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TargetHistamine H3 receptor
LigandBDBM50327477
Substrate/Competitorn/a
Meas. Tech.ChEMBL_664625
Ki 12±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 H3 receptor
Name:Histamine H3 receptor
Synonyms:HH3R
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:48607.98
Organism:Rattus norvegicus (rat)
Description:n/a
Residue:445
Sequence:
MERAPPDGLMNASGTLAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCAS
SVFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMALVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGGREAG
PEPPPDAQPSPPPAPPSCWGCWPKGHGEAMPLHRYGVGEAGPGVEAGEAALGGGSGGGAA
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSITQRFRLSRDKKVAKSL
AIIVSIFGLCWAPYTLLMIIRAACHGRCIPDYWYETSFWLLWANSAVNPVLYPLCHYSFR
RAFTKLLCPQKLKVQPHGSLEQCWK
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50327477
n/a
NameBDBM50327477
Synonyms:(R)-2-(cyclopropylmethyl)-8-(1-isopropylpiperidin-4-yloxy)-3-methyl-3,4-dihydropyrazino[1,2-a]indol-1(2H)-one | CHEMBL1257965
TypeSmall organic molecule
Emp. Form.C24H33N3O2
Mol. Mass.395.5377
SMILESCC(C)N1CCC(CC1)Oc1ccc2n3C[C@@H](C)N(CC4CC4)C(=O)c3cc2c1 |r|
Structure
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