Reaction Details |
| Report a problem with these data |
Target | Histamine H4 receptor |
---|
Ligand | BDBM26391 |
---|
Substrate/Competitor | BDBM7966 |
---|
Meas. Tech. | Radioligand Binding Assay |
---|
pH | 7.4±n/a |
---|
Temperature | 298.15±n/a K |
---|
Ki | 26±4 nM |
---|
Citation | Cowart, MD; Altenbach, RJ; Liu, H; Hsieh, GC; Drizin, I; Milicic, I; Miller, TR; Witte, DG; Wishart, N; Fix-Stenzel, SR; McPherson, MJ; Adair, RM; Wetter, JM; Bettencourt, BM; Marsh, KC; Sullivan, JP; Honore, P; Esbenshade, TA; Brioni, JD Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. J Med Chem51:6547-57 (2008) [PubMed] Article |
---|
More Info.: | Get all data from this article, Solution Info, Assay Method |
---|
|
Histamine H4 receptor |
---|
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
|
|
|
BDBM26391 |
---|
BDBM7966 |
---|
Name | BDBM26391 |
Synonyms: | 5-chloro-2-(piperazin-1-ylcarbonyl)-1H-indole | JNJ 7777120 analogue, 4 |
Type | Small organic molecule |
Emp. Form. | C13H14ClN3O |
Mol. Mass. | 263.723 |
SMILES | Clc1ccc2[nH]c(cc2c1)C(=O)N1CCNCC1 |
Structure |
|