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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 | CaSR | Extracellular calcium-sensing receptor | GPRC2A | PCAR1 | PCaR1 | Parathyroid cell calcium-sensing receptor 1
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:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO Molecular Function GO:0004435 (phosphatidylinositol phospholipase C activity)
GO:0004871 (signal transducer activity)
GO:0004930 (G-protein coupled receptor activity)
GO:0005515 (protein binding)
GO Biological Process GO:0001503 (ossification)
GO:0005513 (detection of calcium ion)
GO:0006874 (cellular calcium ion homeostasis)
GO:0007165 (signal transduction)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007635 (chemosensory behavior)
GO:0009653 (anatomical structure morphogenesis)
GO:0070509 (calcium ion import)
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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