Target
Histamine H3 receptor
Ligand
BDBM50217589
Substrate
n/a
Meas. Tech.
ChEMBL_463175 (CHEMBL948189)
Ki
0.7±n/a nM
Citation
 Ly, KSLetavic, MAKeith, JMMiller, JMStocking, EMBarbier, AJBonaventure, PLord, BJiang, XBoggs, JDDvorak, LMiller, KLNepomuceno, DWilson, SJCarruthers, NI Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors. Bioorg Med Chem Lett 18:39-43 (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:
BDBM50217589
Synonyms:
(6S,10bR)-6-(4-methoxyphenyl)-9-(3-(piperidin-1-yl)propoxy)-1,2,3,5,6,10b-hexahydropyrrolo[2,1-a]isoquinoline | CHEMBL235614
Type:
Small organic molecule
Emp. Form.:
C27H36N2O2
Mol. Mass.:
420.5869
SMILES:
COc1ccc(cc1)[C@@H]1CN2CCC[C@@H]2c2cc(OCCCN3CCCCC3)ccc12
Structure:
Search PDB for entries with ligand similarity: