Contents:
- Gene and Protein Information
- Previous and Unofficial Names
- Database Links
- Natural/Endogenous Ligands
- Rank order lists
- Agonists
- Antagonists
- Transduction Mechanisms
- Tissue Distribution
- Expression Datasets
- Functional Assays
- Physiological Functions
- Physiological Consequences of Altering Gene Expression
- Phenotypes, Alleles and Disease Models
- References
- Contributors
- How to cite this page
Gene and Protein Information  |
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| class A G protein-coupled receptor | ||||||
| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | 7 | 428 | 4p15.2 | CCKAR | cholecystokinin A receptor | 10,56 |
| Mouse | 7 | 436 | 5 29.52 cM | Cckar | cholecystokinin A receptor | 26,52 |
| Rat | 7 | 444 | 14q11 | Cckar | cholecystokinin A receptor | 51,59 |
| Previous and Unofficial Names |
| CCK1-R | cholecystokinin receptor type A | cholecystokinin-1 receptor |
| Database Links |
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| Specialist databases | |
| GPCRdb | cckar_human (Hs), cckar_mouse (Mm), cckar_rat (Rn) |
| Other databases | |
| Alphafold | P32238 (Hs), O08786 (Mm), P30551 (Rn) |
| CATH/Gene3D | 4.10.670.10 |
| ChEMBL Target | CHEMBL1901 (Hs), CHEMBL2798 (Mm), CHEMBL2871 (Rn) |
| DrugBank Target | P32238 (Hs) |
| Ensembl Gene | ENSG00000163394 (Hs), ENSMUSG00000029193 (Mm), ENSRNOG00000043124 (Rn) |
| Entrez Gene | 886 (Hs), 12425 (Mm), 24889 (Rn) |
| Human Protein Atlas | ENSG00000163394 (Hs) |
| KEGG Gene | hsa:886 (Hs), mmu:12425 (Mm), rno:24889 (Rn) |
| OMIM | 118444 (Hs) |
| Pharos | P32238 (Hs) |
| RefSeq Nucleotide | NM_000730 (Hs), NM_009827 (Mm), NM_012688 (Rn) |
| RefSeq Protein | NP_000721 (Hs), NP_033957 (Mm), NP_036820 (Rn) |
| UniProtKB | P32238 (Hs), O08786 (Mm), P30551 (Rn) |
| Wikipedia | CCKAR (Hs) |
| Natural/Endogenous Ligands |
| CCK-58 {Sp: Human} |
| CCK-39 {Sp: Human} |
| CCK-4 {Sp: Human} |
| CCK-33 {Sp: Human} |
| CCK-8 {Sp: Human, Mouse, Rat} |
| CCK-33 {Sp: Mouse} , CCK-33 {Sp: Rat} |
| gastrin-17 {Sp: Human} , gastrin-17 {Sp: Mouse} , gastrin-17 {Sp: Rat} |
| Comments: CCK-58 is an endogenous peptide fragment from the cholecystokinin precursor protein, but there is no affinity data available for this ligand at cholecystokinin receptors. For the rodent homologues of this peptide please see the following ligand entries: CCK-58 (mouse) and CCK-58 (rat). |
| Potency order of endogenous ligands (Human) |
| CCK-8 (CCK, P06307), CCK-58 (CCK, P06307), CCK-39 (CCK, P06307), CCK-33 (CCK, P06307) >> gastrin-17 (GAST, P01350), desulfated cholecystokinin-8 > CCK-4 (CCK, P06307) |
Download all structure-activity data for this target as a CSV file 
| Agonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| View species-specific agonist tables | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Agonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| pIC50 values represent inhibition of binding of [125I]CCK. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Antagonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| View species-specific antagonist tables | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Primary Transduction Mechanisms
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| Transducer | Effector/Response |
| Gq/G11 family | Phospholipase C stimulation |
| References: 10,56 | |
| Secondary Transduction Mechanisms |
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| Transducer | Effector/Response |
| Gs family | Adenylyl cyclase stimulation |
| References: 30 | |
| Tissue Distribution
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| Expression Datasets |
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| Physiological Functions
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| Phenotypes, Alleles and Disease Models
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References
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2. Aquino CJ, Armour DR, Berman JM, Birkemo LS, Carr RA, Croom DK, Dezube M, Dougherty RW, Ervin GN, Grizzle MK, Head JE, Hirst GC, James MK, Johnson MF, Miller LJ, Queen KL, Rimele TJ, Smith DN, Sugg EE. (1996) Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist "trigger". J Med Chem, 39: 562-569. [PMID:8558528]
3. Asin KE, Bednarz L, Nikkel AL, Gore Jr PA, Montana WE, Cullen MJ, Shiosaki K, Craig R, Nadzan AM. (1992) Behavioral effects of A71623, a highly selective CCK-A agonist tetrapeptide. Am J Physiol, 263 (1 Pt 2): R125-35. [PMID:1636779]
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How to cite this page
Beinfeld M, Chen Q, Gao F, Liddle RA, Miller LJ, Rehfeld J. Cholecystokinin receptors in GtoPdb v.2023.1. IUPHAR/BPS Guide to Pharmacology CITE. 2023; 2023(1). Available from: https://doi.org/10.2218/gtopdb/F15/2023.1.
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