Page last updated: 2024-08-07 16:24:56
B2 bradykinin receptor
A B2 bradykinin receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P30411]
Synonyms
B2R;
BK-2 receptor
Research
Bioassay Publications (23)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 1 (4.35) | 18.7374 |
1990's | 7 (30.43) | 18.2507 |
2000's | 8 (34.78) | 29.6817 |
2010's | 6 (26.09) | 24.3611 |
2020's | 1 (4.35) | 2.80 |
Compounds (13)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
bradykinin | Homo sapiens (human) | EC50 | 0.0000 | 1 | 1 |
icatibant | Homo sapiens (human) | Kd | 0.0003 | 1 | 1 |
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
bradykinin | Homo sapiens (human) | ED50 | 0.0016 | 1 | 1 |
bradykinin | Homo sapiens (human) | pD | 8,780,000.0000 | 1 | 1 |
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
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
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
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
Synthesis and biological evaluation of bradykinin B(1)/B(2) and selective B(1) receptor antagonists.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
Synthesis and characterization of bradykinin B(2) receptor agonists containing constrained dipeptide mimics.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Design and synthesis of potent bradykinin agonists containing a benzothiazepine moiety.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Bradykinin receptor antagonists containing N-substituted amino acids: in vitro and in vivo B(2) and B(1) receptor antagonist activity.Journal of medicinal chemistry, , Mar-29, Volume: 39, Issue:7, 1996
Biological activities of photoaffinity labeling analogues of kinins and their irreversible effects on kinin receptors.Journal of medicinal chemistry, , Volume: 24, Issue:12, 1981
Novel small molecule bradykinin B2 receptor antagonists.Journal of medicinal chemistry, , Jul-23, Volume: 52, Issue:14, 2009
A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 3. Discovering bioisosteres of the imidazo[1,2-a] pyridine moiety.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 4. Discovery of novel frameworks mimicking the active conformation.Journal of medicinal chemistry, , Nov-05, Volume: 41, Issue:23, 1998
Potent antiproliferative activity of bradykinin B2 receptor selective agonist FR-190997 and analogue structures thereof: A paradox resolved?European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Discovery of the first non-peptide full agonists for the human bradykinin B(2) receptor incorporating 4-(2-picolyloxy)quinoline and 1-(2-picolyl)benzimidazole frameworks.Journal of medicinal chemistry, , May-20, Volume: 47, Issue:11, 2004
Bradykinin antagonists modified with dipeptide mimetic beta-turn inducers.Bioorganic & medicinal chemistry letters, , May-01, Volume: 16, Issue:9, 2006
A new series of highly potent non-peptide bradykinin B2 receptor antagonists incorporating the 4-heteroarylquinoline framework. Improvement of aqueous solubility and new insights into species difference.Journal of medicinal chemistry, , Mar-25, Volume: 47, Issue:7, 2004
Design and synthesis of potent bradykinin agonists containing a benzothiazepine moiety.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Synthesis and characterization of bradykinin B(2) receptor agonists containing constrained dipeptide mimics.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 2. Overcoming the species difference between guinea pig and man.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 3. Discovering bioisosteres of the imidazo[1,2-a] pyridine moiety.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
Bradykinin receptor antagonists containing N-substituted amino acids: in vitro and in vivo B(2) and B(1) receptor antagonist activity.Journal of medicinal chemistry, , Mar-29, Volume: 39, Issue:7, 1996
Enables
This protein enables 6 target(s):
Target | Category | Definition |
protease binding | molecular function | Binding to a protease or a peptidase. [GOC:hjd] |
phosphatidylinositol phospholipase C activity | molecular function | Catalysis of the reaction: 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate + H2O = 1,2-diacylglycerol + 1D-myo-inositol 1,4,5-trisphosphate + H+. [EC:3.1.4.11, RHEA:33179] |
bradykinin receptor activity | molecular function | Combining with bradykinin to initiate a change in cell activity. [GOC:ai] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
type 1 angiotensin receptor binding | molecular function | Binding to a type 1 angiotensin receptor. [GOC:mah, GOC:nln] |
protein heterodimerization activity | molecular function | Binding to a nonidentical protein to form a heterodimer. [GOC:ai] |
Located In
This protein is located in 4 target(s):
Target | Category | Definition |
endosome | cellular component | A vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797] |
Golgi apparatus | cellular component | A membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [ISBN:0198506732] |
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 16 target(s):
Target | Category | Definition |
smooth muscle contraction | biological process | A process in which force is generated within smooth muscle tissue, resulting in a change in muscle geometry. Force generation involves a chemo-mechanical energy conversion step that is carried out by the actin/myosin complex activity, which generates force through ATP hydrolysis. Smooth muscle differs from striated muscle in the much higher actin/myosin ratio, the absence of conspicuous sarcomeres and the ability to contract to a much smaller fraction of its resting length. [GOC:ef, GOC:jl, GOC:mtg_muscle, ISBN:0198506732] |
inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |
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] |
cell surface receptor protein tyrosine kinase signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor on the surface of the target cell where the receptor possesses tyrosine kinase activity, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb, GOC:signaling] |
positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
blood circulation | biological process | The flow of blood through the body of an animal, enabling the transport of nutrients to the tissues and the removal of waste products. [GOC:mtg_heart, ISBN:0192800825] |
response to salt stress | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating an increase or decrease in the concentration of salt (particularly but not exclusively sodium and chloride ions) in the environment. [GOC:jl] |
regulation of vasoconstriction | biological process | Any process that modulates the frequency, rate or extent of reductions in the diameter of blood vessels. [GOC:jl] |
negative regulation of peptidyl-serine phosphorylation | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the phosphorylation of peptidyl-serine. [GOC:mah] |
vasoconstriction | biological process | A decrease in the diameter of blood vessels, especially arteries, due to constriction of smooth muscle cells that line the vessels, and usually causing an increase in blood pressure. [GOC:pr, ISBN:0192800752] |
vasodilation | biological process | An increase in the internal diameter of blood vessels, especially arterioles or capillaries, due to relaxation of smooth muscle cells that line the vessels, and usually resulting in a decrease in blood pressure. [GOC:pr, ISBN:0192800981] |
regulation of vascular permeability | biological process | Any process that modulates the extent to which blood vessels can be pervaded by fluid. [GOC:jl] |
arachidonic acid secretion | biological process | The controlled release of arachidonic acid from a cell or a tissue. [GOC:ai] |
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stress by p53 class mediator | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of intrinsic apoptotic signaling pathway in response to osmotic stress by p53 class mediator. [GOC:krc, GOC:mtg_apoptosis, GOC:TermGenie, PMID:16571598] |
intrinsic apoptotic signaling pathway in response to osmotic stress by p53 class mediator | biological process | The series of molecular signals in which an intracellular signal is conveyed to trigger the apoptotic death of a cell. The pathway is induced by the cell cycle regulator phosphoprotein p53, or an equivalent protein, in response to the detection of osmotic stress, and ends when the execution phase of apoptosis is triggered. [GOC:krc, GOC:mtg_apoptosis, PMID:16571598] |
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] |