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TargetHistamine H1 receptor
LigandBDBM50172421
Substrate/Competitorn/a
Meas. Tech.ChEMBL_321262 (CHEMBL881887)
IC50>10000±n/a nM
Citation Ulven, TFrimurer, TMReceveur, JMLittle, PBRist, ONørregaard, PKHögberg, T 6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode. J Med Chem48:5684-97 (2005) [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:
BDBM50172421
n/a
NameBDBM50172421
Synonyms:(E)-N-{2-[(2-Dimethylamino-ethyl)-methyl-amino]-4-methyl-quinolin-6-yl}-3-(4-trifluoromethoxy-phenyl)-acrylamide | CHEMBL189118 | N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methylquinolin-6-yl)-3-(4-(trifluoromethoxy)phenyl)acrylamide
TypeSmall organic molecule
Emp. Form.C25H27F3N4O2
Mol. Mass.472.5027
SMILESCN(C)CCN(C)c1cc(C)c2cc(NC(=O)\C=C\c3ccc(OC(F)(F)F)cc3)ccc2n1
Structure
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