Reaction Details |
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Target | Histamine H4 receptor |
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Ligand | BDBM50315318 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_625969 (CHEMBL1103488) |
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IC50 | 169±n/a nM |
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Citation | Cramp, S; Dyke, HJ; Higgs, C; Clark, DE; Gill, M; Savy, P; Jennings, N; Price, S; Lockey, PM; Norman, D; Porres, S; Wilson, F; Jones, A; Ramsden, N; Mangano, R; Leggate, D; Andersson, M; Hale, R Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists. Bioorg Med Chem Lett20:2516-9 (2010) [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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BDBM50315318 |
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n/a |
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Name | BDBM50315318 |
Synonyms: | 8-chloro-4-(5-methyl-2,5-diazabicyclo[2.2.2]octan-2-yl)benzofuro[3,2-d]pyrimidine | CHEMBL1092933 |
Type | Small organic molecule |
Emp. Form. | C17H17ClN4O |
Mol. Mass. | 328.796 |
SMILES | CN1CC2CCC1CN2c1ncnc2c1oc1ccc(Cl)cc21 |
Structure |
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