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Protein / target

Gastrin/cholecystokinin type B receptor

Encoded byCCKBRP32239Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
1
Approved medicines
Open Targets target-level
Small-molecule tractable
Druggability
Approved Drug
1
Research papers

Protein at a glance

Biological role

1-phosphatidylinositol-3-kinase regulator

Strongest disease association

Peptic ulcer disease

Via encoding gene CCKBR · Genetic evidence · score 0.49

Therapeutic position

Established drug target

Small molecules

Research activity

Emerging research

1 papers · latest 2025

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function overview

Receptor for the peptide hormones gastrin and cholecystokinin (CCK).

View complete UniProt function annotation

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 GNAS (PubMed:34556863). 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)

Subcellular location

Cell membrane
Domains and Gene Ontology detail (14)

Gene Ontology

  • Cplasma membrane
  • F1-phosphatidylinositol-3-kinase regulator activity
  • Fcholecystokinin receptor activity
  • Fgastrin receptor activity
  • Fneuropeptide receptor activity
  • Fpeptide hormone binding
  • Ftype B gastrin/cholecystokinin receptor binding
  • Pcell surface receptor signaling pathway
  • Pcholecystokinin signaling pathway
  • PG protein-coupled receptor signaling pathway
  • Pneuropeptide signaling pathway
  • Pphospholipase C-activating G protein-coupled receptor signaling pathway

447 aa · 48 kDa · 3 isoforms

Biological roles

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Cell proliferation & survivalGOG protein-coupled signallingGO
View supporting evidence

Cell proliferation & survival

  • ·positive regulation of cell population proliferation

G protein-coupled signalling

  • ·G protein-coupled receptor signaling pathway
  • ·phospholipase C-activating G protein-coupled receptor signaling pathway

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Strongest disease associations · via encoding gene CCKBR

Gene-level evidence surfaced through the gene CCKBRthat encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.

Gastroesophageal Reflux
0.67Moderately supported

Clinical evidence dominant · Open Targets 0.43

Peptic ulcer disease
0.49Limited support

Genetic evidence dominant · Open Targets 0.30

Duodenal ulcer
0.44Limited support

Genetic evidence dominant · Open Targets 0.26

Ovarian neoplasm
0.30Limited support

Genetic evidence dominant · Open Targets 0.18

Duodenal Diseases
0.23Preliminary

Genetic evidence dominant · Open Targets 0.14

View evidence synthesis (5)
Gastroesophageal RefluxModerately supported
0.67
agreement 0.560.78
Clinical53%Genetic45%Literature2%

Open Targets aggregate 0.43 · 3 independent evidence families

Peptic ulcer diseaseLimited support
0.49
agreement 0.350.63
Genetic99%Literature1%

Open Targets aggregate 0.30 · 2 independent evidence families

Duodenal ulcerLimited support
0.44
agreement 0.300.58
Genetic89%Literature11%

Open Targets aggregate 0.26 · 2 independent evidence families

Ovarian neoplasmLimited support
0.30
agreement 0.160.44
Genetic99%Literature1%

Open Targets aggregate 0.18 · 2 independent evidence families

Duodenal DiseasesPreliminary
0.23
agreement 0.110.35
Genetic100%

Open Targets aggregate 0.14 · 1 independent evidence family

The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the per-type scores above show the calculation.

Show all associations
Gastroesophageal Reflux0.43
Peptic ulcer disease0.30
Duodenal ulcer0.26
Ovarian neoplasm0.18
Duodenal Diseases0.14

Drug development

4 compounds recorded · 1 approved · 3 in clinical development

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines.

View all recorded compounds (4)
NETAZEPIDEPhase 2
CI-988Phase 2
ITRIGLUMIDEPhase 2
PROGLUMIDEApproval

Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.

Tractability

Small moleculesStrong

Approved Drug and High-Quality Ligand support this modality.

AntibodiesEmerging

Feasibility evidence (go cc high conf and uniprot loc med conf) — no clinical-stage drug of this modality recorded.

Protein degradersEmerging

Feasibility evidence (small molecule binder) — no clinical-stage drug of this modality recorded.

Other modalitiesStrong

Advanced Clinical support this modality.

View underlying tractability evidence (8)
SM · Approved DrugSM · High-Quality LigandSM · Druggable FamilyAB · GO CC high confAB · UniProt loc med confAB · UniProt SigP or TMHMMPR · Small Molecule BinderOC · Advanced Clinical

Raw Open Targets tractability assessment buckets, by modality.

Safety-related annotations

higher incidence of diarrhoeaBrennan et al. (2024)dyspepsiaBrennan et al. (2024)nauseaBrennan et al. (2024)HypergastrinaemiaBrennan et al. (2024)flatulenceBrennan et al. (2024)anxietyBrennan et al. (2024)increased gastric pH due to suppression of gastric acid secretionBrennan et al. (2024)

Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.

Research activity

1 papers · to 2025

Papers linked directly to this protein. This is the protein's own literature — descriptor-derived papers are kept separate below.

Most cited

Recent

Europe PMC papers linked directly to this protein.