neuron apoptotic processType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of metanephric glomerulus developmentType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of branching involved in ureteric bud morphogenesisType-2 angiotensin II receptorHomo sapiens (human)
positive regulation of extrinsic apoptotic signaling pathwayType-2 angiotensin II receptorHomo sapiens (human)
inflammatory responseType-2 angiotensin II receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
angiotensin type I receptor activityType-1 angiotensin II receptorHomo sapiens (human)
angiotensin type II receptor activityType-1 angiotensin II receptorHomo sapiens (human)
protein bindingType-1 angiotensin II receptorHomo sapiens (human)
bradykinin receptor bindingType-1 angiotensin II receptorHomo sapiens (human)
protein heterodimerization activityType-1 angiotensin II receptorHomo sapiens (human)
angiotensin type II receptor activityType-2 angiotensin II receptorHomo sapiens (human)
protein bindingType-2 angiotensin II receptorHomo sapiens (human)
receptor antagonist activityType-2 angiotensin II receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
plasma membraneType-1 angiotensin II receptorHomo sapiens (human)
membraneType-1 angiotensin II receptorHomo sapiens (human)
plasma membraneType-1 angiotensin II receptorHomo sapiens (human)
plasma membraneType-2 angiotensin II receptorHomo sapiens (human)
plasma membraneType-2 angiotensin II receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (14)

Assay IDTitleYearJournalArticle
AID1346340Human AT2 receptor (Angiotensin receptors)2014Lancet (London, England), May-10, Volume: 383, Issue:9929
Angiotensin II: from blood pressure to pain control.
AID1346340Human AT2 receptor (Angiotensin receptors)2013Pain medicine (Malden, Mass.), May, Volume: 14, Issue:5
Small molecule angiotensin II type 2 receptor (ATâ‚‚R) antagonists as novel analgesics for neuropathic pain: comparative pharmacokinetics, radioligand binding, and efficacy in rats.
AID1346340Human AT2 receptor (Angiotensin receptors)2014Lancet (London, England), May-10, Volume: 383, Issue:9929
EMA401, an orally administered highly selective angiotensin II type 2 receptor antagonist, as a novel treatment for postherpetic neuralgia: a randomised, double-blind, placebo-controlled phase 2 clinical trial.
AID1684346Efflux ratio of apparent permeability in human Caco-2 cells2021Bioorganic & medicinal chemistry, 01-01, Volume: 29N-(Methyloxycarbonyl)thiophene sulfonamides as high affinity AT2 receptor ligands.
AID1684341Half life in cryopreserved human hepatocytes at 1 uM measured after 15 mins by LC-MS/MS analysis2021Bioorganic & medicinal chemistry, 01-01, Volume: 29N-(Methyloxycarbonyl)thiophene sulfonamides as high affinity AT2 receptor ligands.
AID1560689Inhibition of human AT2 receptor2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
The Other Angiotensin II Receptor: AT
AID1277888Displacement of 125I-[Sar1,Leu8] angiotensin-2 from rat type 1 angiotensin-2 receptor expressed in African green monkey COS7 cells after 24 hrs2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Structural determinants of subtype selectivity and functional activity of angiotensin II receptors.
AID1684342Half life in mouse liver microsomes at 1 uM measured up to 60 mins in presence of NADPH by LC-MS/MS analysis2021Bioorganic & medicinal chemistry, 01-01, Volume: 29N-(Methyloxycarbonyl)thiophene sulfonamides as high affinity AT2 receptor ligands.
AID1684345Apparent permeability across apical to basolateral side and basolateral to apical side in human Caco-2 cells at 5 uM measured up to 60 mins by LC-MS/MS analysis2021Bioorganic & medicinal chemistry, 01-01, Volume: 29N-(Methyloxycarbonyl)thiophene sulfonamides as high affinity AT2 receptor ligands.
AID37842Inhibitory activity against Angiotensin II receptor, type 11996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID1684343Half life in human liver microsomes at 1 uM measured up to 60 mins in presence of NADPH by LC-MS/MS analysis2021Bioorganic & medicinal chemistry, 01-01, Volume: 29N-(Methyloxycarbonyl)thiophene sulfonamides as high affinity AT2 receptor ligands.
AID1277889Binding affinity to type-2 angiotensin-2 receptor (unknown origin)2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Structural determinants of subtype selectivity and functional activity of angiotensin II receptors.
AID1560688Inhibition of human AT1 receptor2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
The Other Angiotensin II Receptor: AT
AID38150Inhibitory activity was evaluated against Angiotensin II receptor, type 21996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (14.29)18.2507
2000's0 (0.00)29.6817
2010's4 (57.14)24.3611
2020's2 (28.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 31.84

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 Index31.84 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.40 (4.65)
Search Engine Demand Index35.70 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (31.84)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (14.29%)5.53%
Reviews2 (28.57%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (57.14%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]