Reaction Details |
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Target | Histamine H3 receptor |
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Ligand | BDBM50353170 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_768592 (CHEMBL1832611) |
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Ki | 5.7±n/a nM |
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Citation | Hudkins, RL; Aimone, LD; Bailey, TR; Bendesky, RJ; Dandu, RR; Dunn, D; Gruner, JA; Josef, KA; Lin, YG; Lyons, J; Marcy, VR; Mathiasen, JR; Sundar, BG; Tao, M; Zulli, AL; Raddatz, R; Bacon, ER Identification of pyridazin-3-one derivatives as potent, selective histamine H3 receptor inverse agonists with robust wake activity. Bioorg Med Chem Lett21:5493-7 (2011) [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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BDBM50353170 |
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n/a |
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Name | BDBM50353170 |
Synonyms: | CHEMBL1829468 |
Type | Small organic molecule |
Emp. Form. | C20H24F3N3O2 |
Mol. Mass. | 395.4187 |
SMILES | C[C@@H]1CCCN1CCCOc1ccc(cc1)-c1ccc(=O)n(CC(F)(F)F)n1 |r| |
Structure |
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