Page last updated: 2024-11-13

endothelins

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 CID44284481
MeSH IDM0024788

Synonyms (4)

Synonym
endothelin
endothelin (porcine)
et 1
bdbm50289653
[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)
Endothelin receptor type BRattus norvegicus (Norway rat)IC50 (µMol)0.00160.00001.17444.4000AID66878
Endothelin receptor type BHomo sapiens (human)IC50 (µMol)0.00020.00010.65659.8000AID66032; AID751683
Endothelin receptor type BHomo sapiens (human)Ki0.00010.00010.05430.3710AID751683
Endothelin-1 receptorHomo sapiens (human)IC50 (µMol)0.00020.00000.76479.9000AID340243; AID346417; AID468184; AID66032; AID751682; AID751886; AID752247
Endothelin-1 receptorHomo sapiens (human)Ki0.00010.00000.430010.0000AID346417; AID751682; AID751886
Endothelin-1 receptorSus scrofa (pig)IC50 (µMol)0.00020.00020.61372.9000AID68646
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (109)

Processvia Protein(s)Taxonomy
negative regulation of transcription by RNA polymerase IIEndothelin receptor type BHomo sapiens (human)
neural crest cell migrationEndothelin receptor type BHomo sapiens (human)
positive regulation of protein phosphorylationEndothelin receptor type BHomo sapiens (human)
renin secretion into blood streamEndothelin receptor type BHomo sapiens (human)
regulation of heart rateEndothelin receptor type BHomo sapiens (human)
regulation of pHEndothelin receptor type BHomo sapiens (human)
cell surface receptor signaling pathwayEndothelin receptor type BHomo sapiens (human)
negative regulation of adenylate cyclase activityEndothelin receptor type BHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayEndothelin receptor type BHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationEndothelin receptor type BHomo sapiens (human)
nervous system developmentEndothelin receptor type BHomo sapiens (human)
peripheral nervous system developmentEndothelin receptor type BHomo sapiens (human)
posterior midgut developmentEndothelin receptor type BHomo sapiens (human)
positive regulation of cell population proliferationEndothelin receptor type BHomo sapiens (human)
gene expressionEndothelin receptor type BHomo sapiens (human)
negative regulation of neuron maturationEndothelin receptor type BHomo sapiens (human)
response to organic cyclic compoundEndothelin receptor type BHomo sapiens (human)
vein smooth muscle contractionEndothelin receptor type BHomo sapiens (human)
calcium-mediated signalingEndothelin receptor type BHomo sapiens (human)
cGMP-mediated signalingEndothelin receptor type BHomo sapiens (human)
heparin metabolic processEndothelin receptor type BHomo sapiens (human)
melanocyte differentiationEndothelin receptor type BHomo sapiens (human)
regulation of fever generationEndothelin receptor type BHomo sapiens (human)
aldosterone metabolic processEndothelin receptor type BHomo sapiens (human)
enteric smooth muscle cell differentiationEndothelin receptor type BHomo sapiens (human)
positive regulation of urine volumeEndothelin receptor type BHomo sapiens (human)
renal sodium excretionEndothelin receptor type BHomo sapiens (human)
epithelial fluid transportEndothelin receptor type BHomo sapiens (human)
vasoconstrictionEndothelin receptor type BHomo sapiens (human)
vasodilationEndothelin receptor type BHomo sapiens (human)
negative regulation of apoptotic processEndothelin receptor type BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionEndothelin receptor type BHomo sapiens (human)
macrophage chemotaxisEndothelin receptor type BHomo sapiens (human)
response to painEndothelin receptor type BHomo sapiens (human)
enteric nervous system developmentEndothelin receptor type BHomo sapiens (human)
regulation of epithelial cell proliferationEndothelin receptor type BHomo sapiens (human)
negative regulation of protein metabolic processEndothelin receptor type BHomo sapiens (human)
canonical Wnt signaling pathwayEndothelin receptor type BHomo sapiens (human)
positive regulation of penile erectionEndothelin receptor type BHomo sapiens (human)
establishment of endothelial barrierEndothelin receptor type BHomo sapiens (human)
renal sodium ion absorptionEndothelin receptor type BHomo sapiens (human)
calcium ion transmembrane transportEndothelin receptor type BHomo sapiens (human)
cellular response to lipopolysaccharideEndothelin receptor type BHomo sapiens (human)
protein transmembrane transportEndothelin receptor type BHomo sapiens (human)
podocyte differentiationEndothelin receptor type BHomo sapiens (human)
endothelin receptor signaling pathwayEndothelin receptor type BHomo sapiens (human)
renal albumin absorptionEndothelin receptor type BHomo sapiens (human)
neuroblast migrationEndothelin receptor type BHomo sapiens (human)
chordate pharynx developmentEndothelin receptor type BHomo sapiens (human)
response to sodium phosphateEndothelin receptor type BHomo sapiens (human)
response to endothelinEndothelin receptor type BHomo sapiens (human)
developmental pigmentationEndothelin receptor type BHomo sapiens (human)
mitotic cell cycleEndothelin-1 receptorHomo sapiens (human)
branching involved in blood vessel morphogenesisEndothelin-1 receptorHomo sapiens (human)
response to hypoxiaEndothelin-1 receptorHomo sapiens (human)
in utero embryonic developmentEndothelin-1 receptorHomo sapiens (human)
blood vessel remodelingEndothelin-1 receptorHomo sapiens (human)
response to amphetamineEndothelin-1 receptorHomo sapiens (human)
regulation of heart rateEndothelin-1 receptorHomo sapiens (human)
glomerular filtrationEndothelin-1 receptorHomo sapiens (human)
cardiac chamber formationEndothelin-1 receptorHomo sapiens (human)
left ventricular cardiac muscle tissue morphogenesisEndothelin-1 receptorHomo sapiens (human)
atrial cardiac muscle tissue developmentEndothelin-1 receptorHomo sapiens (human)
cardiac neural crest cell migration involved in outflow tract morphogenesisEndothelin-1 receptorHomo sapiens (human)
noradrenergic neuron differentiationEndothelin-1 receptorHomo sapiens (human)
intracellular calcium ion homeostasisEndothelin-1 receptorHomo sapiens (human)
smooth muscle contractionEndothelin-1 receptorHomo sapiens (human)
mitochondrion organizationEndothelin-1 receptorHomo sapiens (human)
signal transductionEndothelin-1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayEndothelin-1 receptorHomo sapiens (human)
activation of adenylate cyclase activityEndothelin-1 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayEndothelin-1 receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayEndothelin-1 receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationEndothelin-1 receptorHomo sapiens (human)
respiratory gaseous exchange by respiratory systemEndothelin-1 receptorHomo sapiens (human)
regulation of blood pressureEndothelin-1 receptorHomo sapiens (human)
cell population proliferationEndothelin-1 receptorHomo sapiens (human)
response to woundingEndothelin-1 receptorHomo sapiens (human)
gene expressionEndothelin-1 receptorHomo sapiens (human)
protein kinase A signalingEndothelin-1 receptorHomo sapiens (human)
regulation of glucose transmembrane transportEndothelin-1 receptorHomo sapiens (human)
neural crest cell fate commitmentEndothelin-1 receptorHomo sapiens (human)
artery smooth muscle contractionEndothelin-1 receptorHomo sapiens (human)
neuron remodelingEndothelin-1 receptorHomo sapiens (human)
heparin metabolic processEndothelin-1 receptorHomo sapiens (human)
thyroid gland developmentEndothelin-1 receptorHomo sapiens (human)
cellular response to oxidative stressEndothelin-1 receptorHomo sapiens (human)
embryonic heart tube developmentEndothelin-1 receptorHomo sapiens (human)
aorta developmentEndothelin-1 receptorHomo sapiens (human)
vasoconstrictionEndothelin-1 receptorHomo sapiens (human)
norepinephrine metabolic processEndothelin-1 receptorHomo sapiens (human)
middle ear morphogenesisEndothelin-1 receptorHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionEndothelin-1 receptorHomo sapiens (human)
cellular response to human chorionic gonadotropin stimulusEndothelin-1 receptorHomo sapiens (human)
enteric nervous system developmentEndothelin-1 receptorHomo sapiens (human)
sympathetic nervous system developmentEndothelin-1 receptorHomo sapiens (human)
axon extensionEndothelin-1 receptorHomo sapiens (human)
embryonic skeletal system developmentEndothelin-1 receptorHomo sapiens (human)
neuromuscular processEndothelin-1 receptorHomo sapiens (human)
sodium ion homeostasisEndothelin-1 receptorHomo sapiens (human)
canonical Wnt signaling pathwayEndothelin-1 receptorHomo sapiens (human)
face developmentEndothelin-1 receptorHomo sapiens (human)
axonogenesis involved in innervationEndothelin-1 receptorHomo sapiens (human)
establishment of endothelial barrierEndothelin-1 receptorHomo sapiens (human)
pharyngeal arch artery morphogenesisEndothelin-1 receptorHomo sapiens (human)
renal sodium ion absorptionEndothelin-1 receptorHomo sapiens (human)
calcium ion transmembrane transportEndothelin-1 receptorHomo sapiens (human)
cellular response to follicle-stimulating hormone stimulusEndothelin-1 receptorHomo sapiens (human)
cellular response to luteinizing hormone stimulusEndothelin-1 receptorHomo sapiens (human)
protein transmembrane transportEndothelin-1 receptorHomo sapiens (human)
glomerular endothelium developmentEndothelin-1 receptorHomo sapiens (human)
podocyte differentiationEndothelin-1 receptorHomo sapiens (human)
endothelin receptor signaling pathway involved in heart processEndothelin-1 receptorHomo sapiens (human)
renal albumin absorptionEndothelin-1 receptorHomo sapiens (human)
vascular associated smooth muscle cell developmentEndothelin-1 receptorHomo sapiens (human)
mesenchymal cell apoptotic processEndothelin-1 receptorHomo sapiens (human)
sympathetic neuron axon guidanceEndothelin-1 receptorHomo sapiens (human)
semaphorin-plexin signaling pathway involved in axon guidanceEndothelin-1 receptorHomo sapiens (human)
podocyte apoptotic processEndothelin-1 receptorHomo sapiens (human)
meiotic cell cycle process involved in oocyte maturationEndothelin-1 receptorHomo sapiens (human)
cranial skeletal system developmentEndothelin-1 receptorHomo sapiens (human)
response to acetylcholineEndothelin-1 receptorHomo sapiens (human)
regulation of protein localization to cell leading edgeEndothelin-1 receptorHomo sapiens (human)
positive regulation of cation channel activityEndothelin-1 receptorHomo sapiens (human)
endothelin receptor signaling pathwayEndothelin-1 receptorHomo sapiens (human)
developmental pigmentationEndothelin-1 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
endothelin receptor activityEndothelin receptor type BHomo sapiens (human)
protein bindingEndothelin receptor type BHomo sapiens (human)
peptide hormone bindingEndothelin receptor type BHomo sapiens (human)
type 1 angiotensin receptor bindingEndothelin receptor type BHomo sapiens (human)
phosphatidylinositol phospholipase C activityEndothelin-1 receptorHomo sapiens (human)
endothelin receptor activityEndothelin-1 receptorHomo sapiens (human)
protein bindingEndothelin-1 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
plasma membraneEndothelin receptor type BHomo sapiens (human)
nuclear membraneEndothelin receptor type BHomo sapiens (human)
plasma membraneEndothelin receptor type BHomo sapiens (human)
plasma membraneEndothelin-1 receptorHomo sapiens (human)
plasma membraneEndothelin-1 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (22)

Assay IDTitleYearJournalArticle
AID66878Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranes1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
Design of a functional hexapeptide antagonist of endothelin.
AID159556Endothelin A receptor agonist activity as maximum vasoconstriction in porcine coronary artery1993Journal of medicinal chemistry, Dec-10, Volume: 36, Issue:25
Endothelin-1 analogues substituted at both position 18 and 19: highly potent endothelin antagonists with no selectivity for either receptor subtype ETA or ETB.
AID66032Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
Design of a functional hexapeptide antagonist of endothelin.
AID751683Displacement of [125I]Endothelin-1 from human recombinant ETB receptor expressed in CHOK1 cells after 2 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID752247Binding affinity to human ETA receptor by radioligand displacement assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
AID66212Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
Endothelin: a new challenge.
AID139400Compound induced increase in cystolic free ca+2 concentration in murine peritoneal macrophages was measured1993Journal of medicinal chemistry, Dec-10, Volume: 36, Issue:25
Endothelin-1 analogues substituted at both position 18 and 19: highly potent endothelin antagonists with no selectivity for either receptor subtype ETA or ETB.
AID751682Displacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID751886Binding affinity to human ETA receptor by radioligand displacement assay2013European journal of medicinal chemistry, May, Volume: 63Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
AID346417Displacement of radiolabeled endothelin-1 from human endothelin ETA receptor2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
AID66355Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptor1993Journal of medicinal chemistry, Dec-10, Volume: 36, Issue:25
Endothelin-1 analogues substituted at both position 18 and 19: highly potent endothelin antagonists with no selectivity for either receptor subtype ETA or ETB.
AID468184Inhibition of ETA receptor in human SK-N-MC cells after 60 mins by scintillation counting2009Journal of natural products, Dec, Volume: 72, Issue:12
5-OHKF and NorKA, depsipeptides from a Hawaiian collection of Bryopsis pennata: binding properties for NorKA to the human neuropeptide Y Y1 receptor.
AID165865Antagonism of the endothelin stimulated accumulation of arachidonic acid release (AAR) was determined in cultured rabbit renal artery vascular smooth muscle cells1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
Design of a functional hexapeptide antagonist of endothelin.
AID67028Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
Endothelin: a new challenge.
AID751748Displacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells at 10 uM after 2 hrs relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID66211Compound was evaluated for the binding affinity to Endothelin A receptor in the rat aorta1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
Endothelin: a new challenge.
AID190017Antagonism of the endothelin stimulated accumulation of inositol phosphate (IP3) was determined in cultured rat skin fibroblasts1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
Design of a functional hexapeptide antagonist of endothelin.
AID681599TP_TRANSPORTER: uptake in membrane vesicles from Mrp2-expressing Sf9 cells2000Molecular pharmacology, Mar, Volume: 57, Issue:3
Transport function and hepatocellular localization of mrp6 in rat liver.
AID340243Inhibition of human ETA receptor2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
AID751747Displacement of [125I]Endothelin-1 from human recombinant ETB receptor expressed in CHOK1 cells at 10 uM after 2 hrs relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID68646Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor1993Journal of medicinal chemistry, Dec-10, Volume: 36, Issue:25
Endothelin-1 analogues substituted at both position 18 and 19: highly potent endothelin antagonists with no selectivity for either receptor subtype ETA or ETB.
AID67029Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
Endothelin: a new challenge.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (30.00)18.2507
2000's4 (40.00)29.6817
2010's3 (30.00)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: 65.37

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index65.37 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.46 (4.65)
Search Engine Demand Index132.98 (26.88)
Search Engine Supply Index2.54 (0.95)

This Compound (65.37)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (10.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (90.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]