Reaction Details |
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Target | Histamine H4 receptor |
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Ligand | BDBM50356888 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_785118 (CHEMBL1920856) |
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Ki | 10±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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BDBM50356888 |
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n/a |
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Name | BDBM50356888 |
Synonyms: | CHEMBL1915348 |
Type | Small organic molecule |
Emp. Form. | C15H17F2N5 |
Mol. Mass. | 305.3258 |
SMILES | CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2cc(F)c(F)cc2[nH]1 |r| |
Structure |
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