Target
Histamine H1 receptor
Ligand
BDBM50316921
Substrate
n/a
Meas. Tech.
ChEMBL_630093 (CHEMBL1110013)
Ki
4.8±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 Lett 20:2916-9 (2010) [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:
BDBM50316921
Synonyms:
(S)-1-(1-(2-ethoxyethyl)-1H-benzo[d]imidazol-2-yl)-N,N-dimethylpyrrolidin-3-amine | CHEMBL1087493
Type:
Small organic molecule
Emp. Form.:
C17H26N4O
Mol. Mass.:
302.4145
SMILES:
CCOCCn1c(nc2ccccc12)N1CC[C@@H](C1)N(C)C |r|
Structure:
Search PDB for entries with ligand similarity: