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TargetHistamine receptor (H3)
LigandBDBM50327495
Substrate/Competitorn/a
Meas. Tech.ChEMBL_664613
Ki 27±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 Lett 20:5713-7 (2010) [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:
BDBM50327495
n/a
NameBDBM50327495
Synonyms:2-isopropyl-8-(1-isopropylpiperidin-4-yloxy)-3,4-dihydropyrazino[1,2-a]indol-1(2H)-one | CHEMBL1258874
TypeSmall organic molecule
Emp. Form.C22H31N3O2
Mol. Mass.369.5004
SMILESCC(C)N1CCC(CC1)Oc1ccc2n3CCN(C(C)C)C(=O)c3cc2c1
Structure
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