Reaction Details |
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Target | Histamine H3 receptor |
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Ligand | BDBM50268452 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_523444 (CHEMBL1008296) |
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Ki | 7±n/a nM |
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Citation | Pierson, PD; Fettes, A; Freichel, C; Gatti-McArthur, S; Hertel, C; Huwyler, J; Mohr, P; Nakagawa, T; Nettekoven, M; Plancher, JM; Raab, S; Richter, H; Roche, O; Rodríguez Sarmiento, RM; Schmitt, M; Schuler, F; Takahashi, T; Taylor, S; Ullmer, C; Wiegand, R 5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity. J Med Chem52:3855-68 (2009) [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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BDBM50268452 |
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n/a |
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Name | BDBM50268452 |
Synonyms: | (4-cyclobutylpiperazin-1-yl)(2-(morpholine-4-carbonyl)-1-(2,2,2-trifluoroethyl)-1H-indol-5-yl)methanone | CHEMBL522739 |
Type | Small organic molecule |
Emp. Form. | C24H29F3N4O3 |
Mol. Mass. | 478.5073 |
SMILES | FC(F)(F)Cn1c(cc2cc(ccc12)C(=O)N1CCN(CC1)C1CCC1)C(=O)N1CCOCC1 |
Structure |
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