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Target
Histamine H3 receptor
Ligand
BDBM50139391
Substrate
n/a
Meas. Tech.
ChEMBL_450591 (CHEMBL900877)
EC50
1.29±n/a nM
Citation
 Altenbach, RJ; Liu, H; Banfor, PN; Browman, KE; Fox, GB; Fryer, RM; Komater, VA; Krueger, KM; Marsh, K; Miller, TR; Pan, JB; Pan, L; Sun, M; Thiffault, C; Wetter, J; Zhao, C; Zhou, D; Esbenshade, TA; Hancock, AA; Cowart, MD Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists. J Med Chem 50:5439-48 (2007) [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:
BDBM50139391
Synonyms:
(R)-4-(2-(2-(2-methylpyrrolidin-1-yl)ethyl)benzofuran-5-yl)benzonitrile | 4-{2-[2-((R)-2-Methyl-pyrrolidin-1-yl)-ethyl]-benzofuran-5-yl}-benzonitrile | ABT-239 | CHEMBL351231
Type:
Small organic molecule
Emp. Form.:
C22H22N2O
Mol. Mass.:
330.4229
SMILES:
C[C@@H]1CCCN1CCc1cc2cc(ccc2o1)-c1ccc(cc1)C#N |r|
Structure:
Search PDB for entries with ligand similarity: