An extracellular calcium-sensing receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:P41180]
New aminopropandiol derivatives as orally available and short-acting calcium-sensing receptor antagonists.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 20, Issue:12, 2010
Emerging targets in osteoporosis disease modification.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
Antagonists of the calcium receptor. 2. Amino alcohol-based parathyroid hormone secretagogues.Journal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 2009
The discovery of novel calcium sensing receptor negative allosteric modulators.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 19, Issue:12, 2009
Design, new synthesis, and calcilytic activity of substituted 3H-pyrimidin-4-ones.Bioorganic & medicinal chemistry letters, , May-16, Volume: 15, Issue:10, 2005
3H-Quinazolin-4-ones as a new calcilytic template for the potential treatment of osteoporosis.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 15, Issue:6, 2005
Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 15, Issue:24, 2005
| Target | Category | Definition |
|---|
| 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] |
| G protein-coupled receptor activity | molecular function | Combining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR] |
| integrin binding | molecular function | Binding to an integrin. [GOC:ceb] |
| calcium ion binding | molecular function | Binding to a calcium ion (Ca2+). [GOC:ai] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| amino acid binding | molecular function | Binding to an amino acid, organic acids containing one or more amino substituents. [GOC:ai] |
| protein kinase binding | molecular function | Binding to a protein kinase, any enzyme that catalyzes the transfer of a phosphate group, usually from ATP, to a protein substrate. [GOC:jl] |
| protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
| transmembrane transporter binding | molecular function | Binding to a transmembrane transporter, a protein or protein complex that enables the transfer of a substance, usually a specific substance or a group of related substances, from one side of a membrane to the other. [GOC:BHF, GOC:jl, PMID:33199372] |
| Target | Category | Definition |
|---|
| ossification | biological process | The formation of bone or of a bony substance, or the conversion of fibrous tissue or of cartilage into bone or a bony substance. [GOC:mtg_mpo, PMID:17572649] |
| response to ischemia | biological process | Any process that results in a change in state or activity of an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a inadequate blood supply. [GOC:hjd] |
| detection of calcium ion | biological process | The series of events in which a calcium ion stimulus is received by a cell and converted into a molecular signal. [GOC:pg] |
| intracellular calcium ion homeostasis | biological process | A homeostatic process involved in the maintenance of a steady state level of calcium ions within a cell. [GOC:ceb, GOC:mah] |
| 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] |
| adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the inhibition of adenylyl cyclase activity and a subsequent decrease in the intracellular concentration of cyclic AMP (cAMP). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| 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] |
| JNK cascade | biological process | A MAPK cascade containing at least the JNK (MAPK8) MAP kinase. It starts with the activation of JUN3K (a MAPK3K), which activates JNKK a MAP2K), which in turn activates JNK. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinases in the downstream tier. The JNK cascade is activated by stress signals, as well as by G protein-coupled receptors, growth factors, and cytokines, and results in cellular responses such as cell proliferation, cell differentiation, apoptosis and inflammation. [PMID:11790549, PMID:20811974, PMID:23125017] |
| chemosensory behavior | biological process | Behavior that is dependent upon the sensation of chemicals. [GOC:go_curators] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| anatomical structure morphogenesis | biological process | The process in which anatomical structures are generated and organized. Morphogenesis pertains to the creation of form. [GOC:go_curators, ISBN:0521436125] |
| positive regulation of gene expression | biological process | Any process that increases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
| positive regulation of insulin secretion | biological process | Any process that activates or increases the frequency, rate or extent of the regulated release of insulin. [GOC:mah] |
| bile acid secretion | biological process | The regulated release of bile acid, composed of any of a group of steroid carboxylic acids occurring in bile, by a cell or a tissue. [GOC:ecd] |
| cellular response to hepatocyte growth factor 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 hepatocyte growth factor stimulus. [GOC:bf] |
| 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] |
| positive regulation of vasoconstriction | biological process | Any process that activates or increases the frequency, rate or extent of vasoconstriction. [GOC:go_curators] |
| branching morphogenesis of an epithelial tube | biological process | The process in which the anatomical structures of branches in an epithelial tube are generated and organized. A tube is a long hollow cylinder. [GOC:dgh, GOC:dph, GOC:jid] |
| positive regulation of positive chemotaxis | biological process | Any process that activates or increases the frequency, rate or extent of the directed movement of a motile cell or organism towards a higher concentration in a concentration gradient of a specific chemical. [GOC:ai] |
| fat pad development | biological process | The progression of a fat pad from its initial formation to its mature structure. A fat pad is an accumulation of adipose tissue. [GOC:dph] |
| positive regulation of ERK1 and ERK2 cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:mah] |
| calcium ion import | biological process | The directed movement of calcium ions into a cell or organelle. [GOC:mah] |
| cellular response to vitamin D | 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 vitamin D stimulus. [GOC:mah] |
| cellular response to glucose 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 glucose stimulus. [GOC:mah] |
| cellular response to low-density lipoprotein particle 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 low-density lipoprotein particle stimulus. [GOC:mah] |
| cellular response to hypoxia | 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 stimulus indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:mah] |
| response to fibroblast growth factor | 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 fibroblast growth factor stimulus. [GOC:mah] |
| positive regulation of calcium ion import | biological process | Any process that increases the rate, frequency, or extent of the directed movement of calcium ions into a cell or organelle. [GOC:BHF] |
| cellular response to peptide | 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 peptide stimulus. [GOC:pr, GOC:TermGenie] |
| chloride transmembrane transport | biological process | The process in which chloride is transported across a membrane. [GOC:TermGenie, GOC:vw] |
| regulation of calcium ion transport | biological process | Any process that modulates the frequency, rate or extent of the directed movement of calcium ions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |