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Target
Cannabinoid receptor 1 [H219A]
Ligand
BDBM21278
Substrate
n/a
Meas. Tech.
Radioligand Binding Assay
pH
7.4±n/a
Kd
2.5±0.6 nM
Comments
extracted
Citation
 Shim, JY; Ahn, KH; Kendall, DA Molecular basis of cannabinoid CB1 receptor coupling to the G protein heterotrimer Gaiß¿: identification of key CB1 contacts with the C-terminal helix a5 of Gai. J Biol Chem 288:32449-65 (2013) [PubMed]  Article 
Target
Name:
Cannabinoid receptor 1 [H219A]
Synonyms:
CNR | CNR1 | CNR1_HUMAN | Cannabinoid receptor 1 (CB1 H219A)
Type:
Protein
Mol. Mass.:
52802.40
Organism:
Homo sapiens (Human)
Description:
Human CB1 H219A mutant
Residue:
472
Sequence:
MKSILDGLADTTFRTITTDLLYVGSNDIQYEDIKGDMASKLGYFPQKFPLTSFRGSPFQEKMTAGDNPQLVPADQVNITEFYNKSLSSFKENEENIQCGENFMDIECFMVLNPSQQLAIAVLSLTLGTFTVLENLLVLCVILHSRSLRCRPSYHFIGSLAVADLLGSVIFVYSFIDFHVFHRKDSRNVFLFKLGGVTASFTASVGSLFLTAIDRYISIARPLAYKRIVTRPKAVVAFCLMWTIAIVIAVLPLLGWNCEKLQSVCSDIFPHIDETYLMFWIGVTSVLLLFIVYAYMYILWKAHSHAVRMIQRGTQKSIIIHTSEDGKVQVTRPDQARMDIRLAKTLVLILVVLIICWGPLLAIMVYDVFGKMNKLIKTVFAFCSMLCLLNSTVNPIIYALRSKDLRHAFRSMFPSCEGTAQPLDNSMGDSDCLHKHANNAASVHRAAESCIKSTVKIAKVTMSVSTDTSAEAL
  
Inhibitor
Name:
BDBM21278
Synonyms:
5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide | Acomplia | CHEMBL111 | CHEMBL558598 | RIMONABANT HYDROCHLORIDE | Rimonabant | SR 141716A | SR141716 | SR141716A | [3H]Rimonabant | [3H]SR141716A
Type:
Small organic molecule
Emp. Form.:
C22H21Cl3N4O
Mol. Mass.:
463.787
SMILES:
Cc1c(nn(c1-c1ccc(Cl)cc1)-c1ccc(Cl)cc1Cl)C(=O)NN1CCCCC1
Structure:
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