Endothelin-1 receptor
A named receptor outside the families above. The catch-all is explicit rather than silent: these are receptors, but they are not grouped.
- Measurements
- 24
- Compounds
- 12
- Binding constants
- 7
- Median pX
- —
I · Identity
What this target is
Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.
Endothelin-1 receptor
Receptor for endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of binding affinities for ET-A is: ET1 > ET2 >> ET3
Quoted from UniProt’s FUNCTION annotation for P25101 (reviewed).
What it acts with
STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.
Where it sits in the cell
- Plasma membrane
- Cytosol
Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.
UniProt, curated Cell membrane
Expression by cell type
Single cell type RNA, the 10 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.
- Vascular smooth muscle cells302.2 nCPM
- Pericytes260.6 nCPM
- Endometrial stromal cells191.7 nCPM
- Peritubular myoid cells161.1 nCPM
- Decidual stromal cells133.8 nCPM
- Leydig cells127 nCPM
- Ovarian stromal cells112.2 nCPM
- Cardiomyocytes83.6 nCPM
- Smooth muscle cells81.2 nCPM
- Respiratory ionocytes55.9 nCPM
Expression by tissue
The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.
- seminal vesicle107.2 nTPM
II · Anatomy
Where the gene is transcribed
The same two atlases the compound plates use, asked about this gene alone. Brain on the left, peripheral and autonomic tissues on the right.
Brain
basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.
Measured but not drawn — this anatomogram has no outline for them: pituitary gland 2.7, midbrain 2.4, spinal cord 1.4, retina 0.3.
Body
Square-root ramp · shared scale across both plates
Shading is transcript level — not affinity, and not affinity combined with expression. Outlined but unshaded organs hold none of EDNRA transcript above the atlas’s detection threshold. Anatomy from EMBL-EBI Anatomogram (Apache License 2.0); regions identified by Uberon (uberon.org), CC BY 3.0.
Brain · 10
- cerebral cortex2.9 nTPM
- pituitary gland2.7 nTPM
- midbrain2.4 nTPM
- basal ganglia2.1 nTPM
- hippocampal formation1.6 nTPM
- amygdala1.5 nTPM
- hypothalamus1.5 nTPM
- spinal cord1.4 nTPM
- cerebellum0.5 nTPM
- retina0.3 nTPM
Peripheral and autonomic · 16
- smooth muscle42.1 nTPM
- heart muscle24.4 nTPM
- lung21.4 nTPM
- urinary bladder11.9 nTPM
- spleen7.9 nTPM
- thyroid gland6.7 nTPM
- salivary gland6.2 nTPM
- stomach 15.2 nTPM
- adrenal gland5.2 nTPM
- kidney3.8 nTPM
- skeletal muscle3.7 nTPM
- duodenum3.2 nTPM
- colon3.0 nTPM
- liver2.9 nTPM
- small intestine2.7 nTPM
- pancreas1.1 nTPM
Transcript is not protein. These are RNA levels for EDNRA, shaded on √nTPM so that a three-order range stays legible — on a linear ramp every region but the strongest would read as blank, which looks like absence rather than less. A region carrying no shading is one the atlas reports no consensus value for, not one where the gene is silent. And a gene being transcribed somewhere is not evidence that any compound reaches it. Human Protein Atlas, RNA expression, nTPM (normalized transcripts per million), consensus tissue dataset.
IV · Evidence
Every measurement at this target
Each row links to the ChEMBL assay it came from.
Equilibrium binding constants 7
Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Endothelin-1 receptor | Other named receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909144 |
| Endothelin-1 receptor | Other named receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909144 |
| Endothelin-1 receptor | Other named receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909144 |
| Endothelin-1 receptor | Other named receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909144 |
| Endothelin-1 receptor | Other named receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909144 |
| Endothelin-1 receptor | Other named receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909144 |
| Endothelin-1 receptor | Other named receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909144 |
Functional readouts 15
IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Endothelin-1 receptor | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291785 |
| Endothelin-1 receptor | Other named receptors | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909144 |
| Endothelin-1 receptor | Other named receptors | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909144 |
| Endothelin-1 receptor | Other named receptors | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909144 |
| Endothelin-1 receptor | Other named receptors | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909144 |
| Endothelin-1 receptor | Other named receptors | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909144 |
| Endothelin-1 receptor | Other named receptors | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909144 |
| Endothelin-1 receptor | Other named receptors | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909144 |
| Endothelin-1 receptor | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291785 |
| Endothelin-1 receptor | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291785 |
| Endothelin-1 receptor | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291785 |
| Endothelin-1 receptor | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291785 |
| Endothelin-1 receptor | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291785 |
| Endothelin-1 receptor | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291785 |
| Endothelin-1 receptor | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291785 |
Other measurements 2
Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Endothelin-1 receptor | Other named receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1101407 |
| Endothelin-1 receptor | Other named receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1101406 |