Target
Histamine H1 receptor
Ligand
BDBM50297863
Substrate
n/a
Meas. Tech.
ChEMBL_584293 (CHEMBL1060927)
Ki
1.5±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 Lett 19:4380-4 (2009) [PubMed]  Article 
Target
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:
MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHTVGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFILCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKCETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLRPENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKLYCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSRTDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFIMAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFKRILHIRS
  
Inhibitor
Name:
BDBM50297863
Synonyms:
CHEMBL563451 | N,N-dimethyl-1-(1-(4-methylbenzyl)-1H-benzo[d]imidazol-2-yl)piperidin-4-amine
Type:
Small organic molecule
Emp. Form.:
C22H28N4
Mol. Mass.:
348.4845
SMILES:
CN(C)C1CCN(CC1)c1nc2ccccc2n1Cc1ccc(C)cc1
Structure:
Search PDB for entries with ligand similarity: