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Target
Histamine H3 receptor
Ligand
BDBM50139303
Substrate
n/a
Meas. Tech.
ChEBML_83645
Ki
9.8±n/a nM
Citation
 Gfesser, GA; Zhang, H; Dinges, J; Fox, GB; Pan, JB; Esbenshade, TA; Yao, BB; Witte, D; Miller, TR; Kang, CH; Krueger, KM; Bennani, YL; Hancock, AA; Faghih, R Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists. Bioorg Med Chem Lett 14:673-6 (2004) [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:
BDBM50139303
Synonyms:
CHEMBL350385 | N-[(R)-2-(4-{3-[4-(5-Cyclopentylmethyl-[1,2,4]oxadiazol-3-yl)-3-fluoro-phenoxy]-propyl}-[1,4]diazepan-1-yl)-1-methyl-2-oxo-ethyl]-4-methoxy-benzamide
Type:
Small organic molecule
Emp. Form.:
C33H42FN5O5
Mol. Mass.:
607.7155
SMILES:
COc1ccc(cc1)C(=O)N[C@H](C)C(=O)N1CCCN(CCCOc2ccc(-c3noc(CC4CCCC4)n3)c(F)c2)CC1
Structure:
Search PDB for entries with ligand similarity: