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Target
Histamine H1 receptor
Ligand
BDBM50297861
Substrate
n/a
Meas. Tech.
ChEMBL_630093 (CHEMBL1110013)
Ki
3.9±n/a nM
Citation
 Lavrador-Erb, K; Ravula, SB; Yu, J; Zamani-Kord, S; Moree, WJ; Petroski, RE; Wen, J; Malany, S; Hoare, SR; Madan, A; Crowe, PD; Beaton, 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:
BDBM50297861
Synonyms:
1-(1-(4-fluorobenzyl)-1H-benzo[d]imidazol-2-yl)-N-methyl-N-((tetrahydro-2H-pyran-4-yl)methyl)piperidin-4-amine | CHEMBL550818
Type:
Small organic molecule
Emp. Form.:
C26H33FN4O
Mol. Mass.:
436.5648
SMILES:
CN(CC1CCOCC1)C1CCN(CC1)c1nc2ccccc2n1Cc1ccc(F)cc1
Structure:
Search PDB for entries with ligand similarity: