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Target
Histamine H3 receptor
Ligand
BDBM50205668
Substrate
n/a
Meas. Tech.
ChEMBL_454636 (CHEMBL886656)
Ki
12±n/a nM
Citation
 Letavic, MA; Keith, JM; Ly, KS; Barbier, AJ; Boggs, JD; Wilson, SJ; Lord, B; Lovenberg, TW; Carruthers, NI Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors. Bioorg Med Chem Lett 17:2566-9 (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:
BDBM50205668
Synonyms:
4-(4-methoxyphenyl)-2-methyl-7-(3-(piperidin-1-yl)propoxy)-1,2,3,4-tetrahydro-2,6-naphthyridine | CHEMBL238052
Type:
Small organic molecule
Emp. Form.:
C24H33N3O2
Mol. Mass.:
395.5377
SMILES:
COc1ccc(cc1)C1CN(C)Cc2cc(OCCCN3CCCCC3)ncc12 |w:8.8|
Structure:
Search PDB for entries with ligand similarity: