Target
Histamine H3 receptor
Ligand
BDBM50383167
Substrate
n/a
Meas. Tech.
ChEMBL_819069 (CHEMBL2034391)
Ki
0.8±n/a nM
Citation
 Zhou, DGross, JLAdedoyin, ABAschmies, SBBrennan, JBowlby, MDi, LKubek, KPlatt, BJWang, ZZhang, GBrandon, NComery, TARobichaud, AJ 2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists. J Med Chem 55:2452-68 (2012) [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:
BDBM50383167
Synonyms:
CHEMBL2031741
Type:
Small organic molecule
Emp. Form.:
C22H24N4O
Mol. Mass.:
360.4522
SMILES:
O=C1N(CCN2CCCC2)CCc2cc(ccc12)-n1cnc2ccccc12
Structure:
Search PDB for entries with ligand similarity: