Reaction Details |
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Target | Histamine H3 receptor |
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Ligand | BDBM50293632 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_571442 (CHEMBL1032753) |
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IC50 | 2110±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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BDBM50293632 |
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n/a |
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Name | BDBM50293632 |
Synonyms: | 4-bromo-N-(3-bromo-4-(2-(3-fluoropyrrolidin-1-yl)ethoxy)phenethyl)-4-bromothiophene-2-carboxamide | 4-bromo-N-(3-bromo-4-(2-(3-fluoropyrrolidin-1-yl)ethoxy)phenethyl)thiophene-2-carboxamide | CHEMBL562496 |
Type | Small organic molecule |
Emp. Form. | C19H21Br2FN2O2S |
Mol. Mass. | 520.254 |
SMILES | FC1CCN(CCOc2ccc(CCNC(=O)c3cc(Br)cs3)cc2Br)C1 |
Structure |
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