Target
Histamine H3 receptor
Ligand
BDBM50186275
Substrate
n/a
Meas. Tech.
ChEMBL_370710 (CHEMBL867233)
Ki
12.1±n/a nM
Citation
 Jesudason, CDBeavers, LSCramer, JWDill, JFinley, DRLindsley, CWStevens, FCGadski, RAOldham, SWPickard, RTSiedem, CSSindelar, DKSingh, AWatson, BMHipskind, PA Synthesis and SAR of novel histamine H3 receptor antagonists. Bioorg Med Chem Lett 16:3415-8 (2006) [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:
BDBM50186275
Synonyms:
3-(methylsulfonyl)-7-(3-(piperidin-1-yl)propoxy)-2,3,4,5-tetrahydro-1H-benzo[d]azepine | CHEMBL209120
Type:
Small organic molecule
Emp. Form.:
C19H30N2O3S
Mol. Mass.:
366.518
SMILES:
CS(=O)(=O)N1CCc2ccc(OCCCN3CCCCC3)cc2CC1
Structure:
Search PDB for entries with ligand similarity: