Reaction Details |
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Target | Histamine H1 receptor |
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Ligand | BDBM50316922 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_630093 (CHEMBL1110013) |
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Ki | 8.4±n/a nM |
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Citation | Lavrador-Erb, K; Ravula, SB; Yu, J; Zamani-Kord, S; Moree, WJ; Petroski, RE; Wen, J; Malany, S; Hoare, SR; Madan, A; Crowe, PD; Beaton, G The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia. Bioorg Med Chem Lett20:2916-9 (2010) [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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BDBM50316922 |
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n/a |
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Name | BDBM50316922 |
Synonyms: | (R)-1-(1-(4-methoxybenzyl)-1H-benzo[d]imidazol-2-yl)-N,N-dimethylpyrrolidin-3-amine | CHEMBL1087367 |
Type | Small organic molecule |
Emp. Form. | C21H26N4O |
Mol. Mass. | 350.4573 |
SMILES | COc1ccc(Cn2c(nc3ccccc23)N2CC[C@H](C2)N(C)C)cc1 |r| |
Structure |
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