Reaction Details
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Extracellular calcium-sensing receptor
Ligand
BDBM50272603
Substrate
n/a
Meas. Tech.
ChEMBL_1712580 (CHEMBL4122629)
EC50
1100±n/a nM
Citation
Miyazaki, H; Ikeda, Y; Sakurai, O; Miyake, T; Tsubota, R; Okabe, J; Kuroda, M; Hisada, Y; Yanagida, T; Yoneda, H; Tsukumo, Y; Tokunaga, S; Kawata, T; Ohashi, R; Fukuda, H; Kojima, K; Kannami, A; Kifuji, T; Sato, N; Idei, A; Iguchi, T; Sakairi, T; Moritani, Y Discovery of evocalcet, a next-generation calcium-sensing receptor agonist for the treatment of hyperparathyroidism. Bioorg Med Chem Lett 28:2055-2060 (2018) [PubMed] Article More Info.:
Target
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:
MAFYSCCWVLLALTWHTSAYGPDQRAQKKGDIILGGLFPIHFGVAAKDQDLKSRPESVECIRYNFRGFRWLQAMIFAIEEINSSPALLPNLTLGYRIFDTCNTVSKALEATLSFVAQNKIDSLNLDEFCNCSEHIPSTIAVVGATGSGVSTAVANLLGLFYIPQVSYASSSRLLSNKNQFKSFLRTIPNDEHQATAMADIIEYFRWNWVGTIAADDDYGRPGIEKFREEAEERDICIDFSELISQYSDEEEIQHVVEVIQNSTAKVIVVFSSGPDLEPLIKEIVRRNITGKIWLASEAWASSSLIAMPQYFHVVGGTIGFALKAGQIPGFREFLKKVHPRKSVHNGFAKEFWEETFNCHLQEGAKGPLPVDTFLRGHEESGDRFSNSSTAFRPLCTGDENISSVETPYIDYTHLRISYNVYLAVYSIAHALQDIYTCLPGRGLFTNGSCADIKKVEAWQVLKHLRHLNFTNNMGEQVTFDECGDLVGNYSIINWHLSPEDGSIVFKEVGYYNVYAKKGERLFINEEKILWSGFSREVPFSNCSRDCLAGTRKGIIEGEPTCCFECVECPDGEYSDETDASACNKCPDDFWSNENHTSCIAKEIEFLSWTEPFGIALTLFAVLGIFLTAFVLGVFIKFRNTPIVKATNRELSYLLLFSLLCCFSSSLFFIGEPQDWTCRLRQPAFGISFVLCISCILVKTNRVLLVFEAKIPTSFHRKWWGLNLQFLLVFLCTFMQIVICVIWLYTAPPSSYRNQELEDEIIFITCHEGSLMALGFLIGYTCLLAAICFFFAFKSRKLPENFNEAKFITFSMLIFFIVWISFIPAYASTYGKFVSAVEVIAILAASFGLLACIFFNKIYIILFKPSRNTIEEVRCSTAAHAFKVAARATLRRSNVSRKRSSSLGGSTGSTPSSSISSKSNSEDPFPQPERQKQQQPLALTQQEQQQQPLTLPQQQRSQQQPRCKQKVIFGSGTVTFSLSFDEPQKNAMAHRNSTHQNSLEAQKSSDTLTRHEPLLPLQCGETDLDLTVQETGLQGPVGGDQRPEVEDPEELSPALVVSSSQSFVISGGGSTVTENVVNS
Inhibitor
Name:
BDBM50272603
Synonyms:
CHEMBL4130141
Type:
Small organic molecule
Emp. Form.:
C24H28Cl2N2O2
Mol. Mass.:
447.397
SMILES:
Cl.Cl.C[C@@H](N[C@H]1CCCN(C1)c1ccc(cc1)C(O)=O)c1cccc2ccccc12 |r|
Structure:
