Reaction Details Report a problem with these data
Target
Histamine H3 receptor
Ligand
BDBM22566
Substrate
BDBM22530
Meas. Tech.
Radioligand Binding Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
1318±260 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 
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
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM22530
Synonyms:
N(alpha)-Methylhistamine | N-alpha-methylhistamine | N-methylhistamine | NAMH | [2-(1H-imidazol-5-yl)ethyl](methyl)amine | [3H]N-alpha-methyl histamine
Type:
radiolabeled ligand
Emp. Form.:
C6H11N3
Mol. Mass.:
125.1716
SMILES:
CNCCc1cnc[nH]1
Structure:
Search PDB for entries with ligand similarity: