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Target
Histamine H3 receptor
Ligand
BDBM50199607
Substrate
n/a
Meas. Tech.
ChEMBL_453434 (CHEMBL885433)
Ki
6.9±n/a nM
Citation
 Letavic, MA; Keith, JM; Jablonowski, JA; Stocking, EM; Gomez, LA; Ly, KS; Miller, JM; Barbier, AJ; Bonaventure, P; Boggs, JD; Wilson, SJ; Miller, KL; Lord, B; McAllister, HM; Tognarelli, DJ; Wu, J; Abad, MC; Schubert, C; Lovenberg, TW; Carruthers, 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:
BDBM50199607
Synonyms:
(R)-4-(4-methoxyphenyl)-2-methyl-7-(3-((S)-3-methylmorpholino)propoxy)-1,2,3,4-tetrahydroisoquinoline | CHEMBL247161
Type:
Small organic molecule
Emp. Form.:
C25H34N2O3
Mol. Mass.:
410.5491
SMILES:
COc1ccc(cc1)[C@H]1CN(C)Cc2cc(OCCCN3CCOC[C@@H]3C)ccc12
Structure:
Search PDB for entries with ligand similarity: