Proteins > Gastrin/cholecystokinin type B receptor
Page last updated: 2024-08-07 16:29:56
Gastrin/cholecystokinin type B receptor
A cholecystokinin receptor 2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P32239]
Synonyms
CCK-B receptor;
CCK-BR;
Cholecystokinin-2 receptor;
CCK2-R
Research
Bioassay Publications (48)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 24 (50.00) | 18.2507 |
| 2000's | 16 (33.33) | 29.6817 |
| 2010's | 6 (12.50) | 24.3611 |
| 2020's | 2 (4.17) | 2.80 |
Compounds (26)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.Journal of medicinal chemistry, , Oct-05, Volume: 43, Issue:20, 2000
Synthesis and biological properties of new constrained CCK-B antagonists: discrimination of two affinity states of the CCK-B receptor on transfected CHO cells.Journal of medicinal chemistry, , Nov-21, Volume: 40, Issue:24, 1997
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.Journal of medicinal chemistry, , Aug-18, Volume: 38, Issue:17, 1995
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
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.Journal of medicinal chemistry, , Oct-05, Volume: 43, Issue:20, 2000
Receptor-Ligand Interaction Measured by Inductively Coupled Plasma Mass Spectrometry and Selenium Labeling.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Replacement of glycine with dicarbonyl and related moieties in analogues of the C-terminal pentapeptide of cholecystokinin: CCK(2) agonists displaying a novel binding mode.Journal of medicinal chemistry, , Oct-05, Volume: 43, Issue:20, 2000
Structure-based design of new constrained cyclic agonists of the cholecystokinin CCK-B receptor.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
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
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.Journal of medicinal chemistry, , Oct-05, Volume: 43, Issue:20, 2000
Recent natural products based drug development: a pharmaceutical industry perspective.Journal of natural products, , Volume: 61, Issue:8, 1998
Synthesis and biological properties of new constrained CCK-B antagonists: discrimination of two affinity states of the CCK-B receptor on transfected CHO cells.Journal of medicinal chemistry, , Nov-21, Volume: 40, Issue:24, 1997
5-(Piperidin-2-yl)- and 5-(homopiperidin-2-yl)-1,4-benzodiazepines: high-affinity, basic ligands for the cholecystokinin-B receptor.Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
Controlled modification of acidity in cholecystokinin B receptor antagonists: N-(1,4-benzodiazepin-3-yl)-N'-[3-(tetrazol-5-ylamino) phenyl]ureas.Journal of medicinal chemistry, , Feb-16, Volume: 39, Issue:4, 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
5-Phenyl-3-ureidobenzazepin-2-ones as cholecystokinin-B receptor antagonists.Journal of medicinal chemistry, , Oct-28, Volume: 37, Issue:22, 1994
High-affinity and potent, water-soluble 5-amino-1,4-benzodiazepine CCKB/gastrin receptor antagonists containing a cationic solubilizing group.Journal of medicinal chemistry, , Mar-18, Volume: 37, Issue:6, 1994
Development of 1,4-benzodiazepine cholecystokinin type B antagonists.Journal of medicinal chemistry, , Dec-24, Volume: 36, Issue:26, 1993
Excursions in drug discovery.Journal of medicinal chemistry, , Jul-23, Volume: 36, Issue:15, 1993
Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
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
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
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.Journal of natural products, , Volume: 69, Issue:3, 2006
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
Replacement of glycine with dicarbonyl and related moieties in analogues of the C-terminal pentapeptide of cholecystokinin: CCK(2) agonists displaying a novel binding mode.Journal of medicinal chemistry, , Oct-05, Volume: 43, Issue:20, 2000
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
Structure-based design of new constrained cyclic agonists of the cholecystokinin CCK-B receptor.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
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
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-[2-(N-phenylacetamide)]-1,5-benzodiazepines: orally active, binding selective CCK-A agonists.Journal of medicinal chemistry, , Jul-19, Volume: 39, Issue:15, 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
Development of CCK-tetrapeptide analogues as potent and selective CCK-A receptor agonists.Journal of medicinal chemistry, , Volume: 33, Issue:11, 1990
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
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Replacement of glycine with dicarbonyl and related moieties in analogues of the C-terminal pentapeptide of cholecystokinin: CCK(2) agonists displaying a novel binding mode.Journal of medicinal chemistry, , Oct-05, Volume: 43, Issue:20, 2000
Development of potent and selective CCK-A receptor agonists from Boc-CCK-4: tetrapeptides containing Lys(N epsilon)-amide residues.Journal of medicinal chemistry, , May-29, Volume: 35, Issue:11, 1992
trans-3-n-propyl-L-proline is a highly favorable, conformationally restricted replacement for methionine in the C-terminal tetrapeptide of cholecystokinin. Stereoselective synthesis of 3-allyl- and 3-n-propyl-L-proline derivatives from 4-hydroxy-L-prolineJournal of medicinal chemistry, , Volume: 34, Issue:1, 1991
Development of CCK-tetrapeptide analogues as potent and selective CCK-A receptor agonists.Journal of medicinal chemistry, , Volume: 33, Issue:11, 1990
Enables
This protein enables 6 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] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| gastrin receptor activity | molecular function | Combining with gastrin and transmitting the signal across the membrane by activating an associated G-protein to initiate a change in cell activity. [GOC:ai, GOC:signaling] |
| peptide hormone binding | molecular function | Binding to a peptide with hormonal activity in animals. [GOC:jl, ISBN:0198506732] |
| type B gastrin/cholecystokinin receptor binding | molecular function | Binding to a type B gastrin/cholecystokinin receptor. [GOC:mah, GOC:nln] |
| 1-phosphatidylinositol-3-kinase regulator activity | molecular function | Modulates the activity of the enzyme 1-phosphatidylinositol-3-kinase activity. [GOC:ai] |
Located In
This protein is located in 2 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] |
| intracellular membrane-bounded organelle | cellular component | Organized structure of distinctive morphology and function, bounded by a single or double lipid bilayer membrane and occurring within the cell. Includes the nucleus, mitochondria, plastids, vacuoles, and vesicles. Excludes the plasma membrane. [GOC:go_curators] |
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 9 target(s):
| Target | Category | Definition |
|---|
| gastric acid secretion | biological process | The regulated release of gastric acid (hydrochloric acid) by parietal or oxyntic cells during digestion. [GOC:hjd] |
| cell surface receptor signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor located on the cell surface. The pathway ends with regulation of a downstream cellular process, e.g. transcription. [GOC:signaling] |
| 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] |
| positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| 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] |
| pH reduction | biological process | Any process that reduces the internal pH of an organism, part of an organism or a cell, measured by the concentration of the hydrogen ion. [GOC:go_curators] |
| digestive tract development | biological process | The process whose specific outcome is the progression of the digestive tract over time, from its formation to the mature structure. The digestive tract is the anatomical structure through which food passes and is processed. [GOC:go_curators] |
| gland development | biological process | The process whose specific outcome is the progression of a gland over time, from its formation to the mature structure. A gland is an organ specialised for secretion. [GOC:jid] |