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TargetHistamine H3 receptor
LigandBDBM50269097
Substrate/Competitorn/a
Meas. Tech.ChEMBL_523452 (CHEMBL1008304)
EC50 4±n/a nM
Citation Pierson, PDFettes, AFreichel, CGatti-McArthur, SHertel, CHuwyler, JMohr, PNakagawa, TNettekoven, MPlancher, JMRaab, SRichter, HRoche, ORodríguez Sarmiento, RMSchmitt, MSchuler, FTakahashi, TTaylor, SUllmer, CWiegand, R 5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity. J Med Chem52:3855-68 (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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BDBM50269097
n/a
NameBDBM50269097
Synonyms:(4,4-difluoropiperidin-1-yl)(5-(1-isopropylpiperidin-4-yloxy)-1-(methylsulfonyl)-1H-indol-2-yl)methanone | CHEMBL495639
TypeSmall organic molecule
Emp. Form.C23H31F2N3O4S
Mol. Mass.483.572
SMILESCC(C)N1CCC(CC1)Oc1ccc2n(c(cc2c1)C(=O)N1CCC(F)(F)CC1)S(C)(=O)=O
Structure
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