Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetHistamine H1 receptor
LigandBDBM22877
Substrate/Competitorn/a
Meas. Tech.ChEMBL_584293 (CHEMBL1060927)
Ki 2.7±n/a nM
Citation Coon, TMoree, WJLi, BYu, JZamani-Kord, SMalany, SSantos, MAHernandez, LMPetroski, RESun, AWen, JSullivan, SHaelewyn, JHedrick, MHoare, SJBradbury, MJCrowe, PDBeaton, G Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia. Bioorg Med Chem Lett19:4380-4 (2009) [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:
BDBM22877
n/a
NameBDBM22877
Synonyms:2-((1-(1-(4-fluorobenzyl)-1H-benzo[d]imidazol-2-yl)piperidin-4-yl)(methyl)amino)pyrimidin-4(3H)-one | 2-({1-[1-(4-Fluoro-benzyl)-1H-benzoimidazol-2-yl]-piperidin-4-yl}-methyl-amino)-3H-pyrimidin-4-one | 2-({1-[3-(4-Fluoro-benzyl)-1H-benzoimidazol-2-yl]-piperidin-4-yl}-methyl-amino)-2,3-dihydro-1H-pyrimidin-4-one(Mizolastine) | 2-[(1-{1-[(4-fluorophenyl)methyl]-1H-1,3-benzodiazol-2-yl}piperidin-4-yl)(methyl)amino]-3,4-dihydropyrimidin-4-one | CHEMBL94454 | Mizolastine | Mizollen | Zolistan
TypeSmall organic molecule
Emp. Form.C24H25FN6O
Mol. Mass.432.4933
SMILESCN(C1CCN(CC1)c1nc2ccccc2n1Cc1ccc(F)cc1)c1nccc(=O)[nH]1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: