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TargetExtracellular calcium-sensing receptor
LigandBDBM50325521
Substrate/Competitorn/a
Meas. Tech.ChEMBL_652215 (CHEMBL1228488)
IC50 4±n/a nM
Citation Gerspacher, MAltmann, EBeerli, RBuhl, TEndres, RGamse, RKameni-Tcheudji, JKneissel, MKrawinkler, KHMissbach, MSchmidt, ASeuwen, KWeiler, SWidler, L Penta-substituted benzimidazoles as potent antagonists of the calcium-sensing receptor (CaSR-antagonists). Bioorg Med Chem Lett20:5161-4 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Extracellular calcium-sensing receptor
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50325521
n/a
NameBDBM50325521
Synonyms:2-(4-isopropylphenyl)-7-methoxy-1-(2-methoxyethyl)-5-((2-methoxypyridin-3-yl)methyl)-4-(trifluoromethyl)-1H-benzo[d]imidazole | CHEMBL1223712
TypeSmall organic molecule
Emp. Form.C28H30F3N3O3
Mol. Mass.513.5513
SMILESCOCCn1c(nc2c(c(Cc3cccnc3OC)cc(OC)c12)C(F)(F)F)-c1ccc(cc1)C(C)C
Structure
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