Target
Extracellular calcium-sensing receptor
Ligand
BDBM27989
Substrate
BDBM10852
Meas. Tech.
Calcium-Sensing Receptor Antagonist Fluorescence Assay
pH
7.5±n/a
Temperature
310.15±n/a K
IC50
>30000±n/a nM
Citation
 Yang, WRuan, ZWang, YVan Kirk, KMa, ZArey, BJCooper, CBSeethala, RFeyen, JHDickson, 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:
BDBM27989
Synonyms:
N-(2-phenoxyethyl)-2-[(pyridin-2-ylmethyl)amino]-4-(3,4,5-trimethoxyphenyl)pyrimidine-5-carboxamide | trisubstituted pyrimidine analogue, 6j
Type:
Small organic molecule
Emp. Form.:
C28H29N5O5
Mol. Mass.:
515.5604
SMILES:
COc1cc(cc(OC)c1OC)-c1nc(NCc2ccccn2)ncc1C(=O)NCCOc1ccccc1
Structure:
Search PDB for entries with ligand similarity:
Substrate