Target
Histamine H3 receptor
Ligand
BDBM50209808
Substrate
n/a
Meas. Tech.
ChEMBL_455315 (CHEMBL886091)
Ki
2.7±n/a nM
Citation
 Stocking, EMMiller, JMBarbier, AJWilson, SJBoggs, JDMcAllister, HMWu, JLovenberg, TWCarruthers, NIWolin, RL Synthesis and biological evaluation of diamine-based histamine H3 antagonists with serotonin reuptake inhibitor activity. Bioorg Med Chem Lett 17:3130-5 (2007) [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:
BDBM50209808
Synonyms:
CHEMBL248375 | N,N-dimethyl-3-(4-(3-(piperidin-1-yl)propoxy)phenyl)-3-(4-(trifluoromethyl)phenoxy)propan-1-amine
Type:
Small organic molecule
Emp. Form.:
C26H35F3N2O2
Mol. Mass.:
464.5635
SMILES:
CN(C)CCC(Oc1ccc(cc1)C(F)(F)F)c1ccc(OCCCN2CCCCC2)cc1 |w:5.4|
Structure:
Search PDB for entries with ligand similarity: