Reaction Details Report a problem with these data
Target
Histamine H4 receptor
Ligand
BDBM22566
Substrate
BDBM7966
Meas. Tech.
Radioligand Binding Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
2.7±0.6 nM
Citation
Altenbach, RJ; Adair, RM; Bettencourt, BM; Black, LA; Fix-Stenzel, SR; Gopalakrishnan, SM; Hsieh, GC; Liu, H; Marsh, KC; McPherson, MJ; Milicic, I; Miller, TR; Vortherms, TA; Warrior, U; Wetter, JM; Wishart, N; Witte, DG; Honore, P; Esbenshade, TA; Hancock, AA; Brioni, JD; Cowart, MD Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands. J Med Chem 51:6571-80 (2008) [PubMed] Article
More Info.:
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