Reaction Details |
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Target | Histamine H3 receptor |
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Ligand | BDBM50448290 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1293783 (CHEMBL3123355) |
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Ki | 6.7±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 |
Synonyms: | HH3R | HRH3_RAT | Hrh3 |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 48607.98 |
Organism: | Rattus norvegicus (rat) |
Description: | n/a |
Residue: | 445 |
Sequence: | MERAPPDGLMNASGTLAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCAS
SVFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMALVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGGREAG
PEPPPDAQPSPPPAPPSCWGCWPKGHGEAMPLHRYGVGEAGPGVEAGEAALGGGSGGGAA
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSITQRFRLSRDKKVAKSL
AIIVSIFGLCWAPYTLLMIIRAACHGRCIPDYWYETSFWLLWANSAVNPVLYPLCHYSFR
RAFTKLLCPQKLKVQPHGSLEQCWK
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BDBM50448290 |
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n/a |
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Name | BDBM50448290 |
Synonyms: | CHEMBL3121100 |
Type | Small organic molecule |
Emp. Form. | C26H28FN3O2 |
Mol. Mass. | 433.5178 |
SMILES | Fc1ccc(cc1)N1N=C(C2CC2C1=O)c1ccc(OC2CCN(CC2)C2CCC2)cc1 |c:9| |
Structure |
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