| Reaction Details |
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 | Report a problem with these data |
| Target | Histamine H3 receptor |
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| Ligand | BDBM50247054 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_523447 (CHEMBL1008299) |
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| Ki | 0.12±n/a nM |
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| Citation |  Pierson, PD; Fettes, A; Freichel, C; Gatti-McArthur, S; Hertel, C; Huwyler, J; Mohr, P; Nakagawa, T; Nettekoven, M; Plancher, JM; Raab, S; Richter, H; Roche, O; Rodríguez Sarmiento, RM; Schmitt, M; Schuler, F; Takahashi, T; Taylor, S; Ullmer, C; Wiegand, R 5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity. J Med Chem52:3855-68 (2009) [PubMed] Article |
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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 |
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| Synonyms: | G-protein coupled receptor 97 | GPCR97 | HH3R | HISTAMINE H3 | HRH3 | HRH3_HUMAN | Histamine H3 receptor (H3) | Histamine H3L | Histamine receptor (H3 and H4) |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 48691.47 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Binding assays were using CHO cells stably expressing hH3R receptors. |
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| Residue: | 445 |
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| Sequence: | MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTS
SAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAA
GPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSV
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSL
AVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR
RAFTKLLCPQKLKIQPHSSLEHCWK
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| BDBM50247054 |
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| n/a |
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| Name | BDBM50247054 |
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| Synonyms: | 6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yloxy)-N-methylnicotinamide | CHEMBL517140 | GSK-189254 |
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| Type | Small organic molecule |
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| Emp. Form. | C21H25N3O2 |
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| Mol. Mass. | 351.4421 |
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| SMILES | CNC(=O)c1ccc(Oc2ccc3CCN(CCc3c2)C2CCC2)nc1 |
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| Structure | 
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