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Reaction Details
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TargetHistamine H4 receptor
LigandBDBM22877
Substrate/CompetitorBDBM7966
Meas. Tech.H4R Radioligand Binding Assay
pH7.4±n/a
Temperature310.15±n/a K
Ki>10000 ±n/a nM
CommentsAnalysis 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 HDvan Rijn RMLing PBakker RAThurmond RLLeurs 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 Ther 314:1310-21 (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 | GPRv53 | HH4R | HISTAMINE H4 | 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
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BDBM22877
BDBM7966
NameBDBM22877
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 | Mizolastine | Mizollen | Zolistan
TypeSmall organic molecule
Emp. Form.C24H25FN6O
Mol. Mass.432.4933
SMILESCN(C1CCN(CC1)c1nc2ccccc2n1Cc1ccc(F)cc1)c1nccc(=O)[nH]1
Structure
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