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TargetHistamine H1 receptor
LigandBDBM50290708
Substrate/Competitorn/a
Meas. Tech.ChEMBL_84420 (CHEMBL691452)
IC50 473±n/a nM
Citation Maynard, GDBratton, LDKane, JMBurkholder, TPSantiago, BStewart, KTKudlacz, EMShatzer, SAKnippenberg, RWFarrell, AMLogan, DE Synthesis and sar of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/tachykinin NK1 receptor antagonist activity Bioorg Med Chem Lett7:2819-2824 (1997)    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:
BDBM50290708
n/a
NameBDBM50290708
Synonyms:CHEMBL94834 | [3-(2-{4-[1-(4-Fluoro-benzyl)-1H-benzoimidazole-2-carbonyl]-piperidin-1-yl}-ethyl)-3-(4-trifluoromethyl-phenyl)-pyrrolidin-1-yl]-(3,4,5-trimethoxy-phenyl)-methanone
TypeSmall organic molecule
Emp. Form.C43H44F4N4O5
Mol. Mass.772.8269
SMILESCOc1cc(cc(OC)c1OC)C(=O)N1CCC(CCN2CCC(CC2)C(=O)c2nc3ccccc3n2Cc2ccc(F)cc2)(C1)c1ccc(cc1)C(F)(F)F
Structure
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