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Target
Extracellular calcium-sensing receptor
Ligand
BDBM50272603
Substrate
n/a
Meas. Tech.
ChEMBL_1712581 (CHEMBL4122630)
IC50
>100±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 
Target
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:
MASYSCCLALLALAWHSSAYGPDQRAQKKGDIILGGLFPIHFGVAAKDQDLKSRPESVECIRYNFRGFRWLQAMIFAIEEINSSPSLLPNMTLGYRIFDTCNTVSKALEATLSFVAQNKIDSLNLDEFCNCSEHIPSTIAVVGATGSGVSTAVANLLGLFYIPQVSYASSSRLLSNKNQYKSFLRTIPNDEHQATAMADIIEYFRWNWVGTIAADDDYGRPGIEKFREEAEERDICIDFSELISQYSDEEEIQQVVEVIQNSTAKVIVVFSSGPDLEPLIKEIVRRNITGRIWLASEAWASSSLIAMPEYFHVVGGTIGFGLKAGQIPGFREFLQKVHPRKSVHNGFAKEFWEETFNCHLQEGAKGPLPVDTFVRSHEEGGNRLLNSSTAFRPLCTGDENINSVETPYMDYEHLRISYNVYLAVYSIAHALQDIYTCLPGRGLFTNGSCADIKKVEAWQVLKHLRHLNFTNNMGEQVTFDECGDLVGNYSIINWHLSPEDGSIVFKEVGYYNVYAKKGERLFINEEKILWSGFSREVPFSNCSRDCQAGTRKGIIEGEPTCCFECVECPDGEYSGETDASACDKCPDDFWSNENHTSCIAKEIEFLAWTEPFGIALTLFAVLGIFLTAFVLGVFIKFRNTPIVKATNRELSYLLLFSLLCCFSSSLFFIGEPQDWTCRLRQPAFGISFVLCISCILVKTNRVLLVFEAKIPTSFHRKWWGLNLQFLLVFLCTFMQILICIIWLYTAPPSSYRNHELEDEIIFITCHEGSLMALGSLIGYTCLLAAICFFFAFKSRKLPENFNEAKFITFSMLIFFIVWISFIPAYASTYGKFVSAVEVIAILAASFGLLACIFFNKVYIILFKPSRNTIEEVRSSTAAHAFKVAARATLRRPNISRKRSSSLGGSTGSIPSSSISSKSNSEDRFPQPERQKQQQPLSLTQQEQQQQPLTLHPQQQQQPQQPRCKQKVIFGSGTVTFSLSFDEPQKNAMAHRNSMRQNSLEAQRSNDTLGRHQALLPLQCADADSEMTIQETGLQGPMVGDHQPEMESSDEMSPALVMSTSRSFVISGGGSSVTENVLHS
  
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:
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