Target
Histamine H3 receptor
Ligand
BDBM50198588
Substrate
n/a
Meas. Tech.
ChEMBL_453434 (CHEMBL885433)
Ki
3.8±n/a nM
Citation
 Letavic, MAKeith, JMJablonowski, JAStocking, EMGomez, LALy, KSMiller, JMBarbier, AJBonaventure, PBoggs, JDWilson, SJMiller, KLLord, BMcAllister, HMTognarelli, DJWu, JAbad, MCSchubert, CLovenberg, TWCarruthers, NI Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors. Bioorg Med Chem Lett 17:1047-51 (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:
BDBM50198588
Synonyms:
4-(4-methoxyphenyl)-2-methyl-7-(3-morpholinopropoxy)-1,2,3,4-tetrahydroisoquinoline | CHEMBL233053
Type:
Small organic molecule
Emp. Form.:
C24H32N2O3
Mol. Mass.:
396.5225
SMILES:
COc1ccc(cc1)C1CN(C)Cc2cc(OCCCN3CCOCC3)ccc12 |w:8.8|
Structure:
Search PDB for entries with ligand similarity: