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Target
Histamine H3 receptor
Ligand
BDBM50206218
Substrate
n/a
Meas. Tech.
ChEMBL_454704 (CHEMBL886726)
Ki
2.50±n/a nM
Citation
 Keith, JM; Gomez, LA; Wolin, RL; Barbier, AJ; Wilson, SJ; Boggs, JD; Mazur, C; Fraser, IC; Lord, B; Aluisio, L; Lovenberg, TW; Carruthers, NI Pyrrolidino-tetrahydroisoquinolines as potent dual H3 antagonist and serotonin transporter inhibitors. Bioorg Med Chem Lett 17:2603-7 (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:
BDBM50206218
Synonyms:
6-(4-methoxyphenyl)-9-(3-(piperidin-1-yl)propoxy)-1,2,3,5,6,10b-hexahydropyrrolo[2,1-a]isoquinoline | CHEMBL393516
Type:
Small organic molecule
Emp. Form.:
C27H36N2O2
Mol. Mass.:
420.5869
SMILES:
COc1ccc(cc1)C1CN2CCCC2c2cc(OCCCN3CCCCC3)ccc12 |w:14.14,8.8|
Structure:
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