Reaction Details |
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Target | Histamine H1 receptor |
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Ligand | BDBM50247054 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1277728 (CHEMBL3097144) |
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Ki | >2512±n/a nM |
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Citation | Wilson, DM; Apps, J; Bailey, N; Bamford, MJ; Beresford, IJ; Brackenborough, K; Briggs, MA; Brough, S; Calver, AR; Crook, B; Davis, RK; Davis, RP; Davis, S; Dean, DK; Harris, L; Heslop, T; Holland, V; Jeffrey, P; Panchal, TA; Parr, CA; Quashie, N; Schogger, J; Sehmi, SS; Stean, TO; Steadman, JG; Trail, B; Wald, J; Worby, A; Takle, AK; Witherington, J; Medhurst, AD Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists. Bioorg Med Chem Lett23:6890-6 (2013) [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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BDBM50247054 |
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n/a |
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Name | BDBM50247054 |
Synonyms: | 6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yloxy)-N-methylnicotinamide | CHEMBL517140 | GSK-189254 |
Type | Small organic molecule |
Emp. Form. | C21H25N3O2 |
Mol. Mass. | 351.4421 |
SMILES | CNC(=O)c1ccc(Oc2ccc3CCN(CCc3c2)C2CCC2)nc1 |
Structure |
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