Reaction Details |
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Target | Extracellular calcium-sensing receptor |
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Ligand | BDBM50272596 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1712580 (CHEMBL4122629) |
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EC50 | 17±n/a nM |
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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 Lett28:2055-2060 (2018) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Extracellular calcium-sensing receptor |
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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
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BDBM50272596 |
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n/a |
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Name | BDBM50272596 |
Synonyms: | CHEMBL4126450 |
Type | Small organic molecule |
Emp. Form. | C23H25ClN6 |
Mol. Mass. | 420.938 |
SMILES | Cl.C[C@@H](N[C@H]1CCN(C1)c1ccc(cc1)-c1nn[nH]n1)c1cccc2ccccc12 |r| |
Structure |
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