| Reaction Details |
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 | Report a problem with these data |
| Target | Histamine H3 receptor |
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| Ligand | BDBM50448285 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1293783 (CHEMBL3123355) |
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| Ki | 5.7±n/a nM |
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| Citation |  Hudkins, RL; Josef, KA; Becknell, NC; Aimone, LD; Lyons, JA; Mathiasen, JR; Gruner, JA; Raddatz, R Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): histamine H(3) receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity. Bioorg Med Chem Lett24:1303-6 (2014) [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: | HH3R | HRH3_RAT | Hrh3 |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 48607.98 |
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| Organism: | Rattus norvegicus (rat) |
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| Description: | n/a |
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| Residue: | 445 |
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| Sequence: | MERAPPDGLMNASGTLAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCAS
SVFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMALVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGGREAG
PEPPPDAQPSPPPAPPSCWGCWPKGHGEAMPLHRYGVGEAGPGVEAGEAALGGGSGGGAA
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSITQRFRLSRDKKVAKSL
AIIVSIFGLCWAPYTLLMIIRAACHGRCIPDYWYETSFWLLWANSAVNPVLYPLCHYSFR
RAFTKLLCPQKLKVQPHGSLEQCWK
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| BDBM50448285 |
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| n/a |
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| Name | BDBM50448285 |
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| Synonyms: | CHEMBL3121093 |
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| Type | Small organic molecule |
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| Emp. Form. | C22H29N3O2 |
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| Mol. Mass. | 367.4846 |
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| SMILES | CN1N=C(C2CC2C1=O)c1ccc(OC2CCN(CC2)C2CCCC2)cc1 |c:2| |
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| Structure | 
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