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Reaction Details
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TargetHistamine H4 receptor
LigandBDBM22567
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 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
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  Blast E-value cutoff:
BDBM22567
BDBM7966
NameBDBM22567
Synonyms:3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramine | N-(4-methoxybenzyl)-N ,N -dimethyl-N-pyridin-2-ylethane-1,2-diamine | N-[2-(dimethylamino)ethyl]-N-[(4-methoxyphenyl)methyl]pyridin-2-amine | PYRILAMINE | Pyranisamine | [3H]mepyramine | [3H]pyrilamine
Typeradiolabeled ligand
Emp. Form.C17H23N3O
Mol. Mass.285.384
SMILESCOc1ccc(CN(CCN(C)C)c2ccccn2)cc1
Structure
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