Compounds > tg6-10-1
Page last updated: 2024-11-13

tg6-10-1

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

Description

TG6-10-1: brain-permeant prostaglandin E receptor 2 antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID71499384
CHEMBL ID3264204
MeSH IDM000612536

Synonyms (24)

Synonym
CHEMBL3264204 ,
CS-4637
bdbm50016950
AC-35262
HY-16978
tg6-10-1
1415716-58-3
AKOS027439955
(2e)-n-{2-[2-(trifluoromethyl)-1h-indol-1-yl]ethyl}-3-(3,4,5-trimethoxyphenyl)prop-2-enamide
mfcd29472234
(e)-n-(2-(2-(trifluoromethyl)-1h-indol-1-yl)ethyl)-3-(3,4,5-trimethoxyphenyl)acrylamide
NCGC00484068-01
BCP16857
(e)-n-[2-[2-(trifluoromethyl)indol-1-yl]ethyl]-3-(3,4,5-trimethoxyphenyl)prop-2-enamide
EX-A2407
nsc809120
nsc-809120
A910808
(e)-n-(2-(2-(trifluoromethyl)-1h-indol-3-yl)ethyl) -3-(3,4,5-trimethoxyphenyl)acrylamide
AS-55993
N11432
nsc-792867
nsc792867
wuyoecajfjfufc-cmdggobgsa-n

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (8)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC50 (µMol)75.00000.00010.88018.8500AID1155997
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC50 (µMol)7.50000.00011.18738.9125AID1151393
[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)Kb1.70001.70001.90002.1000AID1151378
Prostaglandin E2 receptor EP4 subtypeHomo sapiens (human)Kb8.60560.01120.01130.0114AID1142165; AID1151380
Prostaglandin E2 receptor EP3 subtypeHomo sapiens (human)Kb5.30000.00065.100210.0000AID1151379
Prostaglandin E2 receptor EP2 subtypeHomo sapiens (human)Kb0.08190.00180.02250.2100AID1142161; AID1151377; AID1151383
Prostacyclin receptorHomo sapiens (human)Kb8.28501.32005.96338.4500AID1142166; AID1151382
Prostaglandin D2 receptorHomo sapiens (human)Kb0.16650.03450.10050.1670AID1142162; AID1151381
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (97)

Processvia Protein(s)Taxonomy
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
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 (18)

Processvia Protein(s)Taxonomy
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
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 (19)

Processvia Protein(s)Taxonomy
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
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 (45)

Assay IDTitleYearJournalArticle
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.
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.
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.
AID1155997Inhibition of 5HT2A receptor (unknown origin)2014European journal of medicinal chemistry, Jul-23, Volume: 82Development of second generation EP2 antagonists with high selectivity.
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.
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.
AID1151392Ratio of drug level in brain to plasma in mouse2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
AID1142179Cmax in C57BL/6 mouse at 5 mg/kg, ip2014Journal 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.
AID1142188Terminal half life in C57BL/6 mouse plasma at 10 mg/kg, po2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1142176Half life in mouse liver microsomes at 10 uM2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
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.
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.
AID1142190Ratio of drug level in brain to plasma in C57BL/6 mouse at 5 mg/kg, ip measured after 1 to 2 hrs2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
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.
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.
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.
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.
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.
AID1151389Selectivity ratio of Kb for FP 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.
AID1142175Half life in human liver microsomes at 10 uM2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1142187Terminal half life in C57BL/6 mouse plasma at 5 mg/kg, ip2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1151391Half life in mouse plasma2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Prostanoid receptor EP2 as a therapeutic target.
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.
AID1151393Inhibition of 5-HT2B receptor (unknown origin)2014Journal 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.
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.
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.
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.
AID1151390Selectivity ratio of Kb for TP 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.
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.
AID1142183AUC(last) in C57BL/6 mouse at 5 mg/kg, ip2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1142191Ratio of drug level in brain to plasma in C57BL/6 mouse at 10 mg/kg, po measured after 1 to 2 hrs2014Journal 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.
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.
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.
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.
AID1142180Cmax in C57BL/6 mouse at 10 mg/kg, po2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Lead optimization studies of cinnamic amide EP2 antagonists.
AID1142184AUC(last) in C57BL/6 mouse at 10 mg/kg, po2014Journal 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.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's10 (66.67)24.3611
2020's5 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.94

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 Index16.94 (24.57)
Research Supply Index2.77 (2.92)
Research Growth Index4.53 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.94)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (13.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (86.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
pilocarpine
Pilocarpine: A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.. (+)-pilocarpine : The (+)-enantiomer of pilocarpine.		2.1110pilocarpineantiglaucoma drug
isoflurophate
Isoflurophate: A di-isopropyl-fluorophosphate which is an irreversible cholinesterase inhibitor used to investigate the NERVOUS SYSTEM.		3.9430dialkyl phosphate
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		2.1310pyrrole;
secondary amine
kainic acid
Kainic Acid: (2S-(2 alpha,3 beta,4 beta))-2-Carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid. Ascaricide obtained from the red alga Digenea simplex. It is a potent excitatory amino acid agonist at some types of excitatory amino acid receptors and has been used to discriminate among receptor types. Like many excitatory amino acid agonists it can cause neurotoxicity and has been used experimentally for that purpose.		2.2110dicarboxylic acid;
L-proline derivative;
non-proteinogenic L-alpha-amino acid;
pyrrolidinecarboxylic acid		antinematodal drug;
excitatory amino acid agonist
paxilline
paxilline: structure given in first source; RN given refers to (2R-(2alpha,4bbeta,6aalpha,12bbeta,12calpha,14abeta))-isomer. paxilline : An indole diterpene alkaloid with formula C27H33NO4 isolated from Penicillium paxilli. It is a potent inhibitor of large conductance Ca2(+)- and voltage-activated K(+) (BK)-type channels.		2.1310diterpene alkaloid;
enone;
organic heterohexacyclic compound;
terpenoid indole alkaloid;
tertiary alcohol		anticonvulsant;
Aspergillus metabolite;
EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor;
genotoxin;
geroprotector;
mycotoxin;
Penicillium metabolite;
potassium channel blocker
ah 6809
6-isopropoxy-9-oxoxanthene-2-carboxylic acid: structure given in UD		3.1910xanthones
kt 5720
KT 5720: indolocarbazole; synthetic derivative of K 252a. KT 5720 : An organic heterooctacyclic compound that is 1H,1'H-2,2'-biindole in which the nitrogens have undergone formal oxidative coupling to positions 2 and 5 of hexyl (3S)-3-hydroxy-2-methyltetrahydrofuran-3-carboxylate (the 2R,3S,5S product), and in which the 3 and 3' positions of the biindole moiety have also undergone formal oxidative coupling to positions 3 and 4 of 1,5-dihydro-2H-pyrrol-2-one.		2.1310carboxylic ester;
gamma-lactam;
hemiaminal;
indolocarbazole;
organic heterooctacyclic compound;
semisynthetic derivative;
tertiary alcohol		EC 2.7.11.11 (cAMP-dependent protein kinase) inhibitor
2-[[2-furanyl(oxo)methyl]amino]-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylic acid ethyl ester
[no description available]		3.1910organosulfur heterocyclic compound
dinoprostone
prostaglandin E2 : Prostaglandin F2alpha in which the hydroxy group at position 9 has been oxidised to the corresponding ketone. Prostaglandin E2 is the most common and most biologically potent of mammalian prostaglandins.		3.9330prostaglandins Ehuman metabolite;
mouse metabolite;
oxytocic
alprostadil
[no description available]		2.1310prostaglandins Eanticoagulant;
human metabolite;
platelet aggregation inhibitor;
vasodilator agent
butaprost
[no description available]		3.1910
ono-ae1-329
ONO-AE1-329: a 16-(m-methoxymethyl)phenyl derivative		2.1310
tg4-155
TG4-155: an EP2 receptor antagonist; structure in first source		3.8930
cp533536
CP533536: an EP2 receptor-selective prostaglandin E2 agonist that induces bone healing; structure in first source		3.1910monocarboxylic acid
butaprost
butaprost: highly selective prostaglandin receptor agonist; structure given in first source		2.1310
ono ae 248
ONO AE 248: structure in first source		2.1310
cp 544326
CP 544326: structure in first source		3.1910
pf-04418948
1-(4-fluorobenzoyl)-3-(((6-methoxy-2-naphthyl)oxy)methyl)azetidine-3-carboxylic acid: structure in first source		3.1910
ConditionIndicatedRelationship StrengthStudiesTrials
Degenerative Diseases, Central Nervous System
[description not available]		03.0110
Apoplexy
[description not available]		03.0110
Eye Disorders
[description not available]		03.0110
Eye Diseases
Diseases affecting the eye.		03.0110
Neurodegenerative Diseases
Hereditary and sporadic conditions which are characterized by progressive nervous system dysfunction. These disorders are often associated with atrophy of the affected central or peripheral nervous system structures.		03.0110
Stroke
A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)		03.0110
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		04.5980
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Cardiovascular Diseases
Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.		02.4110
Central Nervous System Disease
[description not available]		02.2510
Central Nervous System Diseases
Diseases of any component of the brain (including the cerebral hemispheres, diencephalon, brain stem, and cerebellum) or the spinal cord.		02.2510
Acute Brain Injuries
[description not available]		02.2110
Astrocytosis
[description not available]		02.5520
Innate Inflammatory Response
[description not available]		02.2110
Absence Seizure
[description not available]		02.2110
Absence Status
[description not available]		04.1650
Brain Injuries
Acute and chronic (see also BRAIN INJURIES, CHRONIC) injuries to the brain, including the cerebral hemispheres, CEREBELLUM, and BRAIN STEM. Clinical manifestations depend on the nature of injury. Diffuse trauma to the brain is frequently associated with DIFFUSE AXONAL INJURY or COMA, POST-TRAUMATIC. Localized injuries may be associated with NEUROBEHAVIORAL MANIFESTATIONS; HEMIPARESIS, or other focal neurologic deficits.		02.2110
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		02.2110
Seizures
Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.		02.2110
Status Epilepticus
A prolonged seizure or seizures repeated frequently enough to prevent recovery between episodes occurring over a period of 20-30 minutes. The most common subtype is generalized tonic-clonic status epilepticus, a potentially fatal condition associated with neuronal injury and respiratory and metabolic dysfunction. Nonconvulsive forms include petit mal status and complex partial status, which may manifest as behavioral disturbances. Simple partial status epilepticus consists of persistent motor, sensory, or autonomic seizures that do not impair cognition (see also EPILEPSIA PARTIALIS CONTINUA). Subclinical status epilepticus generally refers to seizures occurring in an unresponsive or comatose individual in the absence of overt signs of seizure activity. (From N Engl J Med 1998 Apr 2;338(14):970-6; Neurologia 1997 Dec;12 Suppl 6:25-30)		04.1650
Organophosphorus Poisoning
[description not available]		03.1710
Organophosphate Poisoning
Poisoning due to exposure to ORGANOPHOSPHORUS COMPOUNDS, such as ORGANOPHOSPHATES; ORGANOTHIOPHOSPHATES; and ORGANOTHIOPHOSPHONATES.		03.1710
Brain Inflammation
[description not available]		02.1110
Encephalitis
Inflammation of the BRAIN due to infection, autoimmune processes, toxins, and other conditions. Viral infections (see ENCEPHALITIS, VIRAL) are a relatively frequent cause of this condition.		02.1110
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		02.1110
Age-Related Memory Disorders
[description not available]		02.1310
Anxiety
Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.		02.1310
Memory Disorders
Disturbances in registering an impression, in the retention of an acquired impression, or in the recall of an impression. Memory impairments are associated with DEMENTIA; CRANIOCEREBRAL TRAUMA; ENCEPHALITIS; ALCOHOLISM (see also ALCOHOL AMNESTIC DISORDER); SCHIZOPHRENIA; and other conditions.		02.1310
Endometrioma
An enlarged area of ENDOMETRIOSIS that resembles a tumor. It is usually found in the OVARY. When it is filled with old blood, it is known as a chocolate cyst.		02.1510
Allodynia
[description not available]		02.1510
Endometriosis
A condition in which functional endometrial tissue is present outside the UTERUS. It is often confined to the PELVIS involving the OVARY, the ligaments, cul-de-sac, and the uterovesical peritoneum.		02.1510