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TargetExtracellular calcium-sensing receptor
LigandBDBM50339337
Substrate/Competitorn/a
Meas. Tech.ChEMBL_736451 (CHEMBL1694279)
IC50 8.5±n/a nM
Citation Yoshida, MMori, AKotani, EOka, MMakino, HFujita, HBan, JIkeda, YKawamoto, TGoto, MKimura, HBaba, AYasuma, T Discovery of novel and potent orally active calcium-sensing receptor antagonists that stimulate pulselike parathyroid hormone secretion: synthesis and structure-activity relationships of tetrahydropyrazolopyrimidine derivatives. J Med Chem54:1430-40 (2011) [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:
BDBM50339337
n/a
NameBDBM50339337
Synonyms:CHEMBL1688088 | N-{1-[4-(Benzyloxy)phenyl]-1-ethylpropyl}-7,7-dimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide
TypeSmall organic molecule
Emp. Form.C33H38N4O2
Mol. Mass.522.6804
SMILESCCC(CC)(NC(=O)c1cnn2c1NC(CC2(C)C)c1ccccc1)c1ccc(OCc2ccccc2)cc1
Structure
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