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Reaction Details
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TargetHistamine H4 receptor
LigandBDBM22872
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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BDBM22872
BDBM7966
NameBDBM22872
Synonyms:1-(3-chloro-5,6-dihydrobenzo[b][1]benzothiepin-5-yl)-4-methyl-piperazine;maleate | 1-(8-chloro-10,11-dihydrodibenzo[b,f]thiepin-10-yl)-4-methylpiperazine | 1-{6-chloro-2-thiatricyclo[9.4.0.0^{3,8}]pentadeca-1(15),3(8),4,6,11,13-hexaen-9-yl}-4-methylpiperazine | CHEMBL64249 | CLOROTEPINE (+) | CLOROTEPINE(-) | Clothepin | OCTOCLOTHEPIN,(+) | OCTOCLOTHEPIN,(-) | Octoclothepin | Octoclothepine
TypeSmall organic molecule
Emp. Form.C19H21ClN2S
Mol. Mass.344.901
SMILESCN1CCN(CC1)C1Cc2ccccc2Sc2ccc(Cl)cc12
Structure
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