Reaction Details |
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Target | Histamine H4 receptor |
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Ligand | BDBM22566 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_785117 (CHEMBL1920855) |
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Ki | 8±n/a nM |
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Citation | Mowbray, CE; Bell, AS; Clarke, NP; Collins, M; Jones, RM; Lane, CA; Liu, WL; Newman, SD; Paradowski, M; Schenck, EJ; Selby, MD; Swain, NA; Williams, DH Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist. Bioorg Med Chem Lett21:6596-602 (2011) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Histamine H4 receptor |
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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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BDBM22566 |
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n/a |
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Name | BDBM22566 |
Synonyms: | 5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-indole | CHEMBL129198 | JNJ 7777120 |
Type | Small organic molecule |
Emp. Form. | C14H16ClN3O |
Mol. Mass. | 277.749 |
SMILES | CN1CCN(CC1)C(=O)c1cc2cc(Cl)ccc2[nH]1 |
Structure |
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