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Reaction Details
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TargetCannabinoid receptor 1
LigandBDBM29096
Substrate/CompetitorBDBM21278
Meas. Tech.CB Receptor Radioligand Binding Assay (Ki)
pH7.2±n/a
Temperature295.15±n/a K
Ki 0.32±0.07 nM
Citation Pettersson, HBülow, AEk, FJensen, JOttesen, LKFejzic, AMa, JNDel Tredici, ALCurrier, EAGardell, LRTabatabaei, ACraig, DMcFarland, KOtt, TRPiu, FBurstein, ESOlsson, R Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. J Med Chem52:1975-82 (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 | 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:
MKSILDGLADTTFRTITTDLLYVGSNDIQYEDIKGDMASKLGYFPQKFPLTSFRGSPFQE
KMTAGDNPQLVPADQVNITEFYNKSLSSFKENEENIQCGENFMDIECFMVLNPSQQLAIA
VLSLTLGTFTVLENLLVLCVILHSRSLRCRPSYHFIGSLAVADLLGSVIFVYSFIDFHVF
HRKDSRNVFLFKLGGVTASFTASVGSLFLTAIDRYISIHRPLAYKRIVTRPKAVVAFCLM
WTIAIVIAVLPLLGWNCEKLQSVCSDIFPHIDETYLMFWIGVTSVLLLFIVYAYMYILWK
AHSHAVRMIQRGTQKSIIIHTSEDGKVQVTRPDQARMDIRLAKTLVLILVVLIICWGPLL
AIMVYDVFGKMNKLIKTVFAFCSMLCLLNSTVNPIIYALRSKDLRHAFRSMFPSCEGTAQ
PLDNSMGDSDCLHKHANNAASVHRAAESCIKSTVKIAKVTMSVSTDTSAEAL
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  Blast E-value cutoff:
BDBM29096
BDBM21278
NameBDBM29096
Synonyms:dibenzothiazepine, 12b
TypeSmall organic molecule
Emp. Form.C26H24ClN3OS
Mol. Mass.462.006
SMILESClc1cccc(CNC(=O)c2ccc3Sc4ccccc4C(=Nc3c2)N2CCCCC2)c1 |c:22|
Structure
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