Target
Extracellular calcium-sensing receptor
Ligand
BDBM50325738
Substrate
n/a
Meas. Tech.
ChEMBL_652584
EC50
280±n/a nM
Citation
 Harrington, PESt Jean, DJClarine, JCoulter, TSCroghan, MDavenport, ADavis, JGhiron, CHutchinson, JKelly, MGLott, FLu, JYMartin, DMorony, SPoon, SFPortero-Larragueta, EReagan, JDRegal, KATasker, AWang, MYang, YYao, GZeng, QHenley, CFotsch, C The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core. Bioorg Med Chem Lett 20:5544-7 (2010) [PubMed]  Article  BDB Entry
Target
Name:
Extracellular calcium-sensing receptor
Synonyms:
CASR | CaR | Calcium sensing receptor | Calcium-sensing receptor (CaSR) | Extracellular calcium-sensing receptor | 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:
BDBM50325738
Synonyms:
(R)-N-((6-chloro-4'-(trifluoromethyl)biphenyl-3-yl)methyl)-1-(3-methoxyphenyl)ethanamine | CHEMBL1224344
Type:
Small organic molecule
Emp. Form.:
C23H21ClF3NO
Mol. Mass.:
419.867
SMILES:
COc1cccc(c1)[C@@H](C)NCc1ccc(Cl)c(c1)-c1ccc(cc1)C(F)(F)F |r|
Structure:
Search PDB for entries with ligand similarity: