Page last updated: 2024-11-11

terbogrel

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 CID6449876
CHEMBL ID281398
CHEBI ID177760
SCHEMBL ID42848
SCHEMBL ID15413063
MeSH IDM0290537

Synonyms (35)

Synonym
unii-5z4kwq5ogn
(e)-6-(3-(((cyanoamino)((1,1-dimethylethyl)amino)methylene)amino)phenyl)-6-(3-pyridinyl-5-hexenoic acid
(5e)-6-(m-(3-tert-butyl-2-cyanoguanidino)phenyl)-6-(3-pyridyl)-5-hexenoic acid
terbogrel [usan:inn]
6-(3-(((cyanoamino)((1,1-dimethylethyl)amino)methylene)amino)phenyl)-6-(3-pyridinyl)hexenoic acid
5z4kwq5ogn ,
6-{3-[1-(tert-butylamino)-2-cyano-(e)-1-iminomethylamino]phenyl}-6-(3-pyridyl)-(e)-5-hexenoic acid
bdbm50075624
6-{3-[1-(tert-butylamino)-2-cyano-(z)-1-iminomethylamino]phenyl}-6-(3-pyridyl)-(z)-5-hexenoic acid
(e)-6-[3-[(n'-tert-butyl-n-cyanocarbamimidoyl)amino]phenyl]-6-pyridin-3-ylhex-5-enoic acid
CHEBI:177760
D06077
terbogrel (usan/inn)
149979-74-8
terbogrel
CHEMBL281398 ,
bibv 308 se
bibv-308se
bibv-308-se
L001474
terbogrel [usan]
terbogrel [who-dd]
terbogrel [inn]
(e)-6-(3-(((cyanoamino)((1,1-dimethylethyl)amino)methylene)amino)phenyl)-6-(3-pyridinyl)-5-hexenoic acid
SCHEMBL42848
SCHEMBL15413063
CS-6743
HY-19189
DB12204
Q7701660
e-6-[4-(3-tert-butyl-2-cyanoguanidino)phenyl]-6-(3-pyridyl)hex-5-enoic acid
(e)-6-(3-(((tert-butylamino)(cyanamido)methylene)amino)phenyl)-6-(pyridin-3-yl)hex-5-enoic acid
(e)-6-(3-(((tert-butylamino)(cyanamido)methylene)amino)phenyl)-6-(pyridin-3-yl)hex-5-enoicacid
terbogel
AKOS040742708

Research Excerpts

Overview

Terbogrel is a potent agent having two distinct, complimentary pharmacodynamic actions. It inhibits thromboxane synthase and antagonism of the TxA2 receptor.

ExcerptReferenceRelevance
"Terbogrel is a potent agent having two distinct, complimentary pharmacodynamic actions, namely inhibition of thromboxane synthase and antagonism of the TxA2 receptor. "( Pharmacokinetics and pharmacodynamics of terbogrel, a combined thromboxane A2 receptor and synthase inhibitor, in healthy subjects.
Guth, BD; Narjes, H; Nehmiz, G; Riedel, A; Schubert, HD; Tanswell, P, 2004
)
2.03
"Terbogrel appears to be a compound with an equipotent molar potency as thromboxane A2 synthase inhibitor and receptor antagonist."( Effects of terbogrel on platelet function and prostaglandin endoperoxide transfer.
Muck, S; Schrör, K; Weber, AA, 1998
)
1.41

Pharmacokinetics

ExcerptReferenceRelevance
"Terbogrel is a potent agent having two distinct, complimentary pharmacodynamic actions, namely inhibition of thromboxane synthase and antagonism of the TxA2 receptor."( Pharmacokinetics and pharmacodynamics of terbogrel, a combined thromboxane A2 receptor and synthase inhibitor, in healthy subjects.
Guth, BD; Narjes, H; Nehmiz, G; Riedel, A; Schubert, HD; Tanswell, P, 2004
)
2.03
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
diterpene glycosideA terpene glycoside in which the terpene moiety is a diterpenoid.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Thromboxane A2 receptor Homo sapiens (human)IC50 (µMol)0.01100.00110.71065.2000AID212273
Thromboxane-A synthase Homo sapiens (human)IC50 (µMol)0.00400.00091.230410.0000AID212612
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

Processvia Protein(s)Taxonomy
smooth muscle contractionThromboxane A2 receptor Homo sapiens (human)
G protein-coupled receptor signaling pathwayThromboxane A2 receptor Homo sapiens (human)
response to nutrientThromboxane A2 receptor Homo sapiens (human)
response to xenobiotic stimulusThromboxane A2 receptor Homo sapiens (human)
positive regulation of blood coagulationThromboxane A2 receptor Homo sapiens (human)
response to testosteroneThromboxane A2 receptor Homo sapiens (human)
thromboxane A2 signaling pathwayThromboxane A2 receptor Homo sapiens (human)
response to ethanolThromboxane A2 receptor Homo sapiens (human)
positive regulation of angiogenesisThromboxane A2 receptor Homo sapiens (human)
positive regulation of smooth muscle contractionThromboxane A2 receptor Homo sapiens (human)
cellular response to lipopolysaccharideThromboxane A2 receptor Homo sapiens (human)
negative regulation of cell migration involved in sprouting angiogenesisThromboxane A2 receptor Homo sapiens (human)
inflammatory responseThromboxane A2 receptor Homo sapiens (human)
positive regulation of blood pressureThromboxane A2 receptor Homo sapiens (human)
positive regulation of vasoconstrictionThromboxane A2 receptor Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationThromboxane A2 receptor Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayThromboxane A2 receptor Homo sapiens (human)
prostaglandin biosynthetic processThromboxane-A synthase Homo sapiens (human)
icosanoid metabolic processThromboxane-A synthase Homo sapiens (human)
cyclooxygenase pathwayThromboxane-A synthase Homo sapiens (human)
intracellular chloride ion homeostasisThromboxane-A synthase Homo sapiens (human)
response to ethanolThromboxane-A synthase Homo sapiens (human)
positive regulation of vasoconstrictionThromboxane-A synthase Homo sapiens (human)
response to fatty acidThromboxane-A synthase Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
thromboxane A2 receptor activityThromboxane A2 receptor Homo sapiens (human)
guanyl-nucleotide exchange factor activityThromboxane A2 receptor Homo sapiens (human)
protein bindingThromboxane A2 receptor Homo sapiens (human)
monooxygenase activityThromboxane-A synthase Homo sapiens (human)
thromboxane-A synthase activityThromboxane-A synthase Homo sapiens (human)
iron ion bindingThromboxane-A synthase Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygenThromboxane-A synthase Homo sapiens (human)
heme bindingThromboxane-A synthase Homo sapiens (human)
12-hydroxyheptadecatrienoic acid synthase activityThromboxane-A synthase Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityThromboxane-A synthase Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
acrosomal vesicleThromboxane A2 receptor Homo sapiens (human)
plasma membraneThromboxane A2 receptor Homo sapiens (human)
nuclear speckThromboxane A2 receptor Homo sapiens (human)
plasma membraneThromboxane A2 receptor Homo sapiens (human)
endoplasmic reticulumThromboxane-A synthase Homo sapiens (human)
endoplasmic reticulum membraneThromboxane-A synthase Homo sapiens (human)
cytosolThromboxane-A synthase Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (3)

Assay IDTitleYearJournalArticle
AID212612In vitro activity on thromboxane A2 synthase inhibition in gel filtered human platelets.1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors.
AID89060In vitro activity expressed as EC50 for inhibition of collagen induced platelet aggregation.1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors.
AID212273In vitro activity on thromboxane A2 receptor antagonism in gel filtered human platelets.1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors.
[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's2 (16.67)18.2507
2000's9 (75.00)29.6817
2010's1 (8.33)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.73

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.73 (24.57)
Research Supply Index2.83 (2.92)
Research Growth Index4.57 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.73)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (23.08%)5.53%
Reviews4 (30.77%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (46.15%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]