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Target
Cannabinoid receptor 2
Ligand
BDBM29061
Substrate
BDBM21244
Meas. Tech.
CB1 Radioligand Binding Assay (Ki) and GTP-gamma-[35S] Binding Assay (EC50)
Ki
>10000±n/a nM
Citation
 Dow, RL; Carpino, PA; Hadcock, JR; Black, SC; Iredale, PA; DaSilva-Jardine, P; Schneider, SR; Paight, ES; Griffith, DA; Scott, DO; O'Connor, RE; Nduaka, CI Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. J Med Chem 52:2652-5 (2009) [PubMed]  Article
Target
Name:
Cannabinoid receptor 2
Synonyms:
CANNABINOID CB2 | CB-2 | CB2 | CB2A | CB2B | CNR2 | CNR2_HUMAN | CX5 | Cannabinoid CB2 receptor | Cannabinoid receptor 2 (CB2) | Cannabinoid receptor 2 (CB2R) | hCB2
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
39690.94
Organism:
Homo sapiens (Human)
Description:
P34972
Residue:
360
Sequence:
MEECWVTEIANGSKDGLDSNPMKDYMILSGPQKTAVAVLCTLLGLLSALENVAVLYLILSSHQLRRKPSYLFIGSLAGADFLASVVFACSFVNFHVFHGVDSKAVFLLKIGSVTMTFTASVGSLLLTAIDRYLCLRYPPSYKALLTRGRALVTLGIMWVLSALVSYLPLMGWTCCPRPCSELFPLIPNDYLLSWLLFIAFLFSGIIYTYGHVLWKAHQHVASLSGHQDRQVPGMARMRLDVRLAKTLGLVLAVLLICWFPVLALMAHSLATTLSDQVKKAFAFCSMLCLINSMVNPVIYALRSGEIRSSAHHCLAHWKKCVRGLGSEAKEEAPRSSVTETEADGKITPWPDSRDLDLSDC
  
Inhibitor
Name:
BDBM29061
Synonyms:
CHEMBL201602 | pyrazolopyrimidinone-based antagonist, 3
Type:
n/a
Emp. Form.:
C20H13Cl2F3N4O
Mol. Mass.:
453.245
SMILES:
Cc1nc2c(-c3ccc(Cl)cc3)n(nc2c(=O)n1CC(F)(F)F)-c1ccccc1Cl
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM21244
Synonyms:
2-[(1S,2S,5S)-5-hydroxy-2-(3-hydroxypropyl)cyclohexyl]-5-(2-methyloctan-2-yl)phenol | 3-(2-hydroxy-4-(1,1-dimethylheptyl)phenyl)-4-(3-hydroxypropyl)cyclohexanol | CP 55,940 | CP-55,940 | CP-56667 [(+)-AC],XV | [3H]-56 | [3H]CP55940
Type:
radiolabeled ligand
Emp. Form.:
C24H40O3
Mol. Mass.:
376.5726
SMILES:
CCCCCCC(C)(C)c1ccc([C@H]2C[C@@H](O)CC[C@@H]2CCCO)c(O)c1
Structure:
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