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Reaction Details
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TargetHistamine H3 receptor
LigandBDBM22549
Substrate/CompetitorBDBM22530
Meas. Tech.H3R Radioligand Binding Assay
pH7.4±n/a
Temperature298.15±n/a K
Ki 40±8 nM
Citation Wijtmans, MCelanire, SSnip, EGillard, MRGelens, ECollart, PPVenhuis, BJChristophe, BHulscher, Svan der Goot, HLebon, FTimmerman, HBakker, RALallemand, BILeurs, RTalaga, PEde Esch, IJ 4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists. J Med Chem51:2944-53 (2008) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  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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  Blast E-value cutoff:
BDBM22549
BDBM22530
NameBDBM22549
Synonyms:2-[3-(1H-imidazol-4-ylmethyl)phenyl]-3-oxa-1-azaspiro[4.4]non-1-ene | 4-Benzyl-1H-imidazole derivative, 27
TypeSmall organic molecule
Emp. Form.C17H19N3O
Mol. Mass.281.3523
SMILESC(c1cnc[nH]1)c1cccc(c1)C1=NC2(CCCC2)CO1 |t:14|
Structure
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