Target
Cannabinoid receptor 1
Ligand
BDBM50424491
Substrate
n/a
Meas. Tech.
ChEMBL_937027 (CHEMBL2317166)
EC50
1.3±n/a nM
Citation
 Plowright, ATNilsson, KAntonsson, MAmin, KBroddefalk, JJensen, JLehmann, AJin, SSt-Onge, STomaszewski, MJTremblay, MWalpole, CWei, ZYang, HUlander, J Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease. J Med Chem 56:220-40 (2013) [PubMed]  Article 
Target
Name:
Cannabinoid receptor 1
Synonyms:
CANN6 | CANNABINOID CB1 | CB-R | CB1 | CNR | CNR1 | CNR1_HUMAN | Cannabinoid CB1 receptor | Cannabinoid receptor | Cannabinoid receptor 1 (CB1) | Cannabinoid receptor 1 (brain)
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
52868.96
Organism:
Homo sapiens (Human)
Description:
P21554
Residue:
472
Sequence:
MKSILDGLADTTFRTITTDLLYVGSNDIQYEDIKGDMASKLGYFPQKFPLTSFRGSPFQEKMTAGDNPQLVPADQVNITEFYNKSLSSFKENEENIQCGENFMDIECFMVLNPSQQLAIAVLSLTLGTFTVLENLLVLCVILHSRSLRCRPSYHFIGSLAVADLLGSVIFVYSFIDFHVFHRKDSRNVFLFKLGGVTASFTASVGSLFLTAIDRYISIHRPLAYKRIVTRPKAVVAFCLMWTIAIVIAVLPLLGWNCEKLQSVCSDIFPHIDETYLMFWIGVTSVLLLFIVYAYMYILWKAHSHAVRMIQRGTQKSIIIHTSEDGKVQVTRPDQARMDIRLAKTLVLILVVLIICWGPLLAIMVYDVFGKMNKLIKTVFAFCSMLCLLNSTVNPIIYALRSKDLRHAFRSMFPSCEGTAQPLDNSMGDSDCLHKHANNAASVHRAAESCIKSTVKIAKVTMSVSTDTSAEAL
  
Inhibitor
Name:
BDBM50424491
Synonyms:
CHEMBL2316377
Type:
Small organic molecule
Emp. Form.:
C26H26N6O3
Mol. Mass.:
470.523
SMILES:
COc1ccc(NC(=O)c2ccc(Cn3ccnn3)c3ccccc23)c(n1)C(=O)NCC1CCC1
Structure:
Search PDB for entries with ligand similarity: