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TargetHistamine H1 receptor
LigandBDBM50440737
Substrate/Competitorn/a
Meas. Tech.ChEMBL_986340 (CHEMBL2433831)
Ki 1420±n/a nM
Citation Peddibhotla, SHedrick, MPHershberger, PMaloney, PRLi, YMilewski, MGosalia, PGray, WMehta, ASugarman, EHood, BSuyama, ENguyen, KHeynen-Genel, SVasile, SSalaniwal, SStonich, DSu, YMangravita-Novo, AVicchiarelli, MRoth, GPSmith, LHChung, TDHanson, GRThomas, JBCaron, MGBarak, LSPinkerton, AB Discovery of ML314, a Brain Penetrant Non-Peptidic?-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor. ACS Med Chem Lett4:846-851 (2013) [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:
BDBM50440737
n/a
NameBDBM50440737
Synonyms:CHEMBL2431120
TypeSmall organic molecule
Emp. Form.C24H28N4O3
Mol. Mass.420.5041
SMILESCOc1ccccc1N1CCN(CC1)c1nc(nc2cc(OC)c(OC)cc12)C1CC1
Structure
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