Reaction Details |
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Target | Histamine H4 receptor |
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Ligand | BDBM26229 |
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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 | 275±35 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 |
Synonyms: | HH4R | HRH4_RAT | Hrh4 |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 44045.07 |
Organism: | Rattus norvegicus (rat) |
Description: | Cell pellets from SK-N-MC cells transfected with rat H4 receptor were used in binding assay. |
Residue: | 391 |
Sequence: | MSESNGTDVLPLTAQVPLAFLMSLLAFAITIGNAVVILAFVADRNLRHRSNYFFLNLAIS
DFFVGVISIPLYIPHTLFNWNFGSGICMFWLITDYLLCTASVYSIVLISYDRYQSVSNAV
RYRAQHTGILKIVAQMVAVWILAFLVNGPMILASDSWKNSTNTEECEPGFVTEWYILAIT
AFLEFLLPVSLVVYFSVQIYWSLWKRGSLSRCPSHAGFIATSSRGTGHSRRTGLACRTSL
PGLKEPAASLHSESPRGKSSLLVSLRTHMSGSIIAFKVGSFCRSESPVLHQREHVELLRG
RKLARSLAVLLSAFAICWAPYCLFTIVLSTYRRGERPKSIWYSIAFWLQWFNSLINPFLY
PLCHRRFQKAFWKILCVTKQPAPSQTQSVSS
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BDBM26229 |
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BDBM7966 |
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Name | BDBM26229 |
Synonyms: | 2-Aminopyrimidine analog., 4 | 4-[2-amino-6-(4-methylpiperazin-1-yl)pyrimidin-4-yl]benzonitrile | JMC516547 Compound 2 |
Type | Small organic molecule |
Emp. Form. | C16H18N6 |
Mol. Mass. | 294.3543 |
SMILES | CN1CCN(CC1)c1cc(nc(N)n1)-c1ccc(cc1)C#N |
Structure |
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