| Reaction Details |
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 | Report a problem with these data |
| Target | Histamine H1 receptor |
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| Ligand | BDBM50002087 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_685205 (CHEMBL1287093) |
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| Ki | 0.158±n/a nM |
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| Citation |  Gianotti, M; Botta, M; Brough, S; Carletti, R; Castiglioni, E; Corti, C; Dal-Cin, M; Delle Fratte, S; Korajac, D; Lovric, M; Merlo, G; Mesic, M; Pavone, F; Piccoli, L; Rast, S; Roscic, M; Sava, A; Smehil, M; Stasi, L; Togninelli, A; Wigglesworth, MJ Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders. J Med Chem53:7778-95 (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 |
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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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| BDBM50002087 |
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| n/a |
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| Name | BDBM50002087 |
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| Synonyms: | 4-(1-Methyl-piperidin-4-ylidene)-4,9-dihydro-1-thia-benzo[f]azulen-10-one(Ketotifen hydrogen malate) | 4-(1-Methyl-piperidin-4-ylidene)-4,9-dihydro-1-thia-benzo[f]azulen-10-one(Ketotifen) | 4-(1-methyl-piperidin-4-ylidene)-4,9-dihydro-1-thia-benzo[f]azulen-10-one | CHEMBL534 | KETOTIFEN | Zaditor |
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| Type | Small organic molecule |
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| Emp. Form. | C19H19NOS |
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| Mol. Mass. | 309.425 |
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| SMILES | [#6]-[#7]-1-[#6]-[#6]\[#6](-[#6]-[#6]-1)=[#6]-1\c2ccsc2-[#6](=O)-[#6]-c2ccccc-12 |
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| Structure | 
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