Reaction Details |
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Target | Histamine H1 receptor |
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Ligand | BDBM50079576 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1471696 (CHEMBL3421064) |
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Ki | >10000±n/a nM |
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Citation | Hudkins, RL; Becknell, NC; Lyons, JA; Aimone, LD; Olsen, M; Haltiwanger, RC; Mathiasen, JR; Raddatz, R; Gruner, JA 3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity. Eur J Med Chem95:349-56 (2015) [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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BDBM50079576 |
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n/a |
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Name | BDBM50079576 |
Synonyms: | CHEMBL3417585 |
Type | Small organic molecule |
Emp. Form. | C19H25N3O2 |
Mol. Mass. | 327.4207 |
SMILES | [H][C@@]12C[C@]1([H])C(=NNC2=O)c1ccc(OCCCN2CCC[C@H]2C)cc1 |r,c:6| |
Structure |
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