Reaction Details |
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Target | Histamine H1 receptor |
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Ligand | BDBM50175494 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEBML_84420 |
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IC50 | 10000±n/a nM |
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Citation | Maynard, GD; Bratton, LD; Kane, JM; Burkholder, TP; Santiago, B; Stewart, KT; Kudlacz, EM; Shatzer, SA; Knippenberg, RW; Farrell, AM; Logan, 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 |
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More Info.: | Get all data from this article, Assay Method |
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Histamine H1 receptor |
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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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BDBM50175494 |
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n/a |
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Name | BDBM50175494 |
Synonyms: | 1-{2-[(R)-3-(3,4-Dichloro-phenyl)-1-(3,4,5-trimethoxy-benzoyl)-pyrrolidin-3-yl]-ethyl}-4-phenyl-piperidine-4-carboxylic acid amide | 3-((E)-3-Carboxy-3-phenyl-allyl)-4,6-dichloro-1H-indole-2-carboxylic acid | CHEMBL330366 | MDL 104,335 (S)-enantiomer | MDL-105212 |
Type | Small organic molecule |
Emp. Form. | C34H39Cl2N3O5 |
Mol. Mass. | 640.597 |
SMILES | COc1cc(cc(OC)c1OC)C(=O)N1CC[C@@](CCN2CCC(CC2)(C(N)=O)c2ccccc2)(C1)c1ccc(Cl)c(Cl)c1 |
Structure |
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