Reaction Details Report a problem with these data
Target
Histamine H3 receptor
Ligand
BDBM22566
Substrate
BDBM22530
Meas. Tech.
Radioligand Binding Assay
pH
7.5±n/a
Temperature
298.15±n/a K
Ki
4696±304 nM
Citation
Thurmond, RL; Desai, PJ; Dunford, PJ; Fung-Leung, WP; Hofstra, CL; Jiang, W; Nguyen, S; Riley, JP; Sun, S; Williams, KN; Edwards, JP; Karlsson, L A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther 309:404-13 (2004) [PubMed] Article
More Info.:
Target
Name:
Histamine H3 receptor
Synonyms:
HH3R | HRH3_RAT | Hrh3
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
48607.98
Organism:
Rattus norvegicus (rat)
Description:
n/a
Residue:
445
Sequence:
MERAPPDGLMNASGTLAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCASSVFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMALVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGGREAGPEPPPDAQPSPPPAPPSCWGCWPKGHGEAMPLHRYGVGEAGPGVEAGEAALGGGSGGGAAASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSITQRFRLSRDKKVAKSLAIIVSIFGLCWAPYTLLMIIRAACHGRCIPDYWYETSFWLLWANSAVNPVLYPLCHYSFRRAFTKLLCPQKLKVQPHGSLEQCWK
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