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Target
Histamine H3 receptor
Ligand
BDBM50321467
Substrate
n/a
Meas. Tech.
ChEMBL_640775 (CHEMBL1175767)
Ki
1.4±n/a nM
Citation
 Letavic, MA; Aluisio, L; Atack, JR; Bonaventure, P; Carruthers, NI; Dugovic, C; Everson, A; Feinstein, MA; Fraser, IC; Hoey, K; Jiang, X; Keith, JM; Koudriakova, T; Leung, P; Lord, B; Lovenberg, TW; Ly, KS; Morton, KL; Motley, ST; Nepomuceno, D; Rizzolio, M; Rynberg, R; Sepassi, K; Shelton, J Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development. Bioorg Med Chem Lett 20:4210-4 (2010) [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:
BDBM50321467
Synonyms:
(4-cyclobutyl-1,4-diazepan-1-yl)(6-(4-fluorophenoxy)pyridin-3-yl)methanone | CHEMBL1171754
Type:
Small organic molecule
Emp. Form.:
C21H24FN3O2
Mol. Mass.:
369.4326
SMILES:
Fc1ccc(Oc2ccc(cn2)C(=O)N2CCCN(CC2)C2CCC2)cc1
Structure:
Search PDB for entries with ligand similarity: