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Target
Histamine H4 receptor
Ligand
BDBM26391
Substrate
BDBM7966
Meas. Tech.
Radioligand Binding Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
4±1 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:
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:
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: