Reaction Details |
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Target | Histamine H3 receptor |
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Ligand | BDBM50296175 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_579538 (CHEMBL1061547) |
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IC50 | 0.34±n/a nM |
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Citation | Sasaki, T; Takahashi, T; Nagase, T; Mizutani, T; Ito, S; Mitobe, Y; Miyamoto, Y; Kanesaka, M; Yoshimoto, R; Tanaka, T; Takenaga, N; Tokita, S; Sato, N Synthesis, structure-activity relationships, and biological profiles of a dihydrobenzoxathiin class of histamine H(3) receptor inverse agonists. Bioorg Med Chem Lett19:4232-6 (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 |
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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BDBM50296175 |
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n/a |
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Name | BDBM50296175 |
Synonyms: | (+/-)-1-{3-[4-(8-Methoxy-3-methyl-4,4-dioxo-3,4-dihydro-2H-4lambda*6*-benzo[1,4]oxathiin-2-yl)-phenoxy]-propyl}-piperidine | CHEMBL550050 |
Type | Small organic molecule |
Emp. Form. | C24H31NO5S |
Mol. Mass. | 445.572 |
SMILES | COc1cccc2c1OC(C(C)S2(=O)=O)c1ccc(OCCCN2CCCCC2)cc1 |
Structure |
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