| Reaction Details |
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 | Report a problem with these data |
| Target | Histamine H4 receptor |
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| Ligand | BDBM22872 |
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| Substrate/Competitor | BDBM7966 |
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| Meas. Tech. | H4R Radioligand Binding Assay |
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| pH | 7.4±n/a |
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| Temperature | 310.15±n/a K |
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| Ki | >10000 ±n/a nM |
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| 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. |
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| 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 |
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| More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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| Histamine H4 receptor |
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| Name: | Histamine H4 receptor |
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| 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 |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 44517.02 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Binding assays were using CHO cells stably expressing hH4R receptors. |
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| Residue: | 390 |
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| Sequence: | MPDTNSTINLSLSTRVTLAFFMSLVAFAIMLGNALVILAFVVDKNLRHRSSYFFLNLAIS
DFFVGVISIPLYIPHTLFEWDFGKEICVFWLTTDYLLCTASVYNIVLISYDRYLSVSNAV
SYRTQHTGVLKIVTLMVAVWVLAFLVNGPMILVSESWKDEGSECEPGFFSEWYILAITSF
LEFVIPVILVAYFNMNIYWSLWKRDHLSRCQSHPGLTAVSSNICGHSFRGRLSSRRSLSA
STEVPASFHSERQRRKSSLMFSSRTKMNSNTIASKMGSFSQSDSVALHQREHVELLRARR
LAKSLAILLGVFAVCWAPYSLFTIVLSFYSSATGPKSVWYRIAFWLQWFNSFVNPLLYPL
CHKRFQKAFLKIFCIKKQPLPSQHSRSVSS
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| BDBM22872 |
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| BDBM7966 |
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| Name | BDBM22872 |
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| 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 |
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| Type | Small organic molecule |
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| Emp. Form. | C19H21ClN2S |
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| Mol. Mass. | 344.901 |
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| SMILES | CN1CCN(CC1)C1Cc2ccccc2Sc2ccc(Cl)cc12 |
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| Structure | 
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