Corticotropin-releasing factor receptor 1
A named receptor outside the families above. The catch-all is explicit rather than silent: these are receptors, but they are not grouped.
- Measurements
- 5
- Compounds
- 5
- Binding constants
- 0
- 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.
Corticotropin-releasing hormone receptor 1
G protein-coupled receptor for CRH and UCN stress hormones, which plays a central role in whole body adaptation to stress18292205,18801728,20966082,23576434,23863939,24290358,32004469,32004470. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and downstream effectors, such as adenylate cyclase18292205,32004469,32004470. CRHR1 is mainly coupled to G(s) G protein (GNAS), mediating activation of adenylate cyclase activity and production of cAMP18292205,32004469,32004470. In some conditions, can also couple to G(q) G protein (GNAQ) and mediate production of diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3) second messengers14657255. CRHR1-dependent signaling is a primary mediator of the neuroendocrine, autonomic (fight-or-flight) and behavioral responses to stress, acting as a key regulator of adaptation by activating the hypothalamus-pituitary-adrenal axis, leading to corticotropin hormone (ACTH) production (By similarity). Mediates both anxiogenic and anxiolytic response to stress in glutamatergic and dopaminergic neurons, respectively (By similarity). CRHR1 also plays a critical role in addiction by mediating the brain's stress response, particularly during withdrawal and relapse: it drives the transition to compulsive drug seeking by increasing anxiety and negative emotional states (By similarity)
Does not bind to CRH with high affinity
Quoted from UniProt’s FUNCTION annotation for P34998 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.
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
UniProt, curated Cell membrane
Expression by cell type
Single cell type RNA, the 1 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.
- Brain excitatory neurons35.3 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.
- brain18.7 nTPM
- pituitary gland18.5 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 18.5, retina 1.4, midbrain 0.7, spinal cord 0.6.
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 CRHR1 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
- cerebellum18.7 nTPM
- pituitary gland18.5 nTPM
- cerebral cortex5.6 nTPM
- amygdala3.1 nTPM
- hippocampal formation1.9 nTPM
- retina1.4 nTPM
- hypothalamus1.3 nTPM
- basal ganglia0.9 nTPM
- midbrain0.7 nTPM
- spinal cord0.6 nTPM
Peripheral and autonomic · 5
- smooth muscle0.1 nTPM
- kidney0.1 nTPM
- thyroid gland0.1 nTPM
- skeletal muscle0.1 nTPM
- salivary gland0.1 nTPM
Transcript is not protein. These are RNA levels for CRHR1, 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.
Functional readouts 5
IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Corticotropin-releasing factor receptor 1 | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291775 |
| Corticotropin-releasing factor receptor 1 | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291775 |
| Corticotropin-releasing factor receptor 1 | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291775 |
| Corticotropin-releasing factor receptor 1 | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291775 |
| Corticotropin-releasing factor receptor 1 | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291775 |