Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetHistamine H1 receptor
LigandBDBM50315203
Substrate/Competitorn/a
Meas. Tech.ChEMBL_760134 (CHEMBL1815390)
Ki 2.7±n/a nM
Citation Moree, WJLi, BFZamani-Kord, SYu, JCoon, THuang, CMarinkovic, DTucci, FCMalany, SBradbury, MJHernandez, LMWen, JWang, HHoare, SRPetroski, REJalali, KYang, CSacaan, AMadan, ACrowe, PDBeaton, G Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia. Bioorg Med Chem Lett20:5874-8 (2010) [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:
BDBM50315203
n/a
NameBDBM50315203
Synonyms:(R)-2-(3-(1-(3-methoxypyrazin-2-yl)ethyl)-6-methyl-1H-inden-2-yl)-N,N-dimethylethanamine | CHEMBL1090176
TypeSmall organic molecule
Emp. Form.C21H27N3O
Mol. Mass.337.4586
SMILESCOc1nccnc1[C@H](C)C1=C(CCN(C)C)Cc2cc(C)ccc12 |r,c:11|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: