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TargetHistamine H3 receptor
LigandBDBM50296186
Substrate/Competitorn/a
Meas. Tech.ChEMBL_579538 (CHEMBL1061547)
IC50 8.6±n/a nM
Citation Sasaki, TTakahashi, TNagase, TMizutani, TIto, SMitobe, YMiyamoto, YKanesaka, MYoshimoto, RTanaka, TTakenaga, NTokita, SSato, N Synthesis, structure-activity relationships, and biological profiles of a dihydrobenzoxathiin class of histamine H(3) receptor inverse agonists. Bioorg Med Chem Lett19:4232-6 (2009) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Histamine H3 receptor
Name:Histamine H3 receptor
Synonyms:G-protein coupled receptor 97 | GPCR97 | HH3R | HISTAMINE H3 | HRH3 | HRH3_HUMAN | Histamine H3 receptor (H3) | Histamine H3L | Histamine receptor (H3 and H4)
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:48691.47
Organism:Homo sapiens (Human)
Description:Binding assays were using CHO cells stably expressing hH3R receptors.
Residue:445
Sequence:
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTS
SAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAA
GPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSV
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSL
AVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR
RAFTKLLCPQKLKIQPHSSLEHCWK
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BDBM50296186
n/a
NameBDBM50296186
Synonyms:1-(3-(4-(3-methylbenzo[b][1,4]oxathiin-2-yl)phenoxy)propyl)pyrrolidine | CHEMBL560923
TypeSmall organic molecule
Emp. Form.C22H25NO2S
Mol. Mass.367.504
SMILESCC1=C(Oc2ccccc2S1)c1ccc(OCCCN2CCCC2)cc1 |t:1|
Structure
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