| Reaction Details |
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 | Report a problem with these data |
| Target | Histamine H3 receptor |
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| Ligand | BDBM50361233 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_794973 (CHEMBL1936300) |
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| Ki | 4.2±n/a nM |
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| Citation |  Semple, G; Santora, VJ; Smith, JM; Covel, JA; Hayashi, R; Gallardo, C; Ibarra, JB; Schultz, JA; Park, DM; Estrada, SA; Hofilena, BJ; Smith, BM; Ren, A; Suarez, M; Frazer, J; Edwards, JE; Hart, R; Hauser, EK; Lorea, J; Grottick, AJ Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: discovery of (R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916). Bioorg Med Chem Lett22:71-5 (2011) [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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| BDBM50361233 |
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| n/a |
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| Name | BDBM50361233 |
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| Synonyms: | CHEMBL1934523 |
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| Type | Small organic molecule |
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| Emp. Form. | C23H31NO3S |
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| Mol. Mass. | 401.562 |
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| SMILES | COCCCS(=O)(=O)c1ccc(cc1)-c1ccc(CCN2CCC[C@H]2C)cc1 |r| |
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| Structure | 
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