| Reaction Details |
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 | Report a problem with these data |
| Target | Histamine H1 receptor |
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| Ligand | BDBM50295710 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_577960 (CHEMBL1059633) |
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| IC50 | 35±n/a nM |
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| Citation |  Kubota, K; Kurebayashi, H; Miyachi, H; Tobe, M; Onishi, M; Isobe, Y Synthesis and structure-activity relationships of phenothiazine carboxylic acids having pyrimidine-dione as novel histamine H(1) antagonists. Bioorg Med Chem Lett19:2766-71 (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 |
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| Synonyms: | H1R | HH1R | HISTAMINE H1 | HRH1 | HRH1_HUMAN |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 55808.72 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Cell pellets from SK-N-MC cells transfected with human H1 receptor were used in binding assay. |
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| Residue: | 487 |
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| Sequence: | MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHT
VGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFI
LCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKC
ETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLR
PENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKL
YCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSR
TDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFI
MAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFK
RILHIRS
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| BDBM50295710 |
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| n/a |
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| Name | BDBM50295710 |
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| Synonyms: | 10-(4-(4-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)piperazin-1-yl)butyl)-10H-phenothiazine-2-carboxylic acid | CHEMBL552057 |
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| Type | Small organic molecule |
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| Emp. Form. | C27H31N5O4S |
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| Mol. Mass. | 521.631 |
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| SMILES | Cn1c(cc(=O)n(C)c1=O)N1CCN(CCCCN2c3ccccc3Sc3ccc(cc23)C(O)=O)CC1 |
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| Structure | 
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