General Information of the Protein
Protein ID
PT06044
Protein Name
Extracellular calcium-sensing receptor
Secondarily
Protein Name
Parathyroid cell calcium-sensing receptor
Gene Name
CASR
Secondarily
Gene Name
Gprc2a
Pcar1
Sequence
MASYSCCLALLALAWHSSAYGPDQRAQKKGDIILGGLFPIHFGVAAKDQDLKSRPESVECIRYNFRGFRWLQAMIFAIEEINSSPSLLPNMTLGYRIFDTCNTVSKALEATLSFVAQNKIDSLNLDEFCNCSEHIPSTIAVVGATGSGVSTAVANLLGLFYIPQVSYASSSRLLSNKNQYKSFLRTIPNDEHQATAMADIIEYFRWNWVGTIAADDDYGRPGIEKFREEAEERDICIDFSELISQYSDEEEIQQVVEVIQNSTAKVIVVFSSGPDLEPLIKEIVRRNITGRIWLASEAWASSSLIAMPEYFHVVGGTIGFGLKAGQIPGFREFLQKVHPRKSVHNGFAKEFWEETFNCHLQEGAKGPLPVDTFVRSHEEGGNRLLNSSTAFRPLCTGDENINSVETPYMDYEHLRISYNVYLAVYSIAHALQDIYTCLPGRGLFTNGSCADIKKVEAWQVLKHLRHLNFTNNMGEQVTFDECGDLVGNYSIINWHLSPEDGSIVFKEVGYYNVYAKKGERLFINEEKILWSGFSREVPFSNCSRDCQAGTRKGIIEGEPTCCFECVECPDGEYSGETDASACDKCPDDFWSNENHTSCIAKEIEFLAWTEPFGIALTLFAVLGIFLTAFVLGVFIKFRNTPIVKATNRELSYLLLFSLLCCFSSSLFFIGEPQDWTCRLRQPAFGISFVLCISCILVKTNRVLLVFEAKIPTSFHRKWWGLNLQFLLVFLCTFMQILICIIWLYTAPPSSYRNHELEDEIIFITCHEGSLMALGSLIGYTCLLAAICFFFAFKSRKLPENFNEAKFITFSMLIFFIVWISFIPAYASTYGKFVSAVEVIAILAASFGLLACIFFNKVYIILFKPSRNTIEEVRSSTAAHAFKVAARATLRRPNISRKRSSSLGGSTGSIPSSSISSKSNSEDRFPQPERQKQQQPLSLTQQEQQQQPLTLHPQQQQQPQQPRCKQKVIFGSGTVTFSLSFDEPQKNAMAHRNSMRQNSLEAQRSNDTLGRHQALLPLQCADADSEMTIQETGLQGPMVGDHQPEMESSDEMSPALVMSTSRSFVISGGGSSVTENVLHS
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Organism
Rattus norvegicus, Rat
Protein Classification
Membrane receptor
>
Family C G protein-coupled receptor
>
Ion receptor (family C GPCR)
>
Calcium sensing receptor
>
Calcium sensing receptor
Function
G-protein-coupled receptor that senses changes in the extracellular concentration of calcium ions and plays a key role in maintaining calcium homeostasis (PubMed:7816802). Senses fluctuations in the circulating calcium concentration and modulates the production of parathyroid hormone (PTH) in parathyroid glands (By similarity). The activity of this receptor is mediated by a G-protein that activates a phosphatidylinositol-calcium second messenger system (By similarity). The G-protein-coupled receptor activity is activated by a co-agonist mechanism: aromatic amino acids, such as Trp or Phe, act concertedly with divalent cations, such as calcium or magnesium, to achieve full receptor activation (By similarity).
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Uniprot ID
P48442
Ensembl ID
ENSG00000036828
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0856164
N-[(1S,2S)-2-((R)-1-naphthalen-1-yl-ethylamino)-cyclohexyl]-4-trifluoromethoxy-benzamide hydrochloride
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C26H28ClF3N2O2
 1
1
IC50 = 250 nM
   TI
   LI
   LO
   TS
CP0881777
3,4-dichloro-N-((1S,2S)-2-((R)-1-(naphthalen-1-yl)ethylamino)cyclohexyl)benzamide hydrochloride
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C25H27Cl3N2O
 1
1
IC50 = 330 nM
   TI
   LI
   LO
   TS
CP0172829
(R)-2-chloro-6-(2-hydroxy-3-(2-methyl-1-(naphthalen-2-yl)propan-2-ylamino)propoxy)benzonitrile
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C24H25ClN2O2
 1
1
IC50 = 460 nM
   TI
   LI
   LO
   TS
CP0886344
N1-[4-(trifluoromethoxy)benzoyl]-N2-[1-(1-naphthyl)ethyl]-trans-1,2-diaminocyclohexane hydrochloride
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C26H28ClF3N2O2
 1
1
IC50 = 900 nM
   TI
   LI
   LO
   TS
CP0856099
N-((1R,2R)-2-((R)-1-(naphthalen-1-yl)ethylamino)cyclohexyl)-4-(trifluoromethoxy)benzamide hydrochloride
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C26H28ClF3N2O2
 1
1
IC50 = 1700 nM
   TI
   LI
   LO
   TS
CP0886345
N-[(1S,2S)-2-((R)-1-naphthalen-1-yl-ethylamino)-cyclohexyl]-4-trifluoromethoxy-benzenesulfonamide hydrochloride
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C25H28ClF3N2O3S
 1
1
IC50 = 2600 nM
   TI
   LI
   LO
   TS
CP0856101
N1-[4-(trifluoromethoxy)benzenesulfonyl)-N2-[1-(1-naphthyl)ethyl]-trans-1,2-diaminocyclohexane hydrochloride
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C25H28ClF3N2O3S
 1
1
IC50 = 5400 nM
   TI
   LI
   LO
   TS
CP0853351
4-methoxy-N-((1R,2R)-2-(1-(naphthalen-1-yl)ethylamino)cyclohexyl)benzenesulfonamide hydrochloride
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C25H31ClN2O3S
 1
1
IC50 = 8000 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01916 Extracellular calcium-sensing receptor Homo sapiens, Human
PT07476 Extracellular calcium-sensing receptor Mus musculus, Mouse