Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetExtracellular calcium-sensing receptor
LigandBDBM50272596
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1712580 (CHEMBL4122629)
EC50 17±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 | CASR_HUMAN | CaR | Calcium sensing receptor | Calcium-sensing receptor (CaSR) | Extracellular calcium-sensing receptor | GPRC2A | PCAR1 | Parathyroid Cell calcium-sensing receptor | Parathyroid cell calcium-sensing receptor 1 | Synonyms=GPRC2A | hCasR
Type:Protein
Mol. Mass.:120663.13
Organism:Homo sapiens (Human)
Description:P41180
Residue:1078
Sequence:
MAFYSCCWVLLALTWHTSAYGPDQRAQKKGDIILGGLFPIHFGVAAKDQDLKSRPESVEC
IRYNFRGFRWLQAMIFAIEEINSSPALLPNLTLGYRIFDTCNTVSKALEATLSFVAQNKI
DSLNLDEFCNCSEHIPSTIAVVGATGSGVSTAVANLLGLFYIPQVSYASSSRLLSNKNQF
KSFLRTIPNDEHQATAMADIIEYFRWNWVGTIAADDDYGRPGIEKFREEAEERDICIDFS
ELISQYSDEEEIQHVVEVIQNSTAKVIVVFSSGPDLEPLIKEIVRRNITGKIWLASEAWA
SSSLIAMPQYFHVVGGTIGFALKAGQIPGFREFLKKVHPRKSVHNGFAKEFWEETFNCHL
QEGAKGPLPVDTFLRGHEESGDRFSNSSTAFRPLCTGDENISSVETPYIDYTHLRISYNV
YLAVYSIAHALQDIYTCLPGRGLFTNGSCADIKKVEAWQVLKHLRHLNFTNNMGEQVTFD
ECGDLVGNYSIINWHLSPEDGSIVFKEVGYYNVYAKKGERLFINEEKILWSGFSREVPFS
NCSRDCLAGTRKGIIEGEPTCCFECVECPDGEYSDETDASACNKCPDDFWSNENHTSCIA
KEIEFLSWTEPFGIALTLFAVLGIFLTAFVLGVFIKFRNTPIVKATNRELSYLLLFSLLC
CFSSSLFFIGEPQDWTCRLRQPAFGISFVLCISCILVKTNRVLLVFEAKIPTSFHRKWWG
LNLQFLLVFLCTFMQIVICVIWLYTAPPSSYRNQELEDEIIFITCHEGSLMALGFLIGYT
CLLAAICFFFAFKSRKLPENFNEAKFITFSMLIFFIVWISFIPAYASTYGKFVSAVEVIA
ILAASFGLLACIFFNKIYIILFKPSRNTIEEVRCSTAAHAFKVAARATLRRSNVSRKRSS
SLGGSTGSTPSSSISSKSNSEDPFPQPERQKQQQPLALTQQEQQQQPLTLPQQQRSQQQP
RCKQKVIFGSGTVTFSLSFDEPQKNAMAHRNSTHQNSLEAQKSSDTLTRHEPLLPLQCGE
TDLDLTVQETGLQGPVGGDQRPEVEDPEELSPALVVSSSQSFVISGGGSTVTENVVNS
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50272596
n/a
NameBDBM50272596
Synonyms:CHEMBL4126450
TypeSmall organic molecule
Emp. Form.C23H25ClN6
Mol. Mass.420.938
SMILESCl.C[C@@H](N[C@H]1CCN(C1)c1ccc(cc1)-c1nn[nH]n1)c1cccc2ccccc12 |r|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: