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Target Report Card

Target Name and Classification

Target ID CHEMBL1878
Target Type SINGLE PROTEIN
Preferred Name Calcium sensing receptor
Synonyms CASR | CaR | CaSR | Extracellular calcium-sensing receptor | PCAR1 | PCaR1 | Parathyroid cell calcium-sensing receptor 1 | Synonyms=GPRC2A | hCasR
Organism Homo sapiens
Species Group No
Protein Target Classification
  • membrane receptor > family c g protein-coupled receptor > ion receptor (family c gpcr) > calcium sensing receptor > calcium sensing receptor

Target Components

Component Description Relationship Accession
Extracellular calcium-sensing receptor SINGLE PROTEIN P41180

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1200776 CINACALCET HYDROCHLORIDE Calcium sensing receptor positive allosteric modulator 4 DailyMed
CHEMBL3545184 VELCALCETIDE Calcium sensing receptor agonist 4 PubMed
CHEMBL1198855 RONACALERET Calcium sensing receptor antagonist 2 PubMed
CHEMBL2107572 TECALCET HYDROCHLORIDE Calcium sensing receptor modulator 2 PubMed PubMed PubMed
CHEMBL3545100 ASP7991 Calcium sensing receptor positive allosteric modulator 2 Other

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000036828
Ensembl ENSG00000036828
GO Cellular Component GO:0005634 (nucleus)
GO:0005737 (cytoplasm)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0009986 (cell surface)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0016323 (basolateral plasma membrane)
GO:0016324 (apical plasma membrane)
GO:0030424 (axon)
GO:0043005 (neuron projection)
GO:0043025 (neuronal cell body)
GO:0043679 (axon terminus)
GO Molecular Function GO:0000287 (magnesium ion binding)
GO:0004435 (phosphatidylinositol phospholipase C activity)
GO:0004871 (signal transducer activity)
GO:0004930 (G-protein coupled receptor activity)
GO:0005178 (integrin binding)
GO:0005509 (calcium ion binding)
GO:0005515 (protein binding)
GO:0008144 (drug binding)
GO:0016597 (amino acid binding)
GO:0019808 (polyamine binding)
GO:0019901 (protein kinase binding)
GO:0042803 (protein homodimerization activity)
GO:0044325 (ion channel binding)
GO:0046872 (metal ion binding)
GO Biological Process GO:0001503 (ossification)
GO:0002931 (response to ischemia)
GO:0005513 (detection of calcium ion)
GO:0006816 (calcium ion transport)
GO:0006874 (cellular calcium ion homeostasis)
GO:0006915 (apoptotic process)
GO:0007165 (signal transduction)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007193 (adenylate cyclase-inhibiting G-protein coupled receptor signaling pathway)
GO:0007200 (phospholipase C-activating G-protein coupled receptor signaling pathway)
GO:0007254 (JNK cascade)
GO:0007635 (chemosensory behavior)
GO:0008284 (positive regulation of cell proliferation)
GO:0009653 (anatomical structure morphogenesis)
GO:0010038 (response to metal ion)
GO:0010628 (positive regulation of gene expression)
GO:0014070 (response to organic cyclic compound)
GO:0032024 (positive regulation of insulin secretion)
GO:0032781 (positive regulation of ATPase activity)
GO:0035729 (cellular response to hepatocyte growth factor stimulus)
GO:0042311 (vasodilation)
GO:0045907 (positive regulation of vasoconstriction)
GO:0048754 (branching morphogenesis of an epithelial tube)
GO:0050927 (positive regulation of positive chemotaxis)
GO:0051592 (response to calcium ion)
GO:0051924 (regulation of calcium ion transport)
GO:0060613 (fat pad development)
GO:0070509 (calcium ion import)
GO:0071305 (cellular response to vitamin D)
GO:0071333 (cellular response to glucose stimulus)
GO:0071404 (cellular response to low-density lipoprotein particle stimulus)
GO:0071456 (cellular response to hypoxia)
GO:0071774 (response to fibroblast growth factor)
GO:0090280 (positive regulation of calcium ion import)
GO:1901653 (cellular response to peptide)
Wikipedia Calcium-sensing_receptor

Target Cross References - Protein

canSAR P41180
CGD Hyperparathyroidism, neonatal; Hypocalcemia, autosomal dominant; Hypocalcemia, autosomal dominant, with Bartter syndrome; Hypocalciuric hypercalcemia, type I; Hyperparathyroidism, neonatal severe primary; Hypoparathyroidism, familial isolated; Hyperparathyroidism, familial primary
Human Protein Atlas ENSG00000036828
IntAct P41180
Guide to Pharmacology 54
Open Targets ENSG00000036828
PharmGKB PA26097
Pharos P41180 (Tclin)
Reactome R-HSA-416476 (G alpha (q) signalling events.)
R-HSA-418594 (G alpha (i) signalling events.)
R-HSA-420499 (Class C/3 (Metabotropic glutamate/pheromone receptors).)
UniProt P41180 Q13912 Q16108 Q16109 Q16110 Q16379 Q2M1T0 Q4PJ19

Target Cross References - Domain

InterPro IPR000337 (GPCR_3.)
IPR001828 (ANF_lig-bd_rcpt.)
IPR011500 (GPCR_3_9-Cys_dom.)
IPR017978 (GPCR_3_C.)
IPR017979 (GPCR_3_CS.)
IPR028082 (Peripla_BP_I.)
Pfam PF00003 (7tm_3)
PF01094 (ANF_receptor)
PF07562 (NCD3G)

Target Cross References - Structure

PDBe 5FBH 5FBK 5K5S 5K5T
CREDO 5FBH 5FBK 5K5S 5K5T
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