Reaction Details |
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Target | Histamine H1 receptor |
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Ligand | BDBM50314274 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_624292 (CHEMBL1106977) |
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Ki | 2.9±n/a nM |
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Citation | Moree, WJ; Jovic, F; Coon, T; Yu, J; Li, BF; Tucci, FC; Marinkovic, D; Gross, RS; Malany, S; Bradbury, MJ; Hernandez, LM; O'Brien, Z; Wen, J; Wang, H; Hoare, SR; Petroski, RE; Sacaan, A; Madan, A; Crowe, PD; Beaton, G Novel benzothiophene H1-antihistamines for the treatment of insomnia. Bioorg Med Chem Lett20:2316-20 (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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BDBM50314274 |
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n/a |
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Name | BDBM50314274 |
Synonyms: | (-)-(R)-2-(3-(1-(2-methoxypyridin-3-yl)ethyl)benzo[b]thiophen-2-yl)-N,N-dimethylethanamine | CHEMBL1093294 |
Type | Small organic molecule |
Emp. Form. | C20H24N2OS |
Mol. Mass. | 340.482 |
SMILES | COc1ncccc1[C@@H](C)c1c(CCN(C)C)sc2ccccc12 |r| |
Structure |
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