Reaction Details |
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Target | Extracellular calcium-sensing receptor |
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Ligand | BDBM28022 |
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Substrate/Competitor | BDBM10852 |
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Meas. Tech. | Calcium-Sensing Receptor Antagonist Fluorescence Assay |
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IC50 | 197±n/a nM |
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Citation | Yang, W; Ruan, Z; Wang, Y; Van Kirk, K; Ma, Z; Arey, BJ; Cooper, CB; Seethala, R; Feyen, JH; Dickson, JK Discovery and Structure-Activity Relationships of Trisubstituted Pyrimidines/Pyridines as Novel Calcium-Sensing Receptor Antagonists. J Med Chem52:1204-8 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, 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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BDBM28022 |
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BDBM10852 |
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Name | BDBM28022 |
Synonyms: | 6-{[(3-chlorophenyl)methyl]amino}-2-(2,6-dimethoxypyridin-3-yl)-N-(2-phenoxyethyl)pyridine-3-carboxamide | trisubstituted pyridine analogue, 18h |
Type | Small organic molecule |
Emp. Form. | C28H27ClN4O4 |
Mol. Mass. | 518.991 |
SMILES | COc1ccc(c(OC)n1)-c1nc(NCc2cccc(Cl)c2)ccc1C(=O)NCCOc1ccccc1 |
Structure |
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