Target
Histamine H3 receptor
Ligand
BDBM22909
Substrate
BDBM22530
Meas. Tech.
H3R Radioligand Binding Assay
Ki
1±n/a nM
Citation
 Lim, HDvan Rijn, RMLing, PBakker, RAThurmond, RLLeurs, R Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther 314:1310-21 (2005) [PubMed]  Article 
Target
Name:
Histamine H3 receptor
Synonyms:
G-protein coupled receptor 97 | GPCR97 | HH3R | HISTAMINE H3 | HRH3 | HRH3_HUMAN | Histamine H3 receptor (H3) | Histamine H3L | Histamine receptor (H3 and H4)
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
48691.47
Organism:
Homo sapiens (Human)
Description:
Binding assays were using CHO cells stably expressing hH3R receptors.
Residue:
445
Sequence:
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTSSAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAAGPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSVASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSLAVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFRRAFTKLLCPQKLKIQPHSSLEHCWK
  
Inhibitor
Name:
BDBM22909
Synonyms:
4-(1H-imidazol-5-ylmethyl)-1-methylpiperidine | Methimepip
Type:
Small organic molecule
Emp. Form.:
C10H17N3
Mol. Mass.:
179.2621
SMILES:
CN1CCC(Cc2cnc[nH]2)CC1
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: