Proteins > Cholecystokinin receptor type A
Page last updated: 2024-08-07 16:29:49
Cholecystokinin receptor type A
A cholecystokinin receptor 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P32238]
Synonyms
CCK-A receptor;
CCK-AR;
Cholecystokinin-1 receptor;
CCK1-R
Research
Bioassay Publications (28)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 12 (42.86) | 18.2507 |
| 2000's | 11 (39.29) | 29.6817 |
| 2010's | 5 (17.86) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (19)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
SAR studies of 1,5-diarylpyrazole-based CCK1 receptor antagonists.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 17, Issue:23, 2007
Novel, achiral 1,3,4-benzotriazepine analogues of 1,4-benzodiazepine-based CCK(2) antagonists that display high selectivity over CCK(1) receptors.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Recent natural products based drug development: a pharmaceutical industry perspective.Journal of natural products, , Volume: 61, Issue:8, 1998
Excursions in drug discovery.Journal of medicinal chemistry, , Jul-23, Volume: 36, Issue:15, 1993
Novel, achiral 1,3,4-benzotriazepine analogues of 1,4-benzodiazepine-based CCK(2) antagonists that display high selectivity over CCK(1) receptors.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
CCK-A receptor selective antagonists derived from the CCK-A receptor selective tetrapeptide agonist Boc-Trp-Lys(Tac)-Asp-MePhe-NH2 (A-71623).Journal of medicinal chemistry, , Jan-06, Volume: 38, Issue:1, 1995
Structure-Activity Relationships and Characterization of Highly Selective, Long-Acting, Peptide-Based Cholecystokinin 1 Receptor Agonists.Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.Journal of medicinal chemistry, , May-18, Volume: 49, Issue:10, 2006
A peptide agonist acts by occupation of a monomeric G protein-coupled receptor: dual sites of covalent attachment to domains near TM1 and TM7 of the same molecule make biologically significant domain-swapped dimerization unlikely.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.Journal of medicinal chemistry, , Aug-15, Volume: 40, Issue:17, 1997
3-[2-(N-phenylacetamide)]-1,5-benzodiazepines: orally active, binding selective CCK-A agonists.Journal of medicinal chemistry, , Jul-19, Volume: 39, Issue:15, 1996
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.Journal of medicinal chemistry, , Dec-20, Volume: 39, Issue:26, 1996
3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines: CCK-A agonists that demonstrate oral activity as satiety agents.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist "trigger".Journal of medicinal chemistry, , Jan-19, Volume: 39, Issue:2, 1996
CCK-A receptor selective antagonists derived from the CCK-A receptor selective tetrapeptide agonist Boc-Trp-Lys(Tac)-Asp-MePhe-NH2 (A-71623).Journal of medicinal chemistry, , Jan-06, Volume: 38, Issue:1, 1995
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.Journal of medicinal chemistry, , Aug-18, Volume: 38, Issue:17, 1995
Achiral, selective CCK2 receptor antagonists based on a 1,3,5-benzotriazepine-2,4-dione template.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion.Journal of medicinal chemistry, , Jun-28, Volume: 50, Issue:13, 2007
Novel, achiral 1,3,4-benzotriazepine analogues of 1,4-benzodiazepine-based CCK(2) antagonists that display high selectivity over CCK(1) receptors.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| cholecystokinin receptor activity | molecular function | Combining with cholecystokinin and transmitting the signal across the membrane by activating an associated G-protein to initiate a change in cell activity. Cholecystokinin can act as a neuropeptide or as a gastrointestinal hormone. [GOC:signaling, PMID:9835394] |
| peptide hormone binding | molecular function | Binding to a peptide with hormonal activity in animals. [GOC:jl, ISBN:0198506732] |
| peptide binding | molecular function | Binding to a peptide, an organic compound comprising two or more amino acids linked by peptide bonds. [GOC:jl] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 8 target(s):
| Target | Category | Definition |
|---|
| neuron migration | biological process | The characteristic movement of an immature neuron from germinal zones to specific positions where they will reside as they mature. [CL:0000540, GOC:go_curators] |
| phospholipase C-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| axonogenesis | biological process | De novo generation of a long process of a neuron, including the terminal branched region. Refers to the morphogenesis or creation of shape or form of the developing axon, which carries efferent (outgoing) action potentials from the cell body towards target cells. [GOC:dph, GOC:jid, GOC:pg, GOC:pr, ISBN:0198506732] |
| forebrain development | biological process | The process whose specific outcome is the progression of the forebrain over time, from its formation to the mature structure. The forebrain is the anterior of the three primary divisions of the developing chordate brain or the corresponding part of the adult brain (in vertebrates, includes especially the cerebral hemispheres, the thalamus, and the hypothalamus and especially in higher vertebrates is the main control center for sensory and associative information processing, visceral functions, and voluntary motor functions). [http://www2.merriam-webster.com/cgi-bin/mwmednlm?book=Medical&va=forebrain] |
| cholecystokinin signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by cholecystokinin binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:jc, PMID:11181948] |
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
| cellular response to hormone stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a hormone stimulus. [GOC:mah] |
| regulation of hormone secretion | biological process | Any process that modulates the frequency, rate or extent of the regulated release of a hormone from a cell. [GOC:ai] |