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TargetHistamine receptor (H3)
LigandBDBM22548
Substrate/CompetitorBDBM22530
Meas. Tech.Radioligand Binding Assay and Functional [35S]GTP-gamma-S Binding Assay
pH7.4±n/a
Temperature298.15±n/a K
Ki 1±0.15 nM
EC50 2±1 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 Chem 51:2944-53 (2008) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Histamine receptor (H3)
Name:Histamine receptor (H3 and H4)
Synonyms:G-protein coupled receptor 97 | HH3R | HISTAMINE H3 | HRH3 | Histamine H3 Receptor | 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:
BDBM22548
BDBM22530
NameBDBM22548
Synonyms:2-[3-(1H-imidazol-4-ylmethyl)phenyl]-4,4,6-trimethyl-5,6-dihydro-4H-1,3-oxazine | 4-Benzyl-1H-imidazole derivative, 26
TypeSmall organic molecule
Emp. Form.C17H21N3O
Mol. Mass.283.3681
SMILESCC1CC(C)(C)N=C(O1)c1cccc(Cc2cnc[nH]2)c1 |c:6|
Structure
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