Reaction Details |
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Target | Extracellular calcium-sensing receptor |
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Ligand | BDBM50272593 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1712581 (CHEMBL4122630) |
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IC50 | 116±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_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
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BDBM50272593 |
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n/a |
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Name | BDBM50272593 |
Synonyms: | CHEMBL4129371 |
Type | Small organic molecule |
Emp. Form. | C23H25Cl2F3N2O |
Mol. Mass. | 473.359 |
SMILES | Cl.Cl.C[C@@H](N[C@@H]1CCN(C1)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12 |r| |
Structure |
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