| Reaction Details |
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 | Report a problem with these data |
| Target | Histamine H3 receptor |
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| Ligand | BDBM26226 |
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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 | 933±130 nM |
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| Citation |  Liu, H; Altenbach, RJ; Carr, TL; Chandran, P; Hsieh, GC; Lewis, LG; Manelli, AM; Milicic, I; Marsh, KC; Miller, TR; Strakhova, MI; Vortherms, TA; Wakefield, BD; Wetter, JM; Witte, DG; Honore, P; Esbenshade, TA; Brioni, JD; Cowart, MD cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), A New Histamine H4R Antagonist that Blocks Pain Responses against Carrageenan-Induced Hyperalgesia. J Med Chem51:7094-8 (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 |
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| Synonyms: | G-protein coupled receptor 97 | GPCR97 | HH3R | HISTAMINE H3 | HRH3 | HRH3_HUMAN | Histamine H3 receptor (H3) | Histamine H3L | Histamine receptor (H3 and H4) |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 48691.47 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Binding assays were using CHO cells stably expressing hH3R receptors. |
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| Residue: | 445 |
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| Sequence: | MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTS
SAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAA
GPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSV
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSL
AVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR
RAFTKLLCPQKLKIQPHSSLEHCWK
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| BDBM26226 |
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| BDBM22530 |
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| Name | BDBM26226 |
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| Synonyms: | (12S,17S)-6-(piperazin-1-yl)-11-oxa-3,5-diazatetracyclo[8.7.0.0^{2,7}.0^{12,17}]heptadeca-1(10),2(7),3,5-tetraen-4-amine | A-987306 |
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| Type | Small organic molecule |
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| Emp. Form. | C18H25N5O |
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| Mol. Mass. | 327.424 |
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| SMILES | [H][C@]12CCCC[C@@]1([H])C1=C(CCc3c(nc(N)nc13)N1CCNCC1)O2 |r,t:9| |
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| Structure | 
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