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Reaction Details
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TargetCannabinoid receptor 2
LigandBDBM29065
Substrate/CompetitorBDBM21244
Meas. Tech.CB1 Radioligand Binding Assay (Ki) and GTP-gamma-[35S] Binding Assay (EC50)
Ki 1780±n/a nM
Citation Dow, RLCarpino, PAHadcock, JRBlack, SCIredale, PADaSilva-Jardine, PSchneider, SRPaight, ESGriffith, DAScott, DOO'Connor, RENduaka, 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 Chem52:2652-5 (2009) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Cannabinoid receptor 2
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:
MEECWVTEIANGSKDGLDSNPMKDYMILSGPQKTAVAVLCTLLGLLSALENVAVLYLILS
SHQLRRKPSYLFIGSLAGADFLASVVFACSFVNFHVFHGVDSKAVFLLKIGSVTMTFTAS
VGSLLLTAIDRYLCLRYPPSYKALLTRGRALVTLGIMWVLSALVSYLPLMGWTCCPRPCS
ELFPLIPNDYLLSWLLFIAFLFSGIIYTYGHVLWKAHQHVASLSGHQDRQVPGMARMRLD
VRLAKTLGLVLAVLLICWFPVLALMAHSLATTLSDQVKKAFAFCSMLCLINSMVNPVIYA
LRSGEIRSSAHHCLAHWKKCVRGLGSEAKEEAPRSSVTETEADGKITPWPDSRDLDLSDC
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  Blast E-value cutoff:
BDBM29065
BDBM21244
NameBDBM29065
Synonyms:lactam-based compound, 12d
TypeSmall organic molecule
Emp. Form.C22H21Cl2N3O
Mol. Mass.414.328
SMILESCC(C)CN1CCc2c(nn(c2-c2ccc(Cl)cc2)-c2ccccc2Cl)C1=O
Structure
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