Reaction Details |
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Target | Histamine H1 receptor |
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Ligand | BDBM50297854 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_584293 (CHEMBL1060927) |
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Ki | 6.6±n/a nM |
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Citation | Coon, T; Moree, WJ; Li, B; Yu, J; Zamani-Kord, S; Malany, S; Santos, MA; Hernandez, LM; Petroski, RE; Sun, A; Wen, J; Sullivan, S; Haelewyn, J; Hedrick, M; Hoare, SJ; Bradbury, MJ; Crowe, PD; Beaton, G Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia. Bioorg Med Chem Lett19:4380-4 (2009) [PubMed] 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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BDBM50297854 |
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n/a |
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Name | BDBM50297854 |
Synonyms: | 1'-(1-(4-fluorobenzyl)-1H-benzo[d]imidazol-2-yl)-1,4'-bipiperidin-2-one | CHEMBL552026 |
Type | Small organic molecule |
Emp. Form. | C24H27FN4O |
Mol. Mass. | 406.4958 |
SMILES | Fc1ccc(Cn2c(nc3ccccc23)N2CCC(CC2)N2CCCCC2=O)cc1 |
Structure |
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