Target
Histamine H3 receptor
Ligand
BDBM50276977
Substrate
n/a
Meas. Tech.
ChEMBL_540492 (CHEMBL1030596)
Ki
4.9±n/a nM
Citation
 von Coburg, YKottke, TWeizel, LLigneau, XStark, H Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. Bioorg Med Chem Lett 19:538-42 (2008) [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:
BDBM50276977
Synonyms:
CHEMBL457957 | N-[3-(10,11-Dihydro-dibenzo[a,d]cyclohepten-5-ylidene)-propyl]-N-methyl-2-[4-(3-piperidin-1-yl-propoxy)-phenyl]-acetamide
Type:
Small organic molecule
Emp. Form.:
C35H42N2O2
Mol. Mass.:
522.7202
SMILES:
[#6]-[#7](-[#6]-[#6]\[#6]=[#6]-1/c2ccccc2-[#6]-[#6]-c2ccccc-12)-[#6](=O)-[#6]-c1ccc(-[#8]-[#6]-[#6]-[#6]-[#7]-2-[#6]-[#6]-[#6]-[#6]-[#6]-2)cc1
Structure:
Search PDB for entries with ligand similarity: