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TargetHistamine H1 receptor
LigandBDBM21395
Substrate/Competitorn/a
Meas. Tech.ChEMBL_858207 (CHEMBL2167670)
Ki 2±n/a nM
Citation Lin, XHuang, XPChen, GWhaley, RPeng, SWang, YZhang, GWang, SXWang, SRoth, BLHuang, N Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors. J Med Chem55:5749-59 (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:
BDBM21395
n/a
NameBDBM21395
Synonyms:3-(2-(4-(4-Fluorobenzoyl)piperidinol)ethyl)-2,4(1H,3H)-quinazolinedione | 3-(2-{4-[(4-fluorophenyl)carbonyl]piperidin-1-yl}ethyl)-1,2,3,4-tetrahydroquinazoline-2,4-dione | CHEMBL1628637 | CHEMBL51 | Ketanserin | R-41,468 | R-41-468 | R41,468 | [3H]-Ketanserin
Typeradiolabeled ligand
Emp. Form.C22H22FN3O3
Mol. Mass.395.4268
SMILESFc1ccc(cc1)C(=O)C1CCN(CCn2c(=O)[nH]c3ccccc3c2=O)CC1
Structure
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