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Target
Histamine H4 receptor
Ligand
BDBM26393
Substrate
BDBM7966
Meas. Tech.
Radioligand Binding Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
9.2±1.2 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 
Target
Name:
Histamine H4 receptor
Synonyms:
HH4R | HRH4_RAT | Hrh4
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
44045.07
Organism:
Rattus norvegicus (rat)
Description:
Cell pellets from SK-N-MC cells transfected with rat H4 receptor were used in binding assay.
Residue:
391
Sequence:
MSESNGTDVLPLTAQVPLAFLMSLLAFAITIGNAVVILAFVADRNLRHRSNYFFLNLAISDFFVGVISIPLYIPHTLFNWNFGSGICMFWLITDYLLCTASVYSIVLISYDRYQSVSNAVRYRAQHTGILKIVAQMVAVWILAFLVNGPMILASDSWKNSTNTEECEPGFVTEWYILAITAFLEFLLPVSLVVYFSVQIYWSLWKRGSLSRCPSHAGFIATSSRGTGHSRRTGLACRTSLPGLKEPAASLHSESPRGKSSLLVSLRTHMSGSIIAFKVGSFCRSESPVLHQREHVELLRGRKLARSLAVLLSAFAICWAPYCLFTIVLSTYRRGERPKSIWYSIAFWLQWFNSLINPFLYPLCHRRFQKAFWKILCVTKQPAPSQTQSVSS
  
Inhibitor
Name:
BDBM26393
Synonyms:
2,4-diamino-5,6-disubstituted pyrimidine, 7 | 6-(piperazin-1-yl)-3,5-diazatricyclo[8.4.0.0^{2,7}]tetradeca-1(14),2,4,6,10,12-hexaen-4-amine
Type:
Small organic molecule
Emp. Form.:
C16H19N5
Mol. Mass.:
281.3556
SMILES:
Nc1nc(N2CCNCC2)c2CCc3ccccc3-c2n1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM7966
Synonyms:
2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 | CHEMBL90 | Ceplene | Ergotidine | HISTAMINE DIHYDROCHLORIDE | Histamine | L-histamine | Peremin | [3H]histamine
Type:
Small organic molecule
Emp. Form.:
C5H9N3
Mol. Mass.:
111.1451
SMILES:
NCCc1cnc[nH]1
Structure:
Search PDB for entries with ligand similarity: