Gastrin/cholecystokinin type B 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
- 6
- Compounds
- 6
- 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.
Gastrin/cholecystokinin type B receptor
Receptor for the peptide hormones gastrin and cholecystokinin (CCK). Expressed throughout the central nervous system, where it modulates processes such as anxiety, analgesia, arousal and neuroleptic activity. Couples to both GNAI1 and GNAQ signaling pathways, but not to GNAS34556863. Upon gastrin activation, reduces glucose absorption in intestinal epithelial cells by downregulating SGLT1 and GLUT2 expression through suppression of the PI3K/Akt/eIF4B pathway (By similarity). In the kidney, decreases SGLT2 expression under high-glucose conditions via ERK/NF-kappa-B signaling (By similarity)
Isoform 2 is constitutively activated and may regulate cancer cell proliferation via a gastrin-independent mechanism
Quoted from UniProt’s FUNCTION annotation for P32239 (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
- Vesicles
- Plasma membraneadditional
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 5 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.
- Parietal cells83.1 nCPM
- Granulosa cells72.2 nCPM
- Gastric chief cells53.5 nCPM
- Mucous neck cells45.8 nCPM
- Neuroendocrine cells32.3 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.
- stomach 141.3 nTPM
- pancreas25.5 nTPM
- brain21.1 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: midbrain 1.1, pituitary gland 0.8, 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 CCKBR 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 · 9
- cerebral cortex21.1 nTPM
- cerebellum16.4 nTPM
- amygdala9.7 nTPM
- basal ganglia4.9 nTPM
- hippocampal formation4.6 nTPM
- hypothalamus1.3 nTPM
- midbrain1.1 nTPM
- pituitary gland0.8 nTPM
- spinal cord0.6 nTPM
Peripheral and autonomic · 6
- stomach 141.3 nTPM
- pancreas25.5 nTPM
- duodenum0.2 nTPM
- thyroid gland0.2 nTPM
- colon0.1 nTPM
- adrenal gland0.1 nTPM
Transcript is not protein. These are RNA levels for CCKBR, 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 6
IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Gastrin/cholecystokinin type B receptor | Other named receptors | IC50 | 17,000 | 4.77 | Mus musculus | CHEMBL652241 |
| Gastrin/cholecystokinin type B receptor | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291758 |
| Gastrin/cholecystokinin type B receptor | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291758 |
| Gastrin/cholecystokinin type B receptor | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291758 |
| Gastrin/cholecystokinin type B receptor | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291758 |
| Gastrin/cholecystokinin type B receptor | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291758 |