Reaction Details |
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Target | Extracellular calcium-sensing receptor |
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Ligand | BDBM27999 |
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Substrate/Competitor | BDBM10852 |
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Meas. Tech. | Calcium-Sensing Receptor Antagonist Fluorescence Assay |
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pH | 7.5±n/a |
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Temperature | 310.15±n/a K |
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IC50 | >30000±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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BDBM27999 |
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BDBM10852 |
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Name | BDBM27999 |
Synonyms: | 2-{[(2R)-1-hydroxy-3-phenylpropan-2-yl]amino}-N-(2-phenoxyethyl)-4-(3,4,5-trimethoxyphenyl)pyrimidine-5-carboxamide | trisubstituted pyrimidine analogue, 6t |
Type | Small organic molecule |
Emp. Form. | C31H34N4O6 |
Mol. Mass. | 558.6249 |
SMILES | COc1cc(cc(OC)c1OC)-c1nc(N[C@@H](CO)Cc2ccccc2)ncc1C(=O)NCCOc1ccccc1 |r| |
Structure |
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