Reaction Details |
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Target | Histamine H3 receptor |
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Ligand | BDBM50216247 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_456606 (CHEMBL923983) |
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Ki | 3±n/a nM |
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Citation | Keith, JM; Gomez, LA; Barbier, AJ; Wilson, SJ; Boggs, JD; Lord, B; Mazur, C; Aluisio, L; Lovenberg, TW; Carruthers, NI Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors. Bioorg Med Chem Lett17:4374-7 (2007) [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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BDBM50216247 |
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n/a |
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Name | BDBM50216247 |
Synonyms: | (6S,10bR)-9-(3-morpholinopropoxy)-6-(thiophen-2-yl)-1,2,3,5,6,10b-hexahydropyrrolo[2,1-a]isoquinoline | CHEMBL246927 |
Type | Small organic molecule |
Emp. Form. | C23H30N2O2S |
Mol. Mass. | 398.562 |
SMILES | C(COc1ccc2[C@@H](CN3CCC[C@@H]3c2c1)c1cccs1)CN1CCOCC1 |
Structure |
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