Reaction Details |
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Target | Histamine H3 receptor |
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Ligand | BDBM50321506 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_640775 (CHEMBL1175767) |
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Ki | 18±n/a nM |
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Citation | Letavic, MA; Aluisio, L; Atack, JR; Bonaventure, P; Carruthers, NI; Dugovic, C; Everson, A; Feinstein, MA; Fraser, IC; Hoey, K; Jiang, X; Keith, JM; Koudriakova, T; Leung, P; Lord, B; Lovenberg, TW; Ly, KS; Morton, KL; Motley, ST; Nepomuceno, D; Rizzolio, M; Rynberg, R; Sepassi, K; Shelton, J Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development. Bioorg Med Chem Lett20:4210-4 (2010) [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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BDBM50321506 |
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n/a |
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Name | BDBM50321506 |
Synonyms: | (6-(3,4-dichlorophenoxy)pyridin-3-yl)(4-isopropyl-1,4-diazepan-1-yl)methanone | CHEMBL1171935 |
Type | Small organic molecule |
Emp. Form. | C20H23Cl2N3O2 |
Mol. Mass. | 408.322 |
SMILES | CC(C)N1CCCN(CC1)C(=O)c1ccc(Oc2ccc(Cl)c(Cl)c2)nc1 |
Structure |
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