Reaction Details |
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Target | Histamine H3 receptor |
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Ligand | BDBM50139301 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEBML_83645 |
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Ki | 47±n/a nM |
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Citation | Gfesser, GA; Zhang, H; Dinges, J; Fox, GB; Pan, JB; Esbenshade, TA; Yao, BB; Witte, D; Miller, TR; Kang, CH; Krueger, KM; Bennani, YL; Hancock, AA; Faghih, R Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists. Bioorg Med Chem Lett14:673-6 (2004) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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Histamine H3 receptor |
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Name: | Histamine H3 receptor |
Synonyms: | G-protein coupled receptor 97 | GPCR97 | HH3R | HISTAMINE H3 | HRH3 | HRH3_HUMAN | Histamine H3 receptor (H3) | Histamine H3L | Histamine receptor (H3 and H4) |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 48691.47 |
Organism: | Homo sapiens (Human) |
Description: | Binding assays were using CHO cells stably expressing hH3R receptors. |
Residue: | 445 |
Sequence: | MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTS
SAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAA
GPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSV
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSL
AVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR
RAFTKLLCPQKLKIQPHSSLEHCWK
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BDBM50139301 |
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n/a |
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Name | BDBM50139301 |
Synonyms: | CHEMBL345143 | N-[(R)-2-(4-{3-[4-(5-Cyclopentylmethyl-[1,2,4]oxadiazol-3-yl)-3-fluoro-phenoxy]-propyl}-piperazin-1-yl)-1-methyl-2-oxo-ethyl]-2-(3-dimethylamino-phenyl)-acetamide |
Type | Small organic molecule |
Emp. Form. | C33H43FN6O4 |
Mol. Mass. | 606.7307 |
SMILES | C[C@@H](NC(=O)c1cccc(c1)N(C)C)C(=O)N1CCN(CCCOc2ccc(-c3noc(CC4CCCC4)n3)c(F)c2)CC1 |
Structure |
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