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TargetHistamine H1 receptor
LigandBDBM50356878
Substrate/Competitorn/a
Meas. Tech.ChEMBL_788362 (CHEMBL1918043)
Ki>40000±n/a nM
Citation Masood, MASelby, MDBell, ASMansfield, ACGardner, MSmith, GFLane, CKenyon-Edwards, HOsborne, RJones, RMLiu, WLBrown, CDClarke, NPerrucio, FMowbray, CE Discovery of a series of potent and selective human H4 antagonists using ligand efficiency and libraries to explore structure-activity relationship (SAR). Bioorg Med Chem Lett21:6591-5 (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:
BDBM50356878
n/a
NameBDBM50356878
Synonyms:CHEMBL1915534
TypeSmall organic molecule
Emp. Form.C14H25N5
Mol. Mass.263.3818
SMILESCC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 |r|
Structure
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