| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Histamine H4 receptor |
|---|
| Ligand | BDBM22877 |
|---|
| Substrate/Competitor | BDBM7966 |
|---|
| Meas. Tech. | H4R Radioligand Binding Assay |
|---|
| pH | 7.4±n/a |
|---|
| Temperature | 310.15±n/a K |
|---|
| Ki | >10000 ±n/a nM |
|---|
| Comments | Analysis of the [3H]histamine saturation binding yielded a Kd value of 11 +/- 1 and a Bmax value of 1.8 +/- 0.4 pmol/mg protein. |
|---|
| Citation |  Lim, HD; van Rijn, RM; Ling, P; Bakker, RA; Thurmond, RL; Leurs, R Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther314:1310-21 (2005) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
|---|
| |
| Histamine H4 receptor |
|---|
| Name: | Histamine H4 receptor |
|---|
| 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 |
|---|
| Type: | G Protein-Coupled Receptor (GPCR) |
|---|
| Mol. Mass.: | 44517.02 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | Binding assays were using CHO cells stably expressing hH4R receptors. |
|---|
| Residue: | 390 |
|---|
| Sequence: | MPDTNSTINLSLSTRVTLAFFMSLVAFAIMLGNALVILAFVVDKNLRHRSSYFFLNLAIS
DFFVGVISIPLYIPHTLFEWDFGKEICVFWLTTDYLLCTASVYNIVLISYDRYLSVSNAV
SYRTQHTGVLKIVTLMVAVWVLAFLVNGPMILVSESWKDEGSECEPGFFSEWYILAITSF
LEFVIPVILVAYFNMNIYWSLWKRDHLSRCQSHPGLTAVSSNICGHSFRGRLSSRRSLSA
STEVPASFHSERQRRKSSLMFSSRTKMNSNTIASKMGSFSQSDSVALHQREHVELLRARR
LAKSLAILLGVFAVCWAPYSLFTIVLSFYSSATGPKSVWYRIAFWLQWFNSFVNPLLYPL
CHKRFQKAFLKIFCIKKQPLPSQHSRSVSS
|
|
|
|---|
| BDBM22877 |
|---|
| BDBM7966 |
|---|
| Name | BDBM22877 |
|---|
| Synonyms: | 2-((1-(1-(4-fluorobenzyl)-1H-benzo[d]imidazol-2-yl)piperidin-4-yl)(methyl)amino)pyrimidin-4(3H)-one | 2-({1-[1-(4-Fluoro-benzyl)-1H-benzoimidazol-2-yl]-piperidin-4-yl}-methyl-amino)-3H-pyrimidin-4-one | 2-({1-[3-(4-Fluoro-benzyl)-1H-benzoimidazol-2-yl]-piperidin-4-yl}-methyl-amino)-2,3-dihydro-1H-pyrimidin-4-one(Mizolastine) | 2-[(1-{1-[(4-fluorophenyl)methyl]-1H-1,3-benzodiazol-2-yl}piperidin-4-yl)(methyl)amino]-3,4-dihydropyrimidin-4-one | CHEMBL94454 | Mizolastine | Mizollen | Zolistan |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C24H25FN6O |
|---|
| Mol. Mass. | 432.4933 |
|---|
| SMILES | CN(C1CCN(CC1)c1nc2ccccc2n1Cc1ccc(F)cc1)c1nccc(=O)[nH]1 |
|---|
| Structure | 
|
|---|
Search and Browse
