Target
Histamine H3 receptor
Ligand
BDBM50224191
Substrate
n/a
Meas. Tech.
ChEMBL_634304 (CHEMBL1120717)
Ki
0.19±n/a nM
Citation
 Liu, HAltenbach, RJDiaz, GJManelli, AMMartin, RLMiller, TREsbenshade, TABrioni, JDCowart, MD In vitro studies on a class of quinoline containing histamine H3 antagonists. Bioorg Med Chem Lett 20:3295-300 (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:
BDBM50224191
Synonyms:
(R)-2-(1-(6-ethoxypyridazin-3-yl)-5-methyl-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline | 2-[1-(6-ethoxypyridazin-3-yl)-5-methyl-1H-pyrazol-4-yl]-6-[2-(2-(R)-methylpyrrolidin-1-yl)ethyl]quinoline | CHEMBL237394
Type:
Small organic molecule
Emp. Form.:
C26H30N6O
Mol. Mass.:
442.556
SMILES:
CCOc1ccc(nn1)-n1ncc(c1C)-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1
Structure:
Search PDB for entries with ligand similarity: