Reaction Details |
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Target | Histamine H1 receptor |
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Ligand | BDBM35254 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1339952 (CHEMBL3243859) |
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Ki | 2.0±n/a nM |
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Citation | Li, P; Zhang, Q; Robichaud, AJ; Lee, T; Tomesch, J; Yao, W; Beard, JD; Snyder, GL; Zhu, H; Peng, Y; Hendrick, JP; Vanover, KE; Davis, RE; Mates, S; Wennogle, LP Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. J Med Chem57:2670-82 (2014) [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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BDBM35254 |
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n/a |
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Name | BDBM35254 |
Synonyms: | 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b][1,5]benzodiazepine | CHEMBL715 | Olansek | US8802672, Olanzapine | Zyprexa | olanzapine |
Type | Small organic molecule |
Emp. Form. | C17H20N4S |
Mol. Mass. | 312.432 |
SMILES | CN1CCN(CC1)C1=Nc2ccccc2Nc2sc(C)cc12 |t:8| |
Structure |
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