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Target
Histamine H3 receptor
Ligand
BDBM50174613
Substrate
n/a
Meas. Tech.
ChEMBL_320916 (CHEMBL881343)
Ki
0.13±n/a nM
Citation
 Sun, M; Zhao, C; Gfesser, GA; Thiffault, C; Miller, TR; Marsh, K; Wetter, J; Curtis, M; Faghih, R; Esbenshade, TA; Hancock, AA; Cowart, M Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency. J Med Chem 48:6482-90 (2005) [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:
BDBM50174613
Synonyms:
4-({2-[2-((R)-2-Methyl-pyrrolidin-1-yl)-ethyl]-benzofuran-5-ylmethyl}-amino)-pyridine-2,6-dicarbonitrile | CHEMBL194506
Type:
Small organic molecule
Emp. Form.:
C23H23N5O
Mol. Mass.:
385.4616
SMILES:
C[C@@H]1CCCN1CCc1cc2cc(CNc3cc(nc(c3)C#N)C#N)ccc2o1
Structure:
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