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Target
Histamine H3 receptor
Ligand
BDBM50371289
Substrate
n/a
Meas. Tech.
ChEMBL_463175 (CHEMBL948189)
Ki
0.8±n/a nM
Citation
 Ly, KS; Letavic, MA; Keith, JM; Miller, JM; Stocking, EM; Barbier, AJ; Bonaventure, P; Lord, B; Jiang, X; Boggs, JD; Dvorak, L; Miller, KL; Nepomuceno, D; Wilson, SJ; Carruthers, NI Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors. Bioorg Med Chem Lett 18:39-43 (2008) [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:
BDBM50371289
Synonyms:
CHEMBL258349
Type:
Small organic molecule
Emp. Form.:
C23H28FN3O2
Mol. Mass.:
397.4857
SMILES:
CNCc1cc(ccc1Oc1ccc(F)cc1)C(=O)N1CCCN(CC1)C1CC1
Structure:
Search PDB for entries with ligand similarity: