Reaction Details |
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Target | Histamine H3 receptor |
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Ligand | BDBM27201 |
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Substrate/Competitor | BDBM22530 |
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Meas. Tech. | Radioligand Binding Assay |
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pH | 7.4±n/a |
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Temperature | 298.15±n/a K |
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Ki | 1.66±n/a nM |
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Citation | Zhao, C; Sun, M; Bennani, YL; Gopalakrishnan, SM; Witte, DG; Miller, TR; Krueger, KM; Browman, KE; Thiffault, C; Wetter, J; Marsh, KC; Hancock, AA; Esbenshade, TA; Cowart, MD The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. J Med Chem51:5423-30 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, 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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BDBM27201 |
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BDBM22530 |
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Name | BDBM27201 |
Synonyms: | 4-{methyl[(1R,2S,5S,6S,9R,12S,13R,16S)-6,7,13-trimethyl-7-azapentacyclo[10.8.0.0^{2,9}.0^{5,9}.0^{13,18}]icos-18-en-16-yl]amino}benzonitrile | Conessine analogue, 12g |
Type | Small organic molecule |
Emp. Form. | C30H41N3 |
Mol. Mass. | 443.6666 |
SMILES | [H][C@@]1(C)N(C)C[C@]23CC[C@@]4([H])[C@@]([H])(CC=C5C[C@H](CC[C@]45C)N(C)c4ccc(cc4)C#N)[C@]2([H])CC[C@]13[H] |r,t:14| |
Structure |
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