endothelin (16-21): C-terminal hexapeptide of endothelin; amino acid seq. given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 129432 |
| CHEMBL ID | 34540 |
| CHEBI ID | 189233 |
| SCHEMBL ID | 7996606 |
| MeSH ID | M0170612 |
| Synonym |
|---|
| histidyl-leucyl-aspartyl-isoleucyl-isoleucyl-tryptophan |
| endothelin (16-21) |
| l-tryptophan, n-(n-(n-(n-(n-l-histidyl-l-leucyl)-l-alpha-aspartyl)-l-isoleucyl)-l-isoleucyl)- |
| et-(16-21) |
| CHEMBL34540 , |
| 3-{2-[2-amino-3-(1h-imidazol-4-yl)-propionylamino]-4-methyl-pentanoylamino}-n-(1-{1-[1-carboxy-2-(1h-indol-3-yl)-ethylcarbamoyl]-2-methyl-butylcarbamoyl}-2-methyl-butyl)-succinamic acid |
| bdbm50001216 |
| 3-{2-[2-amino-3-(3h-imidazol-4-yl)-propionylamino]-4-methyl-pentanoylamino}-n-(1-{1-[1-carboxy-2-(1h-indol-3-yl)-ethylcarbamoyl]-2-methyl-butylcarbamoyl}-2-methyl-butyl)-succinamic acid |
| bdbm50000565 |
| (s)-3-{(s)-2-[(s)-2-amino-3-(3h-imidazol-4-yl)-propionylamino]-4-methyl-pentanoylamino}-n-((s)-1-{(s)-1-[(s)-1-carboxy-2-(1h-indol-3-yl)-ethylcarbamoyl]-2-methyl-butylcarbamoyl}-2-methyl-butyl)-succinamic acid |
| CHEBI:189233 |
| his-leu-asp-ile-ile-trp |
| (3s)-3-[[(2s)-2-[[(2s)-2-amino-3-(1h-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-[[(2s,3s)-1-[[(2s,3s)-1-[[(1s)-1-carboxy-2-(1h-indol-3-yl)ethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-oxobutanoic acid |
| 121377-67-1 |
| SCHEMBL7996606 |
| n-[14-amino-2,5-di(butan-2-yl)-8-(carboxymethyl)-1,4,7,10,13-pentahydroxy-15-(1h-imidazol-5-yl)-11-(2-methylpropyl)-3,6,9,12-tetraazapentadeca-3,6,9,12-tetraen-1-ylidene]tryptophan |
| DTXSID40923789 |
| (2s,5s,8s,11s,14s,17s)-2-((1h-indol-3-yl)methyl)-17-amino-5,8-di-sec-butyl-11-(carboxymethyl)-18-(1h-imidazol-4-yl)-14-isobutyl-4,7,10,13,16-pentaoxo-3,6,9,12,15-pentaazaoctadecan-1-oic acid |
| h-his-leu-asp-ile-ile-trp-oh |
| Class | Description |
|---|---|
| peptide | Amide derived from two or more amino carboxylic acid molecules (the same or different) by formation of a covalent bond from the carbonyl carbon of one to the nitrogen atom of another with formal loss of water. The term is usually applied to structures formed from alpha-amino acids, but it includes those derived from any amino carboxylic acid. X = OH, OR, NH2, NHR, etc. |
| [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 | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Endothelin receptor type B | Rattus norvegicus (Norway rat) | IC50 (µMol) | 50.0000 | 0.0000 | 1.1744 | 4.4000 | AID66878 |
| Endothelin receptor type B | Homo sapiens (human) | IC50 (µMol) | 50.0000 | 0.0001 | 0.6565 | 9.8000 | AID66032 |
| Endothelin-1 receptor | Homo sapiens (human) | IC50 (µMol) | 50.0000 | 0.0000 | 0.7647 | 9.9000 | AID66032 |
| Endothelin-1 receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 44.0000 | 0.0000 | 1.7746 | 10.0000 | AID67050 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| endothelin receptor activity | Endothelin receptor type B | Homo sapiens (human) |
| protein binding | Endothelin receptor type B | Homo sapiens (human) |
| peptide hormone binding | Endothelin receptor type B | Homo sapiens (human) |
| type 1 angiotensin receptor binding | Endothelin receptor type B | Homo sapiens (human) |
| phosphatidylinositol phospholipase C activity | Endothelin-1 receptor | Homo sapiens (human) |
| endothelin receptor activity | Endothelin-1 receptor | Homo sapiens (human) |
| protein binding | Endothelin-1 receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Endothelin receptor type B | Homo sapiens (human) |
| nuclear membrane | Endothelin receptor type B | Homo sapiens (human) |
| plasma membrane | Endothelin receptor type B | Homo sapiens (human) |
| plasma membrane | Endothelin-1 receptor | Homo sapiens (human) |
| plasma membrane | Endothelin-1 receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID190017 | Antagonism of the endothelin stimulated accumulation of inositol phosphate (IP3) was determined in cultured rat skin fibroblasts | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Design of a functional hexapeptide antagonist of endothelin. |
| AID67050 | Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle. | 1992 | Journal of medicinal chemistry, May-01, Volume: 35, Issue:9 | Endothelin: a new challenge. |
| AID66032 | Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Design of a functional hexapeptide antagonist of endothelin. |
| AID228168 | Compound was evaluated for the Inositol phosphate accumulation in rat skin fibroblasts. | 1992 | Journal of medicinal chemistry, May-01, Volume: 35, Issue:9 | Endothelin: a new challenge. |
| AID66878 | Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranes | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Design of a functional hexapeptide antagonist of endothelin. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 1 (7.14) | 18.7374 |
| 1990's | 12 (85.71) | 18.2507 |
| 2000's | 1 (7.14) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
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.
| This Compound (12.83) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (13.33%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 13 (86.67%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||