Reaction Details |
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Target | Histamine H3 receptor |
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Ligand | BDBM50496270 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1296757 (CHEMBL3132260) |
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IC50 | 1.7±n/a nM |
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Citation | Brown, DG; Bernstein, PR; Griffin, A; Wesolowski, S; Labrecque, D; Tremblay, MC; Sylvester, M; Mauger, R; Edwards, PD; Throner, SR; Folmer, JJ; Cacciola, J; Scott, C; Lazor, LA; Pourashraf, M; Santhakumar, V; Potts, WM; Sydserff, S; Giguère, P; Lévesque, C; Dasser, M; Groblewski, T Discovery of spirofused piperazine and diazepane amides as selective histamine-3 antagonists with in vivo efficacy in a mouse model of cognition. J Med Chem57:733-58 (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: | 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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BDBM50496270 |
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n/a |
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Name | BDBM50496270 |
Synonyms: | CHEMBL3127679 |
Type | Small organic molecule |
Emp. Form. | C21H37N3O2 |
Mol. Mass. | 363.5374 |
SMILES | CC(C)N1CCN(CC1)C(=O)C1CC2(C1)CCN(CC2)C1CCOCC1 |
Structure |
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