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TargetHistamine H1 receptor
LigandBDBM50418284
Substrate/Competitorn/a
Meas. Tech.ChEMBL_741663 (CHEMBL1769655)
Ki 15.85±n/a nM
Citation Procopiou, PABrowning, CBuckley, JMClark, KLFechner, LGore, PMHancock, APHodgson, STHolmes, DSKranz, MLooker, BEMorriss, KMParton, DLRussell, LJSlack, RJSollis, SLVile, SWatts, CJ The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. J Med Chem54:2183-95 (2011) [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
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  Blast E-value cutoff:
BDBM50418284
n/a
NameBDBM50418284
Synonyms:CHEMBL1765111
TypeSmall organic molecule
Emp. Form.C38H47ClN4O2
Mol. Mass.627.258
SMILESClc1ccc(Cc2nn(C3CCCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c(=O)c3ccccc23)cc1
Structure
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