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Target
Extracellular calcium-sensing receptor
Ligand
BDBM50325517
Substrate
n/a
Meas. Tech.
ChEMBL_652215 (CHEMBL1228488)
IC50
43±n/a nM
Citation
 Gerspacher, M; Altmann, E; Beerli, R; Buhl, T; Endres, R; Gamse, R; Kameni-Tcheudji, J; Kneissel, M; Krawinkler, KH; Missbach, M; Schmidt, A; Seuwen, K; Weiler, S; Widler, L Penta-substituted benzimidazoles as potent antagonists of the calcium-sensing receptor (CaSR-antagonists). Bioorg Med Chem Lett 20:5161-4 (2010) [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:
BDBM50325517
Synonyms:
4-bromo-5-(3,4-dimethoxybenzyl)-2-(4-isopropylphenyl)-7-methoxy-1-(2-methoxyethyl)-1H-benzo[d]imidazole | CHEMBL1222490
Type:
Small organic molecule
Emp. Form.:
C29H33BrN2O4
Mol. Mass.:
553.487
SMILES:
COCCn1c(nc2c(Br)c(Cc3ccc(OC)c(OC)c3)cc(OC)c12)-c1ccc(cc1)C(C)C
Structure:
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