Page last updated: 2024-12-11

tg4-155

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Description

TG4-155: an EP2 receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5886965
CHEMBL ID1368005
SCHEMBL ID14333686
MeSH IDM0582497

Synonyms (24)

Synonym
AKOS001816787
MLS000724641
smr000237431
(e)-n-[2-(2-methylindol-1-yl)ethyl]-3-(3,4,5-trimethoxyphenyl)prop-2-enamide
HMS2242E03
S6793
gtpl5818
tg4-155
SCHEMBL14333686
CHEMBL1368005 ,
1164462-05-8
(2e)-n-[2-(2-methyl-1h-indol-1-yl)ethyl]-3-(3,4,5-trimethoxyphenyl)-2-propenamide
tg 4-155
bdbm50016949
(e)-n-(2-(2-methyl-1h-indol-1-yl)ethyl)-3-(3,4,5-trimethoxyphenyl)acrylamide
F20810
YBHUXHFZLMFETJ-MDZDMXLPSA-N ,
Q27088974
AS-16484
EX-A2930
CS-0014805
HY-18971
nsc767453
nsc-767453
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (20)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency7.07950.003245.467312,589.2998AID2517
Chain A, Beta-lactamaseEscherichia coli K-12Potency35.48130.044717.8581100.0000AID485341
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency89.12510.631035.7641100.0000AID504339
Chain A, CruzipainTrypanosoma cruziPotency39.81070.002014.677939.8107AID1476
glp-1 receptor, partialHomo sapiens (human)Potency28.18380.01846.806014.1254AID624417
ATAD5 protein, partialHomo sapiens (human)Potency12.99530.004110.890331.5287AID504467
TDP1 proteinHomo sapiens (human)Potency24.84460.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency29.88160.180013.557439.8107AID1460; AID1468
67.9K proteinVaccinia virusPotency28.18380.00018.4406100.0000AID720579
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency79.43280.707936.904389.1251AID504333
importin subunit beta-1 isoform 1Homo sapiens (human)Potency19.95265.804836.130665.1308AID540263
snurportin-1Homo sapiens (human)Potency19.95265.804836.130665.1308AID540263
lamin isoform A-delta10Homo sapiens (human)Potency12.58930.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC50 (µMol)2.60000.00011.18738.9125AID1151393
[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)
Prostaglandin E2 receptor EP1 subtypeHomo sapiens (human)Kb2.10001.70001.90002.1000AID1151378
Prostaglandin E2 receptor EP4 subtypeHomo sapiens (human)Kb7.60380.01120.01130.0114AID1142165; AID1151380; AID1551728
Prostaglandin E2 receptor EP3 subtypeHomo sapiens (human)Kb10.00000.00065.100210.0000AID1151379
Prostaglandin E2 receptor EP2 subtypeHomo sapiens (human)Kb0.00360.00180.02250.2100AID1142161; AID1151377; AID1151383; AID1156007; AID1528795; AID1551727
Prostacyclin receptorHomo sapiens (human)Kb31.66001.32005.96338.4500AID1142166; AID1151382
Prostaglandin D2 receptorHomo sapiens (human)Kb0.03450.03450.10050.1670AID1142162; AID1151381
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (72)

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)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo 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)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerProstacyclin receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayProstacyclin receptorHomo sapiens (human)
cell-cell signalingProstacyclin receptorHomo sapiens (human)
negative regulation of platelet-derived growth factor receptor signaling pathwayProstacyclin receptorHomo sapiens (human)
response to lipopolysaccharideProstacyclin receptorHomo sapiens (human)
negative regulation of smooth muscle cell proliferationProstacyclin receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstacyclin receptorHomo sapiens (human)
inflammatory responseProstacyclin receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin D2 receptorHomo sapiens (human)
male sex determinationProstaglandin D2 receptorHomo sapiens (human)
sleepProstaglandin D2 receptorHomo sapiens (human)
mast cell degranulationProstaglandin D2 receptorHomo sapiens (human)
adenosine metabolic processProstaglandin D2 receptorHomo sapiens (human)
cellular response to prostaglandin D stimulusProstaglandin D2 receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin D2 receptorHomo sapiens (human)
inflammatory responseProstaglandin D2 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

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)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
prostaglandin E receptor activityProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
prostaglandin E receptor activityProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
guanyl-nucleotide exchange factor activityProstacyclin receptorHomo sapiens (human)
prostacyclin receptor activityProstacyclin receptorHomo sapiens (human)
prostaglandin J receptor activityProstaglandin D2 receptorHomo sapiens (human)
prostaglandin D receptor activityProstaglandin D2 receptorHomo sapiens (human)
protein bindingProstaglandin D2 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

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)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo 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)
cytosolProstacyclin receptorHomo sapiens (human)
plasma membraneProstacyclin receptorHomo sapiens (human)
plasma membraneProstacyclin receptorHomo sapiens (human)
plasma membraneProstaglandin D2 receptorHomo sapiens (human)
membraneProstaglandin D2 receptorHomo sapiens (human)
plasma membraneProstaglandin D2 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (54)

Assay IDTitleYearJournalArticle
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1142172Metabolic stability in human liver microsomes assessed as compound remaining at 10 uM after 60 mins2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1151394Selectivity ratio of IC50 for 5-HT2B receptor (unknown origin) to Kb for EP2 receptor (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151379Antagonist activity at EP3 receptor (unknown origin) by functional cAMP assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1528795Antagonist activity at human EP2 transfected in rat C6 cells assessed as decrease in intracellular cAMP incubated for 10 mins followed by PGE2 addition and measured after 40 mins by TR-FRET assay2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist for Use in Central Nervous System Disease Models.
AID1142171Metabolic stability in human liver microsomes assessed as compound remaining at 1 uM after 60 mins2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1551729Selectivity index, ratio of kb for EP4 receptor (unknown origin) to kb for human EP2 receptor2019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1142169Cytotoxicity against rat C6 cells assessed as cell viability2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1151365Inhibition of status epilepticus mouse assessed as assessed as blockade of neuronal damage in hippocampus hilus region2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151377Antagonist activity at EP2 receptor (unknown origin) by functional cAMP assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151382Antagonist activity at prostanoid IP receptor (unknown origin) by functional cAMP assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151387Selectivity ratio of Kb for prostanoid IP receptor (unknown origin) to Kb for EP2 receptor (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151393Inhibition of 5-HT2B receptor (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1142165Antagonist activity at human EP4 receptor expressed in rat C6 cells assessed as intracellular cAMP accumulation treated for 10 mins prior to PGE2 challenge for 40 mins by TR-FRET assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1142166Antagonist activity at human IP receptor expressed in rat C6 cells assessed as intracellular cAMP accumulation treated for 10 mins prior to iloprost challenge for 40 mins by TR-FRET assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1142164Aqueous solubility of the compound in PBS buffer with 1% DMSO at pH 7.4 by nephelometry2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1142163Selectivity index, ratio of KB for human DP1 receptor expressed in rat C6 cells to KB for human EP2 receptor expressed in rat C6 cells2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1151380Antagonist activity at EP4 receptor (unknown origin) by functional cAMP assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1156007Competitive antagonist activity at human EP2 receptor assessed as inhibition of PGE2-induced response2014European journal of medicinal chemistry, Jul-23, Volume: 82Development of second generation EP2 antagonists with high selectivity.
AID1142177Cmax in C57BL/6 mouse at 3 mg/kg, iv2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1142168Selectivity index, ratio of KB for human IP receptor expressed in rat C6 cells to KB for human EP2 receptor expressed in rat C6 cells2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1142189Ratio of drug level in brain to plasma in C57BL/6 mouse at 3 mg/kg, iv measured after 1 to 2 hrs2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1151381Antagonist activity at DP1 receptor (unknown origin) by functional cAMP assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151378Antagonist activity at EP1 receptor (unknown origin) by functional cAMP assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151385Selectivity ratio of Kb for EP3 receptor (unknown origin) to Kb for EP2 receptor (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1551728Competitive inhibition of EP4 receptor (unknown origin)2019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1142162Antagonist activity at human DP1 receptor expressed in rat C6 cells assessed as intracellular cAMP accumulation at 10 uM treated for 10 mins prior to BW245C challenge for 40 mins by TR-FRET assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1142174Metabolic stability in mouse liver microsomes assessed as compound remaining at 10 uM after 60 mins2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1151388Selectivity ratio of Kb for DP1 receptor (unknown origin) to Kb for EP2 receptor (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151384Selectivity ratio of Kb for EP1 receptor (unknown origin) to Kb for EP2 receptor (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1142185Terminal half life in C57BL/6 mouse plasma at 3 mg/kg, iv2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1151383Inhibition of EP2 receptor (unknown origin) by competitive binding assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1551727Competitive inhibition of human EP2 receptor expressed in C6G cells preincubated for 5 mins followed by increase in PGE2 concentration measured after 40 mins by radioligand binding assay2019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1151367Inhibition of status epilepticus mouse assessed as assessed as blockade of neuronal damage in hippocampus CA1 region2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1151386Selectivity ratio of Kb for EP4 receptor (unknown origin) to Kb for EP2 receptor (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1142161Antagonist activity at human EP2 receptor expressed in rat C6 cells assessed as 2-fold rightward shift in PGE2 concentration-response curve at 1 uM treated for 10 mins prior to PGE2 challenge for 40 mins by TR-FRET assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1142181AUC(last) in C57BL/6 mouse at 3 mg/kg, iv2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1142173Metabolic stability in mouse liver microsomes assessed as compound remaining at 1 uM after 60 mins2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1151366Inhibition of status epilepticus mouse assessed as assessed as blockade of neuronal damage in hippocampus CA3 region2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1142170Therapeutic index, ratio of CC50 for rat C6 cells to KB for human EP2 receptor expressed in rat C6 cells2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1142167Selectivity index, ratio of KB for human EP4 receptor expressed in rat C6 cells to KB for human EP2 receptor expressed in rat C6 cells2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1346308Human EP2 receptor (Prostanoid receptors)2012Proceedings of the National Academy of Sciences of the United States of America, Feb-21, Volume: 109, Issue:8
Small molecule antagonist reveals seizure-induced mediation of neuronal injury by prostaglandin E2 receptor subtype EP2.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (8.33)29.6817
2010's9 (75.00)24.3611
2020's2 (16.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.30

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 Index17.30 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.68 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.30)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (83.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]