Reaction Details |
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Target | Histamine H1 receptor |
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Ligand | BDBM50090647 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_84423 (CHEMBL691611) |
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Ki | 54±n/a nM |
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Citation | Lagu, B; Tian, D; Jeon, Y; Li, C; Wetzel, JM; Nagarathnam, D; Shen, Q; Forray, C; Chang, RS; Broten, TP; Ransom, RW; Chan, TB; O'Malley, SS; Schorn, TW; Rodrigues, AD; Kassahun, K; Pettibone, DJ; Freidinger, RO; Gluchowski, C De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability. J Med Chem43:2775-8 (2000) [PubMed] |
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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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BDBM50090647 |
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n/a |
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Name | BDBM50090647 |
Synonyms: | (4S,5S)-4-(3,4-Difluoro-phenyl)-5-methyl-2-oxo-oxazolidine-3-carboxylic acid {3-[4-(4-fluoro-phenyl)-piperidin-1-yl]-propyl}-amide | (4S,5S)-4-(3,4-difluorophenyl)-N-(3-(4-(4-fluorophenyl)piperidin-1-yl)propyl)-5-methyl-2-oxooxazolidine-3-carboxamide | 4-(3,4-Difluoro-phenyl)-5-methyl-2-oxo-oxazolidine-3-carboxylic acid {3-[4-(4-fluoro-phenyl)-piperidin-1-yl]-propyl}-amide | CHEMBL96467 | SNAP-7915 |
Type | Small organic molecule |
Emp. Form. | C25H28F3N3O3 |
Mol. Mass. | 475.5033 |
SMILES | C[C@@H]1OC(=O)N([C@H]1c1ccc(F)c(F)c1)C(=O)NCCCN1CCC(CC1)c1ccc(F)cc1 |r| |
Structure |
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