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TargetHistamine receptor (H3)
LigandBDBM50079579
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1471679
Ki 2.3±n/a nM
Citation Hudkins RLBecknell NCLyons JAAimone LDOlsen MHaltiwanger RCMathiasen JRRaddatz RGruner JA 3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity. Eur J Med Chem 95:349-56 (2015) [PubMed]  Article
More Info.:Get all data from this article,  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:
BDBM50079579
n/a
NameBDBM50079579
Synonyms:CHEMBL3417505
TypeSmall organic molecule
Emp. Form.C20H27N3O2
Mol. Mass.341.4473
SMILESC[C@H](COc1ccc(cc1)C1=NNC(=O)C2CC12)CN1CCC[C@H]1C |r,t:11|
Structure
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