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TargetHistamine H3 receptor
LigandBDBM50327486
Substrate/Competitorn/a
Meas. Tech.ChEMBL_664613 (CHEMBL1260327)
Ki 5±n/a nM
Citation Richter, HGFreichel, CHuwyler, JNakagawa, TNettekoven, MPlancher, JMRaab, SRoche, OSchuler, FTaylor, SUllmer, CWiegand, R Discovery of potent and selective histamine H3 receptor inverse agonists based on the 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one scaffold. Bioorg Med Chem Lett20:5713-7 (2010) [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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  Blast E-value cutoff:
BDBM50327486
n/a
NameBDBM50327486
Synonyms:8-(1-isopropylpiperidin-4-yloxy)-2-(pyridin-3-ylmethyl)-3,4-dihydropyrazino[1,2-a]indol-1(2H)-one | CHEMBL1257486
TypeSmall organic molecule
Emp. Form.C25H30N4O2
Mol. Mass.418.5313
SMILESCC(C)N1CCC(CC1)Oc1ccc2n3CCN(Cc4cccnc4)C(=O)c3cc2c1
Structure
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