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TargetHistamine H1 receptor
LigandBDBM50316922
Substrate/Competitorn/a
Meas. Tech.ChEMBL_630093 (CHEMBL1110013)
Ki 8.4±n/a nM
Citation Lavrador-Erb, KRavula, SBYu, JZamani-Kord, SMoree, WJPetroski, REWen, JMalany, SHoare, SRMadan, ACrowe, PDBeaton, G The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia. Bioorg Med Chem Lett20:2916-9 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Histamine H1 receptor
Name:Histamine H1 receptor
Synonyms:H1R | HH1R | HISTAMINE H1 | HRH1 | HRH1_HUMAN
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:55808.72
Organism:Homo sapiens (Human)
Description:Cell pellets from SK-N-MC cells transfected with human H1 receptor were used in binding assay.
Residue:487
Sequence:
MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHT
VGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFI
LCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKC
ETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLR
PENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKL
YCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSR
TDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFI
MAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFK
RILHIRS
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50316922
n/a
NameBDBM50316922
Synonyms:(R)-1-(1-(4-methoxybenzyl)-1H-benzo[d]imidazol-2-yl)-N,N-dimethylpyrrolidin-3-amine | CHEMBL1087367
TypeSmall organic molecule
Emp. Form.C21H26N4O
Mol. Mass.350.4573
SMILESCOc1ccc(Cn2c(nc3ccccc23)N2CC[C@H](C2)N(C)C)cc1 |r|
Structure
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