Reaction Details |
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Target | Histamine H3 receptor |
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Ligand | BDBM50293623 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_571442 (CHEMBL1032753) |
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IC50 | 180±n/a nM |
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Citation | Kennedy, JP; Conn, PJ; Lindsley, CW A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin. Bioorg Med Chem Lett19:3204-8 (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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BDBM50293623 |
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n/a |
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Name | BDBM50293623 |
Synonyms: | CHEMBL551841 | N-(3-bromo-4-(2-(pyrrolidin-1-yl)ethoxy)phenethyl)-4-bromothiophene-2-carboxamide |
Type | Small organic molecule |
Emp. Form. | C19H22Br2N2O2S |
Mol. Mass. | 502.263 |
SMILES | Brc1csc(c1)C(=O)NCCc1ccc(OCCN2CCCC2)c(Br)c1 |
Structure |
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