| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Histamine H4 receptor |
|---|
| Ligand | BDBM26398 |
|---|
| Substrate/Competitor | BDBM7966 |
|---|
| Meas. Tech. | Radioligand Binding Assay |
|---|
| pH | 7.4±n/a |
|---|
| Temperature | 298.15±n/a K |
|---|
| Ki | 3.6±0.6 nM |
|---|
| 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 |
|---|
| More Info.: | Get all data from this article, Solution Info, Assay Method |
|---|
| |
| Histamine H4 receptor |
|---|
| 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
|
|
|
|---|
| BDBM26398 |
|---|
| BDBM7966 |
|---|
| Name | BDBM26398 |
|---|
| Synonyms: | 2,4-diamino-5,6-disubstituted pyrimidine, 12 | 6-[3-(methylamino)azetidin-1-yl]-3,5-diazatricyclo[9.4.0.0^{2,7}]pentadeca-1(15),2(7),3,5,11,13-hexaen-4-amine |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C17H21N5 |
|---|
| Mol. Mass. | 295.3821 |
|---|
| SMILES | CNC1CN(C1)c1nc(N)nc-2c1CCCc1ccccc-21 |
|---|
| Structure | 
|
|---|
Search and Browse
