Reaction Details |
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Target | Histamine H3 receptor |
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Ligand | BDBM50243674 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_491620 (CHEMBL945391) |
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Ki | 4±n/a nM |
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Citation | Santora, VJ; Covel, JA; Hayashi, R; Hofilena, BJ; Ibarra, JB; Pulley, MD; Weinhouse, MI; Semple, G; Ren, A; Pereira, G; Edwards, JE; Suarez, M; Frazer, J; Thomsen, W; Hauser, E; Lorea, J; Grottick, AJ Novel H3 receptor antagonists with improved pharmacokinetic profiles. Bioorg Med Chem Lett18:4133-6 (2008) [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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BDBM50243674 |
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n/a |
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Name | BDBM50243674 |
Synonyms: | ((3aR,6aR)-6-(4-(2-((R)-2-methylpyrrolidin-1-yl)ethyl)phenyl)-1,3a,4,6a-tetrahydrocyclopenta[c]pyrrol-2(1H)-yl)(tetrahydro-2H-pyran-4-yl)methanone | CHEMBL471555 |
Type | Small organic molecule |
Emp. Form. | C26H36N2O2 |
Mol. Mass. | 408.5762 |
SMILES | C[C@@H]1CCCN1CCc1ccc(cc1)C1=CC[C@H]2CN(C[C@@H]12)C(=O)C1CCOCC1 |r,t:16| |
Structure |
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