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TargetCannabinoid receptor 1
LigandBDBM29075
Substrate/CompetitorBDBM21278
Meas. Tech.CB1 Radioligand Binding Assay (Ki) and GTP-gamma-[35S] Binding Assay (EC50)
pH7.4±n/a
Temperature303.15±n/a K
Ki 1.0±0.7 nM
EC50 0.82±0.2 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 Chem 52:2652-5 (2009) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Cannabinoid receptor 1
Name:Cannabinoid receptor 1
Synonyms:CANN6 | CANNABINOID CB1 | CB-R | CB1 | CNR | CNR1 | 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:
MKSILDGLADTTFRTITTDLLYVGSNDIQYEDIKGDMASKLGYFPQKFPLTSFRGSPFQE
KMTAGDNPQLVPADQVNITEFYNKSLSSFKENEENIQCGENFMDIECFMVLNPSQQLAIA
VLSLTLGTFTVLENLLVLCVILHSRSLRCRPSYHFIGSLAVADLLGSVIFVYSFIDFHVF
HRKDSRNVFLFKLGGVTASFTASVGSLFLTAIDRYISIHRPLAYKRIVTRPKAVVAFCLM
WTIAIVIAVLPLLGWNCEKLQSVCSDIFPHIDETYLMFWIGVTSVLLLFIVYAYMYILWK
AHSHAVRMIQRGTQKSIIIHTSEDGKVQVTRPDQARMDIRLAKTLVLILVVLIICWGPLL
AIMVYDVFGKMNKLIKTVFAFCSMLCLLNSTVNPIIYALRSKDLRHAFRSMFPSCEGTAQ
PLDNSMGDSDCLHKHANNAASVHRAAESCIKSTVKIAKVTMSVSTDTSAEAL
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  Blast E-value cutoff:
BDBM29075
BDBM21278
NameBDBM29075
Synonyms:PF-514273
TypeSmall organic molecule
Emp. Form.C21H17Cl2F2N3O2
Mol. Mass.452.281
SMILESCC(F)(F)CN1CCOc2c(nn(c2-c2ccc(Cl)cc2)-c2ccccc2Cl)C1=O
Structure
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