| Reaction Details |
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 | Report a problem with these data |
| Target | Histamine H4 receptor |
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| Ligand | BDBM26399 |
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| Substrate/Competitor | BDBM7966 |
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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 | 1.45±0.1 nM |
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| Citation |  Cowart, MD; Altenbach, RJ; Liu, H; Hsieh, GC; Drizin, I; Milicic, I; Miller, TR; Witte, DG; Wishart, N; Fix-Stenzel, SR; McPherson, MJ; Adair, RM; Wetter, JM; Bettencourt, BM; Marsh, KC; Sullivan, JP; Honore, P; Esbenshade, TA; Brioni, JD Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. J Med Chem51:6547-57 (2008) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Histamine H4 receptor |
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| Name: | Histamine H4 receptor |
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| Synonyms: | HH4R | HRH4_RAT | Hrh4 |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 44045.07 |
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| Organism: | Rattus norvegicus (rat) |
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| Description: | Cell pellets from SK-N-MC cells transfected with rat H4 receptor were used in binding assay. |
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| Residue: | 391 |
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| Sequence: | MSESNGTDVLPLTAQVPLAFLMSLLAFAITIGNAVVILAFVADRNLRHRSNYFFLNLAIS
DFFVGVISIPLYIPHTLFNWNFGSGICMFWLITDYLLCTASVYSIVLISYDRYQSVSNAV
RYRAQHTGILKIVAQMVAVWILAFLVNGPMILASDSWKNSTNTEECEPGFVTEWYILAIT
AFLEFLLPVSLVVYFSVQIYWSLWKRGSLSRCPSHAGFIATSSRGTGHSRRTGLACRTSL
PGLKEPAASLHSESPRGKSSLLVSLRTHMSGSIIAFKVGSFCRSESPVLHQREHVELLRG
RKLARSLAVLLSAFAICWAPYCLFTIVLSTYRRGERPKSIWYSIAFWLQWFNSLINPFLY
PLCHRRFQKAFWKILCVTKQPAPSQTQSVSS
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| BDBM26399 |
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| BDBM7966 |
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| Name | BDBM26399 |
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| Synonyms: | 14-fluoro-6-(piperazin-1-yl)-3,5-diazatricyclo[9.4.0.0^{2,7}]pentadeca-1(15),2(7),3,5,11,13-hexaen-4-amine | 2,4-diamino-5,6-disubstituted pyrimidine, 13 |
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| Type | Small organic molecule |
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| Emp. Form. | C17H20FN5 |
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| Mol. Mass. | 313.3726 |
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| SMILES | Nc1nc(N2CCNCC2)c2CCCc3ccc(F)cc3-c2n1 |
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| Structure | 
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