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Reaction Details
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TargetCannabinoid receptor 1
LigandBDBM27342
Substrate/CompetitorBDBM21278
Meas. Tech.CB Receptor Binding Assay
pH7.4±n/a
Temperature303.15±n/a K
Ki 5.9±n/a nM
Citation Griffith, DAHadcock, JRBlack, SCIredale, PACarpino, PADaSilva-Jardine, PDay, RDiBrino, JDow, RLLandis, MSO'Connor, REScott, DO Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. J Med Chem52:234-7 (2009) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Cannabinoid receptor 1
Name:Cannabinoid receptor 1
Synonyms:Brain-type cannabinoid receptor | CANNABINOID CB1 | CB-R | CB1 | CNR1_RAT | Cannabinoid CB1 receptor | Cannabinoid receptor | Cannabinoid receptor 1 (CB1) | Cnr1 | Skr6
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:52856.55
Organism:Rattus norvegicus (rat)
Description:P20272
Residue:473
Sequence:
MKSILDGLADTTFRTITTDLLYVGSNDIQYEDIKGDMASKLGYFPQKFPLTSFRGSPFQE
KMTAGDNSPLVPAGDTTNITEFYNKSLSSFKENEENIQCGENFMDMECFMILNPSQQLAI
AVLSLTLGTFTVLENLLVLCVILHSRSLRCRPSYHFIGSLAVADLLGSVIFVYSFVDFHV
FHRKDSPNVFLFKLGGVTASFTASVGSLFLTAIDRYISIHRPLAYKRIVTRPKAVVAFCL
MWTIAIVIAVLPLLGWNCKKLQSVCSDIFPLIDETYLMFWIGVTSVLLLFIVYAYMYILW
KAHSHAVRMIQRGTQKSIIIHTSEDGKVQVTRPDQARMDIRLAKTLVLILVVLIICWGPL
LAIMVYDVFGKMNKLIKTVFAFCSMLCLLNSTVNPIIYALRSKDLRHAFRSMFPSCEGTA
QPLDNSMGDSDCLHKHANNTASMHRAAESCIKSTVKIAKVTMSVSTDTSAEAL
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  Blast E-value cutoff:
BDBM27342
BDBM21278
NameBDBM27342
Synonyms:9-(4-chlorophenyl)-8-(2,4-dichlorophenyl)-6-(4-methylpiperazin-1-yl)-9H-purine | Purine antagonist, 3f
TypeSmall organic molecule
Emp. Form.C22H19Cl3N6
Mol. Mass.473.785
SMILESCN1CCN(CC1)c1ncnc2n(c(nc12)-c1ccc(Cl)cc1Cl)-c1ccc(Cl)cc1
Structure
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