Target
Histamine H3 receptor
Ligand
BDBM26230
Substrate
BDBM22530
Meas. Tech.
Radioligand Binding Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
120±19 nM
Citation
 Altenbach, RJAdair, RMBettencourt, BMBlack, LAFix-Stenzel, SRGopalakrishnan, SMHsieh, GCLiu, HMarsh, KCMcPherson, MJMilicic, IMiller, TRVortherms, TAWarrior, UWetter, JMWishart, NWitte, DGHonore, PEsbenshade, TAHancock, AABrioni, JDCowart, 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:
BDBM26230
Synonyms:
2-Aminopyrimidine analog., 25 | 4-[2-amino-6-(piperazin-1-yl)pyrimidin-4-yl]benzonitrile | JMC516547 Compound 5
Type:
Small organic molecule
Emp. Form.:
C15H16N6
Mol. Mass.:
280.3277
SMILES:
Nc1nc(cc(n1)-c1ccc(cc1)C#N)N1CCNCC1
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: