Target
Histamine H1 receptor
Ligand
BDBM50297310
Substrate
n/a
Meas. Tech.
ChEMBL_582981 (CHEMBL1051819)
Ki
0.9±n/a nM
Citation
 Moree, WJLi, BFJovic, FCoon, TYu, JGross, RSTucci, FMarinkovic, DZamani-Kord, SMalany, SBradbury, MJHernandez, LMO'Brien, ZWen, JWang, HHoare, SRPetroski, RESacaan, AMadan, ACrowe, PDBeaton, G Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia. J Med Chem 52:5307-10 (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:
BDBM50297310
Synonyms:
(-)-Dimethyl-{2-[3-((R)-1-pyridin-2-yl-ethyl)-benzofuran-2-yl]-ethyl}-amine | CHEMBL563920
Type:
Small organic molecule
Emp. Form.:
C19H22N2O
Mol. Mass.:
294.3908
SMILES:
C[C@H](c1c(CCN(C)C)oc2ccccc12)c1ccccn1 |r|
Structure:
Search PDB for entries with ligand similarity: