Reaction Details Report a problem with these data
Target
Histamine H4 receptor
Ligand
BDBM26394
Substrate
BDBM7966
Meas. Tech.
Radioligand Binding Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
13±0.8 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 Chem 51:6547-57 (2008) [PubMed] Article
More Info.:
Target
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:
MPDTNSTINLSLSTRVTLAFFMSLVAFAIMLGNALVILAFVVDKNLRHRSSYFFLNLAISDFFVGVISIPLYIPHTLFEWDFGKEICVFWLTTDYLLCTASVYNIVLISYDRYLSVSNAVSYRTQHTGVLKIVTLMVAVWVLAFLVNGPMILVSESWKDEGSECEPGFFSEWYILAITSFLEFVIPVILVAYFNMNIYWSLWKRDHLSRCQSHPGLTAVSSNICGHSFRGRLSSRRSLSASTEVPASFHSERQRRKSSLMFSSRTKMNSNTIASKMGSFSQSDSVALHQREHVELLRARRLAKSLAILLGVFAVCWAPYSLFTIVLSFYSSATGPKSVWYRIAFWLQWFNSFVNPLLYPLCHKRFQKAFLKIFCIKKQPLPSQHSRSVSS
Inhibitor
Name:
BDBM26394
Synonyms:
2,4-diamino-5,6-disubstituted pyrimidine, 8 | 4-(piperazin-1-yl)-5H-indeno[1,2-d]pyrimidin-2-amine
Type:
Small organic molecule
Emp. Form.:
C15H17N5
Mol. Mass.:
267.329
SMILES:
Nc1nc-2c(Cc3ccccc-23)c(n1)N1CCNCC1