Reaction Details Report a problem with these data
Target
Extracellular calcium-sensing receptor
Ligand
BDBM28009
Substrate
BDBM10852
Meas. Tech.
Calcium-Sensing Receptor Antagonist Fluorescence Assay
IC50
6900±n/a nM
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 Chem 52:1204-8 (2009) [PubMed]  Article 
Target
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:
MAFYSCCWVLLALTWHTSAYGPDQRAQKKGDIILGGLFPIHFGVAAKDQDLKSRPESVECIRYNFRGFRWLQAMIFAIEEINSSPALLPNLTLGYRIFDTCNTVSKALEATLSFVAQNKIDSLNLDEFCNCSEHIPSTIAVVGATGSGVSTAVANLLGLFYIPQVSYASSSRLLSNKNQFKSFLRTIPNDEHQATAMADIIEYFRWNWVGTIAADDDYGRPGIEKFREEAEERDICIDFSELISQYSDEEEIQHVVEVIQNSTAKVIVVFSSGPDLEPLIKEIVRRNITGKIWLASEAWASSSLIAMPQYFHVVGGTIGFALKAGQIPGFREFLKKVHPRKSVHNGFAKEFWEETFNCHLQEGAKGPLPVDTFLRGHEESGDRFSNSSTAFRPLCTGDENISSVETPYIDYTHLRISYNVYLAVYSIAHALQDIYTCLPGRGLFTNGSCADIKKVEAWQVLKHLRHLNFTNNMGEQVTFDECGDLVGNYSIINWHLSPEDGSIVFKEVGYYNVYAKKGERLFINEEKILWSGFSREVPFSNCSRDCLAGTRKGIIEGEPTCCFECVECPDGEYSDETDASACNKCPDDFWSNENHTSCIAKEIEFLSWTEPFGIALTLFAVLGIFLTAFVLGVFIKFRNTPIVKATNRELSYLLLFSLLCCFSSSLFFIGEPQDWTCRLRQPAFGISFVLCISCILVKTNRVLLVFEAKIPTSFHRKWWGLNLQFLLVFLCTFMQIVICVIWLYTAPPSSYRNQELEDEIIFITCHEGSLMALGFLIGYTCLLAAICFFFAFKSRKLPENFNEAKFITFSMLIFFIVWISFIPAYASTYGKFVSAVEVIAILAASFGLLACIFFNKIYIILFKPSRNTIEEVRCSTAAHAFKVAARATLRRSNVSRKRSSSLGGSTGSTPSSSISSKSNSEDPFPQPERQKQQQPLALTQQEQQQQPLTLPQQQRSQQQPRCKQKVIFGSGTVTFSLSFDEPQKNAMAHRNSTHQNSLEAQKSSDTLTRHEPLLPLQCGETDLDLTVQETGLQGPVGGDQRPEVEDPEELSPALVVSSSQSFVISGGGSTVTENVVNS
  
Inhibitor
Name:
BDBM28009
Synonyms:
2-[benzyl(methyl)amino]-4-(3,4-dimethoxyphenyl)-N-(2-phenoxyethyl)pyrimidine-5-carboxamide | trisubstituted pyrimidine analogue, 11j
Type:
Small organic molecule
Emp. Form.:
C29H30N4O4
Mol. Mass.:
498.5729
SMILES:
COc1ccc(cc1OC)-c1nc(ncc1C(=O)NCCOc1ccccc1)N(C)Cc1ccccc1
Structure:
Search PDB for entries with ligand similarity:
Substrate