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Target
Histamine H4 receptor
Ligand
BDBM22566
Substrate
n/a
Meas. Tech.
ChEMBL_785249 (CHEMBL1921330)
Ki
4.27±n/a nM
Citation
 Mowbray, CE; Bell, AS; Clarke, NP; Collins, M; Jones, RM; Lane, CA; Liu, WL; Newman, SD; Paradowski, M; Schenck, EJ; Selby, MD; Swain, NA; Williams, DH Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist. Bioorg Med Chem Lett 21:6596-602 (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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