| Reaction Details |
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 | Report a problem with these data |
| Target | Histamine H4 receptor |
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| Ligand | BDBM26397 |
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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 | 3.5±0.3 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: | AXOR35 | G-protein coupled receptor 105 | GPCR105 | GPRv53 | HH4R | HISTAMINE H4 | HRH4 | HRH4_HUMAN | Histamine H4 receptor | Histamine H4 receptor (H4R) | Histamine receptor (H3 and H4) | Pfi-013 | SP9144 |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 44517.02 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Binding assays were using CHO cells stably expressing hH4R receptors. |
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| Residue: | 390 |
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| Sequence: | MPDTNSTINLSLSTRVTLAFFMSLVAFAIMLGNALVILAFVVDKNLRHRSSYFFLNLAIS
DFFVGVISIPLYIPHTLFEWDFGKEICVFWLTTDYLLCTASVYNIVLISYDRYLSVSNAV
SYRTQHTGVLKIVTLMVAVWVLAFLVNGPMILVSESWKDEGSECEPGFFSEWYILAITSF
LEFVIPVILVAYFNMNIYWSLWKRDHLSRCQSHPGLTAVSSNICGHSFRGRLSSRRSLSA
STEVPASFHSERQRRKSSLMFSSRTKMNSNTIASKMGSFSQSDSVALHQREHVELLRARR
LAKSLAILLGVFAVCWAPYSLFTIVLSFYSSATGPKSVWYRIAFWLQWFNSFVNPLLYPL
CHKRFQKAFLKIFCIKKQPLPSQHSRSVSS
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| BDBM26397 |
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| BDBM7966 |
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| Name | BDBM26397 |
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| Synonyms: | 2,4-diamino-5,6-disubstituted pyrimidine, 11 | 6-[(3R)-3-(methylamino)pyrrolidin-1-yl]-3,5-diazatricyclo[9.4.0.0^{2,7}]pentadeca-1(15),2(7),3,5,11,13-hexaen-4-amine |
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| Type | Small organic molecule |
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| Emp. Form. | C18H23N5 |
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| Mol. Mass. | 309.4087 |
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| SMILES | CN[C@@H]1CCN(C1)c1nc(N)nc-2c1CCCc1ccccc-21 |r| |
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| Structure | 
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