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TargetHistamine H1 receptor
LigandBDBM50394143
Substrate/Competitorn/a
Meas. Tech.ChEMBL_856370
Ki 5.01±n/a nM
Citation Bahl ABarton PBowers KCaffrey MVDenton RGilmour PHawley SLinannen TLuckhurst CAMochel TPerry MWRiley RJRoe ESpringthorpe BStein LWebborn P Scaffold-hopping with zwitterionic CCR3 antagonists: identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092. Bioorg Med Chem Lett 22:6694-9 (2012) [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
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:
BDBM50394143
n/a
NameBDBM50394143
Synonyms:CHEMBL2158829
TypeSmall organic molecule
Emp. Form.C25H30Cl2N2O4
Mol. Mass.493.423
SMILESOC(=O)COc1cccc(c1)N1CCC(CN2CCC(CC2)Oc2ccc(Cl)c(Cl)c2)CC1
Structure
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