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Target
Histamine H3 receptor
Ligand
BDBM50198612
Substrate
n/a
Meas. Tech.
ChEMBL_440971 (CHEMBL890061)
Ki
8.7±n/a nM
Citation
 Keith, JM; Gomez, LA; Letavic, MA; Ly, KS; Jablonowski, JA; Seierstad, M; Barbier, AJ; Wilson, SJ; Boggs, JD; Fraser, IC; Mazur, C; Lovenberg, TW; Carruthers, NI Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore. Bioorg Med Chem Lett 17:702-6 (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:
BDBM50198612
Synonyms:
7-(3-(4,4-difluoropiperidin-1-yl)propoxy)-4-(4-methoxyphenyl)-2-methyl-1,2,3,4-tetrahydroisoquinoline | CHEMBL395096
Type:
Small organic molecule
Emp. Form.:
C25H32F2N2O2
Mol. Mass.:
430.5306
SMILES:
COc1ccc(cc1)C1CN(C)Cc2cc(OCCCN3CCC(F)(F)CC3)ccc12 |w:8.8|
Structure:
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