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Target
Histamine H4 receptor
Ligand
BDBM22566
Substrate
n/a
Meas. Tech.
ChEMBL_795784 (CHEMBL1936671)
Ki
6±n/a nM
Citation
 Smits, RA; Lim, HD; van der Meer, T; Kuhne, S; Bessembinder, K; Zuiderveld, OP; Wijtmans, M; de Esch, IJ; Leurs, R Ligand based design of novel histamine H4 receptor antagonists; fragment optimization and analysis of binding kinetics. Bioorg Med Chem Lett 22:461-7 (2011) [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:
BDBM22566
Synonyms:
5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-indole | CHEMBL129198 | JNJ 7777120
Type:
Small organic molecule
Emp. Form.:
C14H16ClN3O
Mol. Mass.:
277.749
SMILES:
CN1CCN(CC1)C(=O)c1cc2cc(Cl)ccc2[nH]1
Structure:
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