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TargetExtracellular calcium-sensing receptor
LigandBDBM50272593
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1712581 (CHEMBL4122630)
IC50 116±n/a nM
Citation Miyazaki, HIkeda, YSakurai, OMiyake, TTsubota, ROkabe, JKuroda, MHisada, YYanagida, TYoneda, HTsukumo, YTokunaga, SKawata, TOhashi, RFukuda, HKojima, KKannami, AKifuji, TSato, NIdei, AIguchi, TSakairi, TMoritani, Y Discovery of evocalcet, a next-generation calcium-sensing receptor agonist for the treatment of hyperparathyroidism. Bioorg Med Chem Lett28:2055-2060 (2018) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Extracellular calcium-sensing receptor
Name:Extracellular calcium-sensing receptor
Synonyms:CASR_RAT | Calcium sensing receptor | Casr | Gprc2a | Parathyroid Cell calcium-sensing receptor | Pcar1
Type:PROTEIN
Mol. Mass.:120858.46
Organism:Rattus norvegicus
Description:ChEMBL_750426
Residue:1079
Sequence:
MASYSCCLALLALAWHSSAYGPDQRAQKKGDIILGGLFPIHFGVAAKDQDLKSRPESVEC
IRYNFRGFRWLQAMIFAIEEINSSPSLLPNMTLGYRIFDTCNTVSKALEATLSFVAQNKI
DSLNLDEFCNCSEHIPSTIAVVGATGSGVSTAVANLLGLFYIPQVSYASSSRLLSNKNQY
KSFLRTIPNDEHQATAMADIIEYFRWNWVGTIAADDDYGRPGIEKFREEAEERDICIDFS
ELISQYSDEEEIQQVVEVIQNSTAKVIVVFSSGPDLEPLIKEIVRRNITGRIWLASEAWA
SSSLIAMPEYFHVVGGTIGFGLKAGQIPGFREFLQKVHPRKSVHNGFAKEFWEETFNCHL
QEGAKGPLPVDTFVRSHEEGGNRLLNSSTAFRPLCTGDENINSVETPYMDYEHLRISYNV
YLAVYSIAHALQDIYTCLPGRGLFTNGSCADIKKVEAWQVLKHLRHLNFTNNMGEQVTFD
ECGDLVGNYSIINWHLSPEDGSIVFKEVGYYNVYAKKGERLFINEEKILWSGFSREVPFS
NCSRDCQAGTRKGIIEGEPTCCFECVECPDGEYSGETDASACDKCPDDFWSNENHTSCIA
KEIEFLAWTEPFGIALTLFAVLGIFLTAFVLGVFIKFRNTPIVKATNRELSYLLLFSLLC
CFSSSLFFIGEPQDWTCRLRQPAFGISFVLCISCILVKTNRVLLVFEAKIPTSFHRKWWG
LNLQFLLVFLCTFMQILICIIWLYTAPPSSYRNHELEDEIIFITCHEGSLMALGSLIGYT
CLLAAICFFFAFKSRKLPENFNEAKFITFSMLIFFIVWISFIPAYASTYGKFVSAVEVIA
ILAASFGLLACIFFNKVYIILFKPSRNTIEEVRSSTAAHAFKVAARATLRRPNISRKRSS
SLGGSTGSIPSSSISSKSNSEDRFPQPERQKQQQPLSLTQQEQQQQPLTLHPQQQQQPQQ
PRCKQKVIFGSGTVTFSLSFDEPQKNAMAHRNSMRQNSLEAQRSNDTLGRHQALLPLQCA
DADSEMTIQETGLQGPMVGDHQPEMESSDEMSPALVMSTSRSFVISGGGSSVTENVLHS
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50272593
n/a
NameBDBM50272593
Synonyms:CHEMBL4129371
TypeSmall organic molecule
Emp. Form.C23H25Cl2F3N2O
Mol. Mass.473.359
SMILESCl.Cl.C[C@@H](N[C@@H]1CCN(C1)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12 |r|
Structure
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