Reaction Details Report a problem with these data
Target
Cannabinoid receptor 1
Ligand
BDBM50306235
Substrate
n/a
Meas. Tech.
ChEMBL_606748 (CHEMBL1065338)
IC50
0.26±n/a nM
Citation
Receveur, JM; Murray, A; Linget, JM; Nørregaard, PK; Cooper, M; Bjurling, E; Nielsen, PA; Högberg, T Conversion of 4-cyanomethyl-pyrazole-3-carboxamides into CB1 antagonists with lowered propensity to pass the blood-brain-barrier. Bioorg Med Chem Lett 20:453-7 (2010) [PubMed] Article
More Info.:
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:
BDBM50306235
Synonyms:
2-(1-(2-chlorophenyl)-5-(4-chlorophenyl)-3-(4-hydroxy-4-phenylpiperidine-1-carbonyl)-1H-pyrazol-4-yl)acetamide | CHEMBL605109
Type:
Small organic molecule
Emp. Form.:
C29H26Cl2N4O3
Mol. Mass.:
549.448
SMILES:
NC(=O)Cc1c(nn(c1-c1ccc(Cl)cc1)-c1ccccc1Cl)C(=O)N1CCC(O)(CC1)c1ccccc1