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Target
Histamine H3 receptor
Ligand
BDBM50346209
Substrate
n/a
Meas. Tech.
ChEMBL_749354 (CHEMBL1785144)
Ki
0.21±n/a nM
Citation
 Swanson, DM; Shah, CR; Lord, B; Morton, K; Dvorak, LK; Mazur, C; Apodaca, R; Xiao, W; Boggs, JD; Feinstein, M; Wilson, SJ; Barbier, AJ; Bonaventure, P; Lovenberg, TW; Carruthers, NI Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists. Eur J Med Chem 44:4413-25 (2009) [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:
BDBM50346209
Synonyms:
5-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yloxy)-N-methylpyrazine-2-carboxamide | CHEMBL1783890
Type:
Small organic molecule
Emp. Form.:
C20H24N4O2
Mol. Mass.:
352.4302
SMILES:
CNC(=O)c1cnc(Oc2ccc3CCN(CCc3c2)C2CCC2)cn1
Structure:
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