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TargetHistamine H1 receptor
LigandBDBM50402109
Substrate/Competitorn/a
Meas. Tech.ChEMBL_884700 (CHEMBL2215148)
Ki 25.12±n/a nM
Citation Furber, MAlcaraz, LLuckhurst, CBahl, ABeaton, HBowers, KCollington, JDenton, RDonald, DKinchin, EMacDonald, CRigby, ARiley, RSoars, MSpringthorpe, BWebborn, P Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H1 antagonists. Part II: optimising in vivo clearance. Bioorg Med Chem Lett22:7707-10 (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 | 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:
BDBM50402109
n/a
NameBDBM50402109
Synonyms:CHEMBL2207659
TypeSmall organic molecule
Emp. Form.C20H24ClF3N4O3
Mol. Mass.460.878
SMILESCc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2cn[nH]c2C(F)(F)F)CC1 |r|
Structure
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